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    Catalog No. Name Description
    GY03791 New DL-AP4 DL-AP4 is a Broad spectrum EAA antagonist.
    GY03798 New Substance P free acid Substance P free acid is a Sensory neuropeptide and inflammatory mediator. Exerts excitatory effects on central and peripheral neurons, constricts bronchioles and is involved in pain transmission.
    GY03802 New AM 281 AM281 is a potent and selective central cannabinoid (CB1) receptor antagonist/inverse agonist (Ki =12 nM and 4,200 nM for CB1 and CB2, respectively).
    GY03860 New Sarecycline Sarecycline, also known as P005672, is a novel, tetracycline-derived, narrow-spectrum antibiotic being developed for use as an oral once daily antibiotic treatment for patients suffering from moderate to severe acne vulgaris.
    GY03864 New SU 5214 SU 5214 is a modulator of tyrosine kinase signal transduction.
    GY06665 New GS-441524 GS-441524 inhibits replication of serotype II FIP virus (FIPV) in CRFK cell cultures with EC50 of ~1 uM.
    GY03885 New NE-100 Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
    GY03994 New Cambendazol Cambendazol is an antihelmintic that, at a dose of 50 mg/kg/day in mice, eradicates S. ratti adult worms from intestine and S. stercoralis larva from muscle.
    GY03995 New Methylphenidate HCl Methylphenidate hydrochloride is a central nervous system stimulant
    GY04004 New Losartan Carboxylic Acid Losartan carboxylic acid is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver.
    GY04124 New HBX41108 HBX 41108 is an inhibitor of ubiquitin-specific protease (USP) 7 activity (IC50 = 424 nM).
    GY04129 New SRT3025 SRT3025 is a sirt1 activator.
    GY04130 New Tazarotenic acid Tazarotenic acid, an active metabolite of tazarotene, is a potent and selective agonist of the retinoid receptor (RAR) that binds to RARα, RARβ, and RARγ.
    GY04136 New Etelcalcetide HCl Etelcalcetide (AMG 416) is a novel, long-acting selective peptide agonist of the calcium sensing receptor, activates calcium sensing receptor on parathyroid glands reducing PTH synthesis and secretion.
    GY04151 New RN-1 RN-1 (hydrochloride) is a potent and irreversible LSD1 inhibitor with IC50 values of 10-70 nM. However, RN-1 is much less effective against MAO-A and MAO-B with IC50 values of 0.51 and 2.785 μM
    GY04262 New PBIT PBIT is a potent, cell-permeable inhibitor of Jumonji histone demethylase (JHDM). Innhibits JARID1B (also known as KDM5B or PLU1) with an IC50 of about 3 μm in vitro.
    GY04296 New Ximelagatran Ximelagatran is an orally active direct thrombin inhibitor.
    GY04363 New PS-47 PS47 has a E-configuration in comparison with its active Z-isomer PS48.
    GY04365 New LHW090-A7 LHW090-A7 is a potential inhibitor of neutral endopeptidase (NEP).
    GY04503 New Auten-99 Auten-99 is a novel inhibitor of the myotubularin phosphatase Jumpy (also called MTMR14), acrossing the blood-brain barrier and exerting potent neuroprotective effects.
    GY04607 New Beta-guanidinopropionic acid Beta-guanidinopropionic acid is a novel creatine kinase inhibitor.
    GY04625 New DNQX disodiumsalt DNQX is a AMPA receptor antagonists.
    GY04626 New 1-EBIO 1-EBIO is an Epithelial KCa channel activator.
    GY04668 New RGX-104 RGX-104 is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene. RGX-104 depletes myeloid derived suppressor cells (MDSCs) and stimulates dendritic cells (DCs), activating cytotoxic lymphocytes (CTLs) with anti-tumor activity.
    GY04670 New Gefapixant(AF-219,MK-7264) Gefapixant(AF-219,MK-7264) is novel P2X3 receptor antagonist.
    GY05001 New DLin-MC3-DMA D-Lin-MC3-DMA(MC3) is the most potent cationic lipid that has been synthesized for Lipid nanoparticles (LNPs) to deliver the siRNA.
    GY05012 New NAV-2729 NAV-2729 is a dual Arf1/Arf6 activation inhibitor.
    GY05018 New KHS101 KHS101 is primarily found to selectively induce a neuronal differentiation phenotype by interaction with TACC3 protein, with the ability to cross the blood-brain barrier. KHS101 is recently found to promote tumor cell death in diverse glioblastoma multiforme (GBM) cell models, independent of their tumor subtype, and without affecting the viability of noncancerous brain cell lines.
    GY05023 New (-)-CXL017 (-)-CXL017 is a small molecule that has selective cytotoxicity toward MDR cancer cell lines in vitro, through inhibition of the sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA) with IC50 of 13.5 uM.
    GY05024 New (5Z)-7-Oxozeaenol (5Z)-7-Oxozeaenol is a potent and selective TAK1 inhibitor with IC50 of 8 nM, displays >33-fold and >62-fold selectivity over MEKK1 and MEKK4 respectively.
    GY05030 New (R)-Oxiracetam the R-enantiomer of the nootropic drug oxiracetam (ISF 2522), which is a nootropic drug of the racetam family and stimulant..
    GY07313 New RTS-V5 RTS-V5 is the first-in-class dual histone deacetylase-proteasome inhibitor with IC50 of 0.27 µM for HDAC6 and blocks the chymotrypsin-like proteasome activity.
    GY07334 New PC786 PC786 is a potent and selective inhibitor of RSV RNA-dependent RNA polymerase (RdRp).
    GY06916 New DS-8500a DS-8500a is a novel, orally available, selective GPR119 agonist and increases intracellular cAMP in human, rat, and mouse GPR119 expressing CHO-K1 cells with EC50 of 51.5 nM, 98.4 nM and 108.1 nM, respectively.
    GY07287 New GSK2646264 GSK2646264 is a potent and selective spleen tyrosine kinase inhibitor with pIC50 of 7.1 and demonstrates good selectivity (at least 30-fold) against the other kinases (Aurora A, Aurora B, VEGFR2, JAK2, GSK3β, LCK and LRRK2)
    GY07290 New NYX-2925 NYX-2925 is a non-opioid, selective, and central-acting NMDAR modulator.
    GY07279 New AZD3229 AZD3229 is a potent pan-Kit mutant inhibitor and demonstrates potent single digit nM growth inhibition across a broad cell panel, with good margin to KDR-driven effects.
    GY07300 New TUG-1375 TUG-1375 is a potent thiazolidine free fatty acid receptor 2 agonist with pKi of 6.69.
    GY07303 New LY3298176 LY3298176 is a novel dual GIP and GLP-1 receptor agonist with Ki of 0.135 and 4.23, respectively.
    GY07308 New GSK852A GSK852A is a NS5B inhibitor.
    GY07309 New GSK8175 GSK8175 is a NS5B inhibitor.
    GY07316 New TT-10 TT-10 is a novel multifaceted fluorinated compound, which increases cardiomyocytes and protect the heart after ischemic injury.
    GY07317 New GS-441524 Triphosphate Active triphosphate metabolite of GS-441524, which inhibits replication of serotype II FIP virus (FIPV) in CRFK cell cultures with EC50 of ~1 uM.
    GY07318 New NVR 3-778 NVR 3-778 is the first capsid assembly modulator (CAM) that inhibits viral replication (rcDNA formation) and the production of secreted HBV DNA virions in HepG2.2.15 cells with EC50 of 0.34 µM and 0.40 µM, respectively.
    GY07319 New Compound 8 Compound 8 (ZINC05007751) is a novel inhibitor of the NIMA-related kinase with IC50 of 3.4 µM.
    GY07320 New XL-13m XL-13m is an ENL YEATS-selective inhibitor with IC50 of 0.56 μM.
    GY07322 New VU0424238 VU0424238 (Auglurant) is a novel negative allosteric modulator of mGlu5 with Ki of 4.4 nM, which is more than 900-fold selectivity versus the other mGlu receptors.
    GY07323 New VU0652835 VU0652835 is a potent negative allosteric modulator of mGlu5 with excellent CNS penetration.
    GY07324 New PROTAC 15 PROTAC 15 is a novel B-cell lymphoma 6 (BCL6) PROTAC,, which degrades BCL6 across a number of DLBCL cell lines via the expected ubiquitin-proteasome mediated pathway.
    GY07336 New HMG499 HMG499 (HMGCR degrader Cmpd 81) is a potent HMG-CoA reductase degrader with EC50 of 0.41μM.
    GY07337 New PF-06305591 PF-06305591 is a potent highly selective NaV1.8 blocker with IC50 of 15 nM.
    GY07338 New MDI-2268 MDI-2268 is noval oral inhibitor of a plasminogen-activator inhibitor type-1 (PAI-1).
    GY07339 New COH000 COH000 is a highly specific covalent allosteric inhibitor of SUMO E1.
    GY07340 New TD-0212 TD-0212 is an orally active, dual AT1 antagonist/NEP inhibitor (ARNI) with pKi and pIC50 of 8.9 and 9.2, respectively.
    GY03847 Special AN3365 Epetraborole hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor, which inhibits protein synthesis by binding "to the terminal adenosine ribose (A76) of leucyl-tRNA synthetase".
    GY03894 Special GBT-440 GBT 440 is a modulator of sickle hemoglobin (HbS), extracted from patent WO2015116061A1, compound 5, which can be used in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    GY02921 Special NCT-503 NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 µM.
    GY02978 Special WNK463 WNK463 is an orally bioavailable pan-WNK-kinase inhibitor.
    GY03139 Special AVN-944 AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.
    GY03805 Special PTC-028 PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification.
    GY03931 Special Cl-amidine Cl-amidine is an irreversible pan-peptidylarginine deiminase (PAD) inhibitor with IC50 values of 5.9 ± 0.3 μM, 0.8 ± 0.3 μM, 6.2 ± 1.0 μM for PAD4, PAD1 and PAD3, respectively.
    GY03970 Special Alsterpaullone Alsterpaullone is a potent ATP-competitive and cell cycle cyclin-dependent kinase inhibitor, that is reported to be the most active Paullone.
    GY03986 Special 3-Cyano-7-ethoxycoumarin 3-Cyano-7-ethoxycoumarin is a fluorogenic cytochrome P-450 substrate that generates blue fluorescent product upon enzyme cleavage Target.
    GY03996 Special GSK-8573(negative control of GSK-2801) GSK-8573 is the inactive control of GSK-2801.
    GY04024 Special CPI-169(R), EZH2 Inhibitor CPI-169 is a novel and potent EZH2 inhibitor, with IC50s of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
    GY01157 Special RSL3 1S, 3R- RSL3 is the inhibitor of the glutathione (GSH) peroxidase 4, which can inhibit the cysteine/glutamate amino acid transporter system that blocks GSH synthesis with an IC50 of 100 nM.
    GY01560 Special RK-33 RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells.
    GY01584 Special Indirubin (Couroupitine B) Indirubin(Couroupitine B) is a purple 3,2- bisindole and a stable isomer of indigo isolated from Indigo naturalis (Apiaceae); anti-inflammatory and anticancer activities.
    GY01643 Special StemRegenin 1 StemRegenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
    GY01679 Special PFK-015 PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.
    GY01793 Special TH-302 TH-302 is a hypoxia-activated prodrug with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.
    GY02461 Special PBTZ169 PBTZ169 is a new drug candicate that inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043 target: DprE1 In vitro: PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.
    GY03154 Special Glutaminase C-IN-1 Glutaminase C-IN-1 (968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
    GY03547 Special Nicaraven Nicaraven is a novel chemically synthesized hydroxyl radical-specific scavenger.
    GY03662 Special SCH900776 S-isomer SCH900776 S-isomer is the S-isomer of SCH900776. SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with IC50 of 3 nM.
    GY03747 Special Ezutromid Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
    GY04085 Special CPHPC Miridesap is a ligand for serum amyloid P component (SAP) and intends to inhibit and dissociate SAP binding to amyloid fibrils and tangles.
    GY04086 Special LTI-291 LTI-291 is an activator of glucocerebrosidase (Gcase) extracted from patent WO 2017192841 A1.
    GY04116 Special GJ103 sodium salt GJ103 sodium salt is an active analog of the read-through compound GJ072.
    GY04148 Special Mad2 inhibitor-1 (M2I-1) M2I-1 a small Mad2 inhibitor-1.
    GY04173 Special 1-Methyl-7-nitroisatoic anhydride 1-methyl-7-nitroisatoic anhydride is a reagent that detects local nucleotide flexibility, for probing 2'-hydroxyl reactivity.
    GY04175 Special Eupatilin Eupatilin, a lipophilic flavonoid isolated from Artemisia species, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.
    GY04192 Special GKT137831 GKT137831 is a novel, specific dual NADPH oxidase (NOX1/4) inhibitor. GKT137831 has potency both on human Nox4 (Ki=140±40 nM) and human Nox1 (Ki=110±30 nM) and is found 15-fold less potent on Nox2 (Ki=1750±700 nM) and 3-fold less potent on Nox5 (Ki=410±100 nM).
    GY04195 Special J-147 J-147 is a broad spectrum neuroprotective phenyl hydrazide compound(EC50=60-115 nM) with significant neurotrophic properties related to the induction of brain-derived neurotrophic factor (BDNF).
    GY04202 Special ISX9 ISX-9 is a small molecule inducer of adult neural stem cell differentiation.
    GY04211 Special Bindarit Bindarit(AF-2838), a CCL2, CCL7 and CCL8 inhibitor, is an anti-inflammatory agent.
    GY04220 Special BVT 2733 BVT 2733 is a new, small molecule, non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
    GY04223 Special Lomitapide Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
    GY04311 Special Ethofibrate Etofibrate is the ethandiol-1,2 diester of the nicotinic and clofibric acids. Etofibrate has been shown to be a potent hypolipidemic agent in animal and human.
    GY04318 Special Teriflunomide Teriflunomide is the active metabolite of leflunomide, which inhibits pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.
    GY04331 Special Genistin Genistin is the major isoflavonoid of soybeans and soy products.
    GY04357 Special Tirasemtiv Tirasemtiv is an activator of the fast skeletal muscle troponin complex.
    GY04364 Special Lycopene Lycopene is naturally occurring carotenoids found in tomato, tomato products, and in other red fruits and vegetables; exhibits antioxidant effects.
    GY04375 Special RG3039 RG3039 (PF-06687859) is an orally bioavailable and brain-penetrant DcpS inhibitor with an IC50 of 0.069 nM.
    GY04377 Special TPT-260 TPT-260(TPU260) is a thiophene thiourea derivative with molecule weight 260.00 in free base form; There is no formal name yet, we temporally call this molecule as TPT-260.
    GY04399 Special CH-223191 CH-223191 is a ligand-selective antagonist of the Ah (Dioxin) receptor.
    GY04409 Special Etomoxir Etomoxir is a potent inhibitor of carnitine palmitoyltransferase-I (CPT-1).
    GY04432 Special L-BMAA Beta-N-methylamino-L-alanine (L-BMAA) is a potent agonist of 'metabolotropic' glutamate receptors.
    GY04456 Special Proteinase K Proteinase K is used to digest protein and remove contamination from preparations of nucleic acid.
    GY04459 Special Ciraparantag Ciraparantag(PER977) is an intravenously administered anticoagulant Reversal Agent.
    GY04513 Special ASP7663 ASP 7663 is a selective TRPA1 activator (EC50 values are ~0.5 μM in human, mouse and rat).
    GY04678 Special SB9200 SB 9200 is a novel agonist of innate immunity, shows potent antiviral activity against resistant HCV variants.
    GY04679 Special Inarigivir (ORI-9020, SB-9000) Inarigivir (ORI-9020;SB-9000) is a dinucleotide which can significantly reduce extracellular (virion) HBV DNA levels with EC50 of 1.2 μM.
    GY02883 3PO 3PO is a novel small-molecule inhibitor of the PFKFB3 isozyme, 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM).
    GY01302 Thalidomide Thalidomide can directly inhibit angiogenesis induced by bFGF or VEGF in vivo.
    GY01364 4-Methylumbelliferone 4-Methylumbelliferone is a hyaluronic acid biosynthesis inhibitor with antitumoral and antimetastatic effects.
    GY01546 Glycyrrhizic acid Glycyrrhizic acid is a triterpenoid saponinl, extracted from the licorice root, with anti-tumor, anti-diabetic activities.
    GY01572 Mycophenolate mofetil Mycophenolate Mofetil(RS 61443) is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively.
    GY01660 Leflunomide Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
    GY01804 Mirin Mirin is a small-molecule inhibitor of MRN (Mre11, Rad50, and Nbs1) complex.
    GY01857 L-Ascorbic acid sodium L-Ascorbic acid (sodium) is a more bioavailable form of vitamin C that is an antioxidant agent.
    GY01873 Evodiamine Evodiamine is an alkaloid isolated from the fruit of Evodia rutaecarpa Bentham with diverse biological activities including anti-inflammatory, anti-obesity, and antitumor.
    GY01877 Chlormethine HCl Chlormethine hydrochloride is a vesicant and necrotizing irritant destructive to mucous membranes. The hydrochloride is used as an antineoplastic in Hodgkin's disease and lymphomas.
    GY01888 Mitotane Mitotane(2,4′-DDD), an isomer of DDD and derivative of DDT, is an antineoplastic medication used in the treatment of adrenocortical carcinoma.
    GY01889 Astragaloside A Astragaloside A is one of the major active constituents of Astragalus membranaceus in Traditional Chinese Medicine; has been widely used to treat ischemic diseases.
    GY01905 Gimeracil Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.
    GY01919 INH1 INH1 is a small molecule targeting the Hec1/Nek2 mitotic pathway suppresses tumor cell growth in culture and in animal.
    GY01925 Alendronate sodium hydrate (MK 217) Alendronate (sodium hydrate) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM.
    GY01926 Aloin Aloin(Aloin-A; Barbaloin-A) is a natural antitumor anthraquinone glycoside with iron chelating and non-atherogenic activities.
    GY01930 CCF642 CCF642 is a novel PDI-inhibiting compound with antimyeloma activity.
    GY01932 Coumarin Coumarin is the primary bioactive ingredient in Radix Glehniae, named Beishashen in China, which possesses many pharmacological activities, including anticancer, anti-inflammation and antivirus activities.
    GY01936 Mesna 2-mercaptoethane sulfonate (Mesna), is a synthetic small molecule, widely used as a systemic protective agent against chemotherapy toxicity, but is primarily used to reduce hemorrhagic cystitis induced by cyclophosphamide.
    GY01942 (S)-10-Hydroxycamptothecin (S)-10-Hydroxycamptothecin is a clinical therapy agent against hepatoma.
    GY01950 Amygdalin Amygdalin is a plant glucoside isolated from the stones of rosaceous fruits, such as apricots, peaches, almond, cherries, and plums.
    GY01960 10-Deacetylbaccatin III 10-Deacetylbaccatin-III is an intermediate for taxol analog preparations.
    GY01967 INH6 INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.
    GY02479 Erianin Erianin, often used as an antipyretic and analgesic agent, could inhibit IDO-induced tumor angiogenesis.
    GY01982 Methyl-β-cyclodextrin Methyl-β-cyclodextrin, a cyclic heptasaccharide, is an effective agent for the depletion of cholesterol from cells; also inhibits PEL cell growth with an IC50 of 3.33-4.23 mM.
    GY02024 Pimelic Diphenylamide 106 analog Pimelic Diphenylamide 106 analog is an analog of Pimelic Diphenylamide 106 with unknown biological activity.
    GY02029 N-deacetylated BMS-202 N-deacetylated BMS-202 is the deacetylated of BMS-202. BMS-202 is an inhibitor of the PD-l/PD-Ll interaction, mainly used for cancer treatment.
    GY02040 NSC-601980 NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
    GY02044 MUC5AC motif peptide MUC5AC motif peptide is a 16-amino acid fragment of mucin 5.
    GY02048 Ser-Leu-Leu-Lys SLLK, Control Peptide for TSP1 Inhibitor is a control peptide for LSKL (leucine-serine-lysine-leucine)
    GY02050 rGHRH(1-29)NH2 rGHRH(1-29)NH2 is a synthetic peptide which can stimulate the growth hormone (GH) secretion.
    GY02083 GK921 GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.
    GY02087 3-arylisoquinolinamine derivative 3-arylisoquinolinamine derivative is a 3-arylisoquinolinamine derivative with antitumor activity.
    GY02089 Vapreotide (RC160) Vapreotide, a synthetic analog of somatostatin, has NK1R antagonist activity.
    GY02125 ABL127 ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
    GY02127 A-802715 A802715 is a methylxanthine derivative. A802715 has a TD50 (toxic dose of 50%) of 0.9-1.1 mM.
    GY02134 Vitamin CK3 Vitamin CK3 is the combination of Vitamin C and vitamin K3 and has been shown to inhibit tumor growth and lung metastasis.
    GY02155 Cinobufotalin Cinobufotalin is one of the bufadienolides prepared from toad venom; has anticancer activity.
    GY02165 ASP-9521 ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.
    GY02169 Amcasertib Amcasertib is an orally administered investigational agent designed to inhibit cancer stem cell pathways, including Nanog, by targeting stemness kinases.
    GY02170 Exherin trifluoroacetate Exherin trifluoroacetate is an N-cadherin antagonist, which inhibits N-cadherin mediated cell adhesion.
    GY02178 Urolithin A Urolithin A is an intestinal metabolite of ellagic acid with antioxidant and antiproliferative effects; inhibits T24 and Caco-2 cell growth with IC50 values of 43.9 and 49 μM, respectively.
    GY02185 Tubeimoside II Tubeimoside II(Tubeimoside-B) is a natural analogue of oleanane type of triterpenoid saponin; show anti-inflammatory, antitumor, and antitumor-promoting effects.
    GY02210 Carglumic Acid Carglumic acid, a functional analogue of N-acetylglutamate (NAG) and a carbamoyl phosphate synthetase 1 (CPS1) activator, is used to treat acute and chronic hyperammonemia associated with NAG synthase (NAGS) deficiency.
    GY02230 Fmoc-Ser(O-α-D-GalNAc(OAc)3)-OH Fmoc-Ser(O-α-D-GalNAc(OAc)3)-OH is a drug for cancer.
    GY02247 TCV-309 chloride TCV-309 (chloride) is a platelet activating factor (PAF) antagonist.
    GY02248 DMCM HCl DMCM (hydrochloride) is Benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity.
    GY02260 STK16-IN-1 STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM.
    GY02266 4, 4'-Dimethoxybenzil 4,4'-Dimethoxybenzil is a human intestinal carboxyl esterase (hiCE) inhibitor with Ki of 70 nM.
    GY02297 Nesiritide (BNP-32) Nesiritide is a endogenous peptide secreted from cardiac ventricles in response to volume increase and pressure overload that acts as an agonist at atrial natriuretic peptide (ANP) receptor A (NRP1).
    GY02302 Oxyphenisatine Oxyphenisatine (Oxyphenisatin) is a laxative. Oxyphenisatin acetate is the pro-drug of oxyphenisatin with anticancer activity.
    GY02304 Fatostatin A Fatostatin A is a inhibitor of SREBP that directly binds SCAP and blocks its ER-to-Golgi transport with IC50 of 2.5 and 10 μM in mammalian cells.
    GY02343 Retinyl acetate Retinyl acetate is a natural form of vitamin A and has potential antineoplastic and chemo preventive activities.
    GY02349 Noscapine Noscapine is an orally administrable drug used worldwide for cough suppression, primarily mediated by its σ-receptor agonist activity, and possess anticancer activity.
    GY02351 TNP-470 TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.
    GY02387 GSK2194069 GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM in an assay detecting released CoA.
    GY02402 LTX-315 LTX-315 is an oncolytic peptide with potent anticancer activity; inhibits MRC-5, A20 and AT84 with IC50s of 34.3, 8.3 and 11 µM, respectively.
    GY02414 RR6 RR6 is a selective, reversible, and competitive vanin inhibitor.
    GY02441 Protein kinase inhibitors 1 Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
    GY02443 TDCPP TDCPP is a chlorinated analog of tris(2,3-dibromopropyl)phosphate (Tris) which is one of the most detected organophosphorus flame retardants (OPFRs) in the environment.
    GY02473 N3PT N3PT(N3-pyridyl thiamine) is a potent and selective transketolase(TK) inhibitor (IC50= 22 nM for Apo-TK) both in vitro and in vivo.
    GY02475 HAMNO HAMNO is a novel protein interaction inhibitor of replication protein A (RPA).
    GY02477 (2S)-Octyl-α-hydroxyglutarate (2S)-Octyl-α-hydroxyglutarate ((2S)-Octyl-2-HG) is a modified form of S-isomer 2-Hydroxyglutarate.
    GY02478 (2R)-Octyl-α-hydroxyglutarate (2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a modified form of D-isomer 2-Hydroxyglutarate.
    GY02488 ISA-2011B ISA-2011B is a PIP5Kα inhibitor with promising anticancer effects .
    GY02505 ML281 ML281 is a potent and selective STK33 inhibitor with IC50 of 14 nM.
    GY02521 GSK2795039 GSK2795039 is a novel small molecule NADPH Oxidase 2 Inhibitor.
    GY02525 UNC1079 UNC1079 is the piperidine analog of UNC1021, as a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies.
    GY02537 9-Dihydro-13-acetylbaccatin III 9-Dihydro-13-acetylbaccatin III (9-DHAB III) is an intermediate for taxol analog preparations.
    GY02552 VI 16832 VI 16832 is a broad spectrum Type I kinase inhibitor which can be used as an enrichment tool for the comparative expression analysis of protein kinases in different cancer cell lines.
    GY02592 SP-13786 FAP-IN-1 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 3.2 nM; also inhibits prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM.
    GY02603 HUHS015 HUHS015 is a potent PCA-1/ALKBH3 inhibitor both in vitro and in vivo.
    GY02608 PFK-158 PFK-158 is a potent and selective inhibitor of PFKFB3 that is currently being investigated in a phase I study in patients with advanced solid malignancies.
    GY02619 Calcein-AM Calcein-AM is cell-permeable fluorescent dye used to determine the cell viability.
    GY02625 GNE-3511 GNE-3511 is a potent and selective zipper kinase (DLK, MAP3K12) inhibitors.
    GY02633 SDZ281-977 SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A.
    GY02643 EF-5 EF-5 (EF5; 2-Nitroimidazole) is a hypoxia labeling agent used to identify hypoxia in cells.
    GY02656 Catechin Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
    GY02694 HA15 HA15 is a molecule that targets specifically BiP/GRP78/HSPA5.
    GY02704 Ro 48-8071 Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
    GY02725 RET Kinase inhibitor 1 RET Kinase inhibitor 1 is a RET kinase inhibitor extracted from patent WO2014141187A1, compound example 27, has an IC50 of < 100 nM.
    GY02752 tBID tBID is a selective inhibitor of homeodomain–interacting protein kinase 2 (HIPK2) with an IC50 of  0.33 µM.
    GY02758 Fumarate hydratase-IN-1 Fumarate hydratase-IN-1, an enzyme of the TCA cycle.
    GY02767 Fmoc-1, 6-diaminohexane Fmoc-1,6-diaminohexane is an analog of Osw-1 which can be used to treat Alzheimer's disease and cancer, extracted from patent US 20140135279 A1.
    GY02781 Tetracosactide Tetracosactide (INN) is a synthetic peptide and analogue of adrenocorticotrophic hormone (ACTH) .
    GY02795 Efaproxiral sodium Efaproxiral sodium is a synthetic allosteric modifier of haemoglobin (Hb), decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy.
    GY02801 Estradiol 3-sulfamate Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) is a potent, long-acting, and orally active steroid sulfatase inhibitor; inhibits estrone sulfatase with an IC50 of 251 nM and a Ki of 133 nM.
    GY02804 HMN-154 HMN-154 is a novel benzenesulfonamide anticancer compound; inhibits KB and colon38 cells with IC50 values of 0.0026 and 0.003 μg/mL, respectively.
    GY02805 HMN-176 HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1), without significant effect on tubulin polymerization. 
    GY02811 Glyoxalase I inhibitor free base Glyoxalase I inhibitor (free base) is a potent Glyoxalase I inhibitor, candidate for anticancer agents.
    GY02816 Phorbol Phorbol is a highly toxic diterpene, whose esters have important biological properties.
    GY02817 CCT007093 CCT 007093 is an effective PPM1D inhibitor that selectively reduces viability of human tumour cell lines.
    GY02831 NSC-23005 sodium NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.
    GY02840 BAY-876 BAY-876 is the first highly selective GLUT1 inhibitor with IC50 of 0.002 uM.
    GY02846 OICR-0547 OICR-0547 is a closely related derivative of OICR-9429. OICR-942 is a novel small-molecule antagonist of the Wdr5-MLL interaction, while OICR-0547 cannot bind to WDR5.
    GY02856 Fulvestrant (ICI 182780) R enantiomer Fulvestrant R enantiomer is the R enantiomer of Fulvestrant. Fulvestrant is a selective estrogen receptor (ER) antagonist which can be used to treat breast cancer.
    GY02859 GGTI298 GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
    GY02894 Tetrahydrouridine Tetrahydrouridine is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
    GY02904 DMA DMA is a fluorescent compound (λex=340 nm, λem=478 nm).
    GY02908 Ro 48-8071 fumarate Ro 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
    GY02916 Gracillin Gracillin is a kind of steroidal saponin isolated from the root bark of wild yam Dioscorea nipponica with antitumor agent.
    GY02922 Tenacissoside H Tenacissoside H is a Chinese medicine monomer extracted, isolated from Caulis Marsdeniae Tenacissimae.
    GY02935 Abiraterone metabolite 1 Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal drug, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
    GY02939 PDD 00017273 PDD 00017273 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with an IC50 of 26 nM, and a KD of 1.45 nM.
    GY02940 SAR405 R enantiomer SAR405 R enantiomer is an enantiomer of SAR405. SAR405 is a PIK3C3/Vps34 inhibitor.
    GY02957 Panaxadiol Panaxadiol is a novel antitumor agent extracted from the Chinese medical herb Panax ginseng.
    GY02959 NKP-1339 NKP-1339 is the first-in-class ruthenium-based anticancer drug in clinical development against solid cancer and has recently been studied successfully in a phase I clinical trial.
    GY02982 Ac-DEVD-AFC Ac-DEVD-AFC is a fluorogenic substrate (λex=400 nm, λem=530 nm).
    GY02984 EC330 EC330 is a leukemia inhibitory factor (LIF) inhibitor.
    GY02989 Solamargine Solamargine is a major steroidal alkaloid glycoside extracted from a traditional Chinese medicinal herb, Solanum nigrum L. (SNL); has been shown to inhibit growth and induce apoptosis of various cancer cells.
    GY02991 Arctiin (Arctigenin-4-glucoside) Arctiin(NSC 315527), a plant lignan that can be extracted from the Arctium lappa (burdock) seeds, is a possible environmental endocrine disruptor compounds and have been shown to influence sex hormone metabolism as well as protein synthesis, steroid biosynthesis.
    GY02997 Amifostine Amifostine is a cytoprotective adjuvant used in cancer chemotherapy and radiotherapy involving DNA-binding chemotherapeutic agents.
    GY03000 Calycosin Calycosin (Cyclosin) is a natural active compound with anti-oxidative and anti-inflammation activity.
    GY03018 DMA 3HCl DMA trihydrochloride is a fluorescent compound (λex=340 nm, λem=478 nm).
    GY03027 Cy5.5 Cy5.5 is a near-infrared fluorescent dye used to label biological molecules, such as peptides, proteins, and oligonucleotides.
    GY03036 Glucoraphanin Glucoraphanin, a natural glucosinolate found in cruciferous vegetable, is a stable precursor of the Nrf2 inducer sulforaphane, which possesses antioxidant, anti-inflammatory, and anti-carcinogenic effects.
    GY03041 5α-Pregnane-3β, 6α-diol-20-one 5α-Pregnane-3β,6α-diol-20-one is a mitogenic metabolite of progesterone, and it can be produced in starved androgen-responsive prostate cancer cells.
    GY03043 Imisopasem manganese Imisopasem manganese (M40403) is a stable non-peptidyl mimetic of manganese superoxide MnSOD.
    GY03045 5, 15-Diacetyl-3-benzoyllathyrol 5,15-Diacetyl-3-benzoyllathyrol is one of the lathyrane diterpenoids, that has anti-cancer activity.
    GY03047 3α-Aminocholestane 3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.
    GY03049 Glyoxalase I inhibitor Glyoxalase I inhibitor is a potent Glyoxalase I inhibitor, candidate for anticancer agents.
    GY03055 Zotarolimus Zotarolimus is a tetrazole-containing Rapamycin analog which is used as animmunomodulator, and is useful in the treatment of restenosis, immune, and autoimmune diseases.
    GY03056 42-(2-Tetrazolyl)rapamycin 42-(2-Tetrazolyl)rapamycin is a prodrug compound of a rapamycin analog extracted from patent US 20080171763 A1, Example 1. Rapamycin is a specific mTOR inhibitor.
    GY03065 Collagen proline hydroxylase inhibitor-1 Collagen proline hydroxylase inhibitor-1 is an antifibroproliferative agents.
    GY03066 Collagen proline hydroxylase inhibitor Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor; useful for antifibroproliferative agents.
    GY03070 Miquelianin Miquelianin (Quercetin 3-O-glucuronide) is a metabolite of quercetin and a type of natural flavonoid.
    GY03080 Hoechst 33258 Hoechst 33258 is a fluorescent dyes, which can be used as a cell dye for DNA.
    GY03081 Hoechst 33258 3HCl Hoechst 33258 trihydrochloride is a fluorescent dyes, which can be used as a cell dye for DNA.
    GY03086 (-)-Cephalotaxine Cephalotaxine is an antiviral as well as antitumor agent.
    GY03094 Sincalide (CCK-8) Sincalide (INN) is a cholecystokinetic drug administered by injection to aid in researching disorders of the gallbladder and pancreas.
    GY03101 Sotetsuflavone Sotetsuflavone is a potent inhibitor of DENV-NS5 RdRp (Dengue virus NS5 RNA-dependent RNA polymerase) with an IC50 of 0.16 uM, is the most active compound of this series .
    GY03102 Fluridil (Topilutamide) Topilutamide is a topical nonsteroidal antiandrogen (NSAA).
    GY03104 6-Aminochrysene 6-Aminochrysene (6-Aminochrysene) is an aromatic amine used as a chemotherapeutic agent in the treatment of splenomegaly, myeloid leukemia, and breast cancer.
    GY03105 NADPH tetrasodium salt NADPH tetrasodium salt is a ubiquitous cofactor and biological reducing agent that acts as an electron donor in many biological reactions.
    GY03107 Harringtonine Harringtonine, a natural Cephalotaxus alkaloid, is an inhibitor of protein synthesis.
    GY03109 3β, 7β, 17β-Trihydroxyandrost-5-ene 3b,7a,17a-Trihydroxyandrost-5-ene is a immune modulator extracted from patent US20030060425.
    GY03112 Tirapazamine Tirapazamine(SR259075; Win59075; SR4233) is an experimental anticancer drug that is activated to a toxic radical only at very low levels of oxygen; a phenomenon known as tumor hypoxia.
    GY03114 Geniposidic acid Geniposidic acid is an effective anticancer and radioprotection agent.
    GY03117 Bavachalcone Bavachalcone is a major bioactive compounds isolated from Psoralea corylifolia L.; has been widely used as traditional Chinese medicine; antibiotic or anticancer agent.
    GY03163 Tetrahydroxyquinone Tetrahydroxyquinone is a molecule best known as a primitive anticataract drug, is also a highly redox active molecule that can take part in a redox cycle with semiquinone radicals, leading to the formation of reactive oxygen species (ROS).
    GY03166 N-(5-Aminopentyl)acetamide N-Acetylcadaverine is the acetylated form of the polyamine cadaverine.
    GY03178 (E)-2-Decenoic acid (E)-2-Decenoic acid is an interesting fatty acid isolated from royal jelly secretions of honey bees.
    GY03182 Fucoxanthin Fucoxanthin is a marine carotenoid and shows anti-obesity, anti-diabetic, anti-oxidant, anti-inflammatory and anticancer activities.
    GY03188 Lathyrol Lathyrol is a natural product, and is used for cancer treatment.
    GY03194 Emeramide Emeramide is a novel lipid-soluble, thiol-redox antioxidant and heavy metal chelator.
    GY03195 HLM006474 HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
    GY03199 N-Desethyl Sunitinib N-Desethyl Sunitinib is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively.
    GY03205 F16 F16 is a small molecule that selectively inhibits proliferation of mammary epithelial, neu-overexpressing cells, as well as a variety of mouse mammary tumor and human breast cancer cell lines.
    GY03207 NVP 231 NVP-231 is a potent, specific, and reversible CerK inhibitor(IC50=12±2 nM) that competitively inhibits binding of ceramide to CerK.
    GY03208 YL-109 YL-109 is a novel anticancer agent which has ability to inhibit breast cancer cell growth and invasiveness in vitro and in vivo.
    GY03223 Cyclic somatostatin Cyclic somatostatin is a growth hormone-release inhibiting factor used in the treatment of severe, acute hemorrhages of gastroduodenal ulcers.
    GY03229 Aviptadil Aviptadil (INN) is an analog of vasoactive intestinal polypeptide (VIP) for the treatment of erectile dysfunction.
    GY03239 (-)-Bruceantin Bruceantin(NSC165563) is first isolated from Brucea antidysenterica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.
    GY03244 (-)-Gallocatechin gallate (-)-Gallocatechin gallate is the polyphenol isolated from tea, with cancer-preventive activities.
    GY03260 Timonacic Timonacic is used as an adjuvant in the treatment of acute and hepatic disorders. It has also been used for the treatment of some cases of cancer, through the induction of the reverse transformation.
    GY03262 ITE ITE is a aryl hydrocarbon receptor (AhR) agonist with Ki of 3 nM, and the estimated IC50 of ITE for OVCAR-3 cell proliferation was 0.2 nM.
    GY03268 Nitracrine Nitracrine is an antitumor drug that has been used clinically for several years.
    GY03274 Arenobufagin Arenobufagin is a natural bufadienolide from toad venom; has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells.
    GY03277 Bufalin Bufalin a major digoxin-like immunoreactive component of the Chinese medicine Chan Su; has been shown to exert a potential for anticancer activity against various human cancer cell lines in vitro.
    GY03278 Resibufogenin Resibufogenin, a component of huachansu, has been shown to exhibit the anti-proliferative effect against cancer cells, and this may be attributed to the degradation of cyclin D1 caused by the activation of GSK-3β.
    GY03279 Hederagenin Hederagenin is a triterpenoid saponin. It can inhibit LPS-stimulated expression of iNOS, COX-2, and NF-κB.
    GY03283 Bufotalin Bufotalin is a cardiotoxic bufanolide steroid, cardiac glycoside analogue, secreted by a number of toad species; a novel anti-osteoblastoma agent.
    GY03285 ADDA 5 HCl ADDA 5 hydrochloride is a partial non-competitive inhibitor of cytochrome c oxidase (CcO), with IC50s of 18.93 μM and 31.82 μM for purified CcO from human glioma and bovine heart, respectively.
    GY03288 Daucosterol Daucosterol is a natural sterolin.
    GY03292 Lucidin Lucidin (NSC 30546) is a natural component of Rubia tinctorum L. lucidin is mutagenic in bacteria and mammalian cells.
    GY03294 Calcitonin salmon Calcitonin, Salmon is a calcium regulating hormone secreted from mammalian thyroid parafollicular cells and in non-mammalian species from the ultimobranchial gland.
    GY03302 HI-TOPK-032 HI-TOPK-032 is a potent and specific TOPK inhibitor.
    GY03308 Lurbinectedin Lurbinectedin (PM01183) is a new DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
    GY03313 Tat-NR2B9c Tat-NR2B9c is a 20-aa peptide, which acts as a postsynaptic density-95 (PSD-95) inhibitor, with an EC50 of 6.7 nM for PSD-95d2 (PSD-95 PDZ domain 2), and 670 nM for PSD-95d1; also reduces NMDA-induced p38 activation, and possesses neuroprotective efficacy.
    GY03333 Canthaxanthin Canthaxanthin is a red-orange carotenoid with various biological activities, such as antioxidant, antitumor properties.
    GY03336 Urethane Urethane has been used as an antineoplastic agent and for other medicinal purposes.
    GY03340 Teriparatide (PTH 1-34) Teriparatide is a PHT agonist, binds to the receptor for PHT present in bone and stimulates the G-protein-related production of cyclic monophosphate.
    GY03350 Trolox Troloxa is a cell-permeable and water-soluble vitamin E analogue and is a powerful antioxidant.
    GY03351 Anethole trithione Anethole trithione is a drug used in the treatment of dry mouth, being studied in the treatment of cancer.
    GY03357 Corylin Corylin is a major bioactive compound isolated from Psoralea corylifolia L; antibiotic or anticancer compound.
    GY03365 Pipobroman Pipobroman is an anti-cancer drug that probably acts as an alkylating agent.
    GY03366 Protodioscin Protodioscin, a major steroidal saponin in dioscoreae rhizome, has been shown to exhibit multiple biological actions, such as anti-hyperlipidemia, anti-cancer, sexual effects and cardiovascular properties.
    GY03370 Pentagastrin pentagastrin is a synthetic polypeptide that has effects like gastrin when given parenterally,which can cause the secretion and synthesis of salivary proteins.
    GY03376 Coelenterazine Coelenterazine is widely distributed among marine organisms which can produce bioluminescence by calcium-dependent oxidation mediated by the photoprotein aequorin.
    GY03378 Sucralose Sucralose is an intense organochlorine artificial sweetener.
    GY03383 URB602 URB602 is a selective monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL with IC50 of 28±4 μM through a noncompetitive mechanism.
    GY03385 Glycerol Glycerol is a clear, colourless, viscous, sweet-tasting liquid. Glycerol is used in sample preparation and gel formation for polyacrylamide gel electrophoresis.
    GY03388 Vitamin K4 Vitamin K4 is a chemically synthesized Vitamin K which plays an important role in the normal blood coagulation system.
    GY03402 (+)-α-Tocopherol (+)-α-Tocopherol is a vitamin E derivative. vitamin E is a fat-soluble antioxidant.
    GY03405 Imexon Imexon is an iminopyrrolidone aziridine with anti-cancer activity.
    GY03409 Veratramine (NSC-23880) Veratramine(NSC17821; NSC23880) is useful as a signal transduction inhibitor for treating tumors.
    GY03416 Schisandrin C Schisandrin C is a phytochemical lignan isolated from Schizandra chinensis Baill; shows anticancer-effects in human leukemia U937 cells.
    GY03418 alpha-Mangostin Alpha-mangostin is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
    GY03432 5-IAF 5-IAF is an idoacetamide derivate of fluoresceine.
    GY03434 Uridine triphosphate Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a pyrimidine nucleoside triphosphate that participates in glycogen metabolism and synthesis of RNA during transcription.
    GY03443 R162 R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1), with anti-cancer properties.
    GY03448 ATN-224 ATN-224 is an oral Cu2+/Zn2+-superoxide dismutase 1 (SOD1) inhibitor. ATN-224 inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM.
    GY03450 MT-DADMe-ImmA MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
    GY03459 Importazole Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
    GY03472 Psoralen Psoralen(Furocoumarin) is an active ingredient from Fructus Psoraleae; has anticancer activity.
    GY03473 Perhexiline maleate Perhexiline maleate is a potent carnitine palmitoyltransferase 1 (CPT 1) inhibitor with IC50s of 77 and 148 μM for rat heart and liver CPT 1, respectively.
    GY03478 Pulsatilla saponin D (SB365) Pulsatilla saponin D(SB365) isolated from the root of Pulsatilla koreana, has exhibited potential beneficial effects as a chemopreventive agent for critical health conditions including cancer.
    GY03482 CBR-5884 CBR-5884 is a novel and noncompetitive 3-Phosphoglycerate dehydrogenase (PHGDH) inhibitor with IC50=33 μM).
    GY03498 L-Glutathione reduced L-Glutathione reduced (GSH; γ-L-Glutamyl-L-cysteinyl-glycine) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
    GY03505 1-Acetyl-3-o-toluyl-5-fluorouracil 1-Acetyl-3-o-toluyl-5-fluorouracil is a potent an antineoplastic agent.
    GY03506 TG003 TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
    GY03512 Brassinolide Brassinolide is a predominant plant growth modulator that regulate plant cell elongation.
    GY03513 Atractylenolide III Atractylenolide III is a major component of Atractylodes rhizome can induce apoptosis of the lung carcinoma cells.
    GY03515 Atractylenolide II Atractylenolide II is a sesquiterpene compound isolated from the dried rhizome of Atractylodes macrocephala (Baizhu in Chinese); anti-proliferative activity.
    GY03523 NVX-207 NVX-207 is a derivative of betulinic acid with anti-cancer activity.
    GY03526 Bestrabucil (KM2210) Atrimustine is a conjugate of chlorambucil and β-estradiol benzoate with the antitumor activity.
    GY03538 Hydroxysafflor yellow A Hydroxysafflor yellow A is a flavonoid derived and isolated from traditional Chinese medicine Carthamus tinctorius L., possesses anti-tumor activity.
    GY03550 Castanospermine Castanospermine inhibits all forms of α- and β-glucosidases, especially glucosidase l (required for glucoprotein processing by transfer of mannose and glucose from asparagine-linked lipids).
    GY03560 Trichlormethine HCl Trichlormethine hydrochloride is a cytostatic agent in the treatment of cancer and arthritis; shows carcinogenic effects to humans.
    GY03565 2OH-BNPP1 2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.
    GY03591 PSI-697 PSI-697is a P-selectin inhibitor.
    GY03603 Rabacfosadine Rabacfosadine (GS-9219), a novel prodrug of the nucleotide analogue PMEG, is designed as a cytotoxic agent that preferentially targets lymphoid cells.
    GY03606 23-Hydroxybetulinic acid 23-hydroxybetulinic acid is one of the bioactive components responsible for its anticancer activity.
    GY03639 Ecteinascidin-Analog-1 Ecteinascidin-Analog-1 is a useful intermediate for chemical sythesis of Ecteinascidin analogues; Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities.
    GY03641 LM985 LM985 is one of a series of compounds based on the flavone ring structure, with anti-tumor activities.
    GY03645 BBT594 BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.
    GY03650 HJC0350 HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 µM.
    GY03661 BAMB-4 BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 uM in ADP-Glo Assay.
    GY03674 Hyaluronic acid Hyaluronic acid is a biopolymer composed of repeating units of disaccharides with various applications.
    GY03678 Luciferase Luciferase is a class of enzyme which could oxidize D-luciferin to chemically generate visible light, and is widely used for biological assays and imaging.
    GY03686 Hyaluronic acid sodium salt Hyaluronic acid sodium salt is a biopolymer composed of repeating units of disaccharides with various applications.
    GY03735 Gastrin-Releasing Peptide, human Gastrin-Releasing Peptide, human (GRP) belongs to the bombesin-like peptide family, and is not a classical hypothalamic-hypophyseal regulatory hormone since it plays only a perfunctory role in the mediation of pituitary hormone release.
    GY03744 QS11 QS11 is a GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor.
    GY03763 FPH2 FPH2 induces of functional proliferation of primary human hepatocytes and may lead to the development of new therapeutics for liver diseases.
    GY03766 Brequinar (DUP785) Brequinar is a potent inhibitor of dihydroorotate dehydrogenase, with potent activities against a broad spectrum of viruses.
    GY03767 Hepsulfam Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.
    GY03768 Kallikrein Inhibitor Kallikrein Inhibitor is a synthetic peptide. The synthetic kallikrein inhibitor can attenuate breast cancer cell invasion.
    GY03777 Esonarimod Esonarimod is an antirheumatic drug.
    GY03783 DL 071-IT HCl DL 071-IT is a potent non-selective beta-adrenoceptor antagonist.
    GY03784 QCC-374 QCC-374 is prostanoid agonist potentially for the treatment of pulmonary arterial hypertension.
    GY03785 SPI-112Me SPI-112Me is a prodrug for SPI-112, which preferentially inhibits the PTPase activity of Shp2 over Shp1 and PTP1B by a factor of 20 in cell-free assays.
    GY03786 Pyronaridine Pyronaridine, also known as Malaridine, is an antimalarial drug.
    GY03789 Ehp-inhibitor-1 A novel Ehp inhibitor
    GY03790 Ehp-inhibitor-2 A novel Ehp inhibitor
    GY03800 LGD-3033 LGD-3303 is a drug which acts as a selective androgen receptor modulator (SARM), with good oral bioavailability.
    GY03807 CycLuc1(Luciferase substrate) CycLuc1 is a luciferase substrate which offers brighter bioluminescence and improved imaging in mouse models at lower doses than the standard D-luciferin.
    GY03810 MDK1088(T.cruzi Inhibitor) MDK-1088, also known as T.cruzi Inhibitor, is a Trypanosoma cruzi inhibitor. MDK-1088 has CAS#1350920-22-7 . The last 4 digit f CAS# was used in its name.
    GY03811 MDK74978(Multi-kinase inhibitor) MDK74978, also known as Multi-kinase inhibitor I, is a Multi-kinase inhibitor. MDK74978 has CAS#778274-97-8. The last 5 digit was used in its name.
    GY03812 MDK-8582(Hnps-PLA Inhibitor) MDK-8582, also known as Hnps-PLA Inhibitor, is an nhibitor of human nonpancreatic secretory Phospholipase A (hnps-PLA).
    GY03816 Methyl 13-cis-4-Oxoretinoate Methyl 13-cis-4-Oxoretinoate is a bioactive chemical.
    GY03817 Cyantraniliprole Cyantraniliprole(HGW-86) is an insecticide of the ryanoid class; has activity against pests such as Diaphorina citri that have developed resistance to other classes insecticides.
    GY03818 ADT-OH ADT-OH is a derivative of anethole dithiolethione (ADT) and synthetic hydrogen sulfide (H2S) donor.
    GY03821 Succinobucol Succinobucol is a phenolic antioxidant with anti-inflammatory and antiplatelet effects.
    GY03822 Diroximel Fumarete ALKS-8700 also known as diroximel fumarate, is a prodrug of monomethyl fumarate in a controlled-release formulation that rapidly and efficiently converts to MMF in the body.
    GY03826 SPI 112 SPI 112 is novel Shp2 PTP inhibitor.
    GY03827 AG 1406 AG 1406 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 .
    GY03828 Gemcitabine monophosphate Gemcitabine monophosphate disodium salt, also called GemMP, is a monophosphate derivative of Gemcitabine.
    GY03829 ASL 601 Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide.
    GY03830 Tolcide 2230 An antimicrobial agent used as a substitute for chlorophenols
    GY03836 SU 5205 SU 5205 is a VEGFR2 inhibitor.
    GY03837 SU 4942 SU 4942 is a bioactive chemical.
    GY03838 SU 4313 SU 4313 is a bioactive chemical.
    GY03839 NSC-247030 NSC 247030 is a bioactive chemical.
    GY03841 Brevianamide F Brevianamide F , also known as cyclo-(L-Trp-L-Pro), belongs to a class of naturally occurring 2,5-diketopiperazines.
    GY03849 Cyclo(RGDfC) Cyclo (RGDfC), avb3 Integrin Binding Cyclic RGD Peptide,This is a cyclic RGDfC sequence, an integrin avb3-affine peptide.
    GY03853 S-2765(FXa substrate) S-2765 is specific to activated factor X (FXa),short peptide covalently bound to pNA (4-nitroaniline).
    GY03854 CP 376395 CP 376395 is a potent and selective Corticotropin releasing factor 1 (CRF1) receptor antagonist.
    GY03878 Cyazofamid Cyazofamid is a foliar fungicide approved for use in the EU.
    GY03888 BT-11 BT-11 is an orally available LANCL2 binding compound for treating inflammatory bowel disease.
    GY03891 ST-271 ST271 is a potent inhibitor of protein tyrosine kinase (PTK).
    GY03893 Toxoflavin Toxoflavin is an inhibitor of survivin expression and antagonist of Tcf4/b-catenin signaling
    GY03905 LH-21 LH 21 is a 1,2,4-triazole that acts as a cannabimimetic.
    GY03916 ARM390 HCl ARM390 is a non-peptidic, low-internalizing δ-selective opioid receptor agonist.
    GY03921 GJ103 Torsemide is a pyridine-sulfonyl urea type loop diuretic.
    GY03927 Selamectin Selamectin is an anthelminthic which can be used on dogs and cats.
    GY03928 4-P-PDOT 4P-PDOT, also known as 4-phenyl-2- propionamidotetralin, is a MT2-receptor-specific antagonist. MT2 melatonin receptor may be a novel target for analgesic drug development.
    GY03933 Enclomiphene citrate Enclomiphene is a non-steroidal estrogen receptor antagonist that promotes gonadotropin-dependent testosterone secretion by the testes.
    GY03934 Etizolam Etizolam(AHR3219; Y7131) is a benzodiazepine analog.
    GY03939 EBE-A22 EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
    GY03940 TPPU TTPU is a soluble epoxide hydrolase (sEH) inhibitor with IC50 values of 37 and 3.7 nM for monkey and human sEH, respectively.
    GY03946 MELK-8a MELK-8a is a novel MELK inhibitor.
    GY03952 AZ-7371(DprE1-IN-1) DprE1-IN-1 is a potent DprE1 inhibitor, with ic50 of 10 nM, also inhibits PDE6, with IC50 of 6 uM.
    GY03953 (+)-Narwedine (+)-Narwedine. Galantamine(Narwedin) is a competitive and reversible cholinesterase(AChE) inhibitor.
    GY03956 (+)-Etomoxir (sodium salt) A PPARα agonist and an irreversible CPT-1 inhibitor.
    GY03965 PP2 analog PP2 analog is the analog of PP2,a Src family kinase inhibitor.
    GY03991 Naloxegol Oxalate Naloxegol is the first oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation.
    GY04021 Dihydroethidium Dihydroethidium(Hydroethidine; PD-MY 003) is a superoxide indicator; exhibits blue-fluorescence in the cytosol until oxidized, where it intercalates within the cell's DNA, staining its nucleus a bright fluorescent red.
    GY04026 NSC-41589 N-[2-(methylsulfanyl) phenyl]acetamide.
    GY04045 LSN2814617 LSN2814617 is a neurotoxic positive allosteric modulator.
    GY04048 Des(benzylpyridyl) Atazanavir The N-dealkylated metabolite (M1) of Atazanavir (A790051), a HIV protease inhibitor.
    GY04049 CM 346(Obenoxazine) Fabomotizole is an anxiolytic drug; produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions.
    GY04051 Etofenamate Etofenamate is a non-steroidal anti-inflammatory drug used for the treatment joint and muscular pain.
    GY04053 STATIL Statil is shown to be a potent aldose reductase inhibitor.
    GY04057 Ametantrone Ametantrone is a new anthracenedione antineoplastic agents, produced a concentration-dependent inhibition of hepatic microsomal lipid peroxidation.
    GY04059 Ro 61-8048 Ro 61-8048 is a potent and selective inhibitors of kynurenine hydroxylase with IC50 of 37 nM.
    GY04060 RGW 611 RGW 611 is a morpholine derivative.
    GY04069 PTZ-343 PTZ-343 is a phenothiazine derivative with chemical name: sodium 3-(10H-phenothiazin-10-yl)propane-1-sulfonate.
    GY04070 TPT-260 2HCl TPT-260 2Hcl (TPU260 2Hcl) is a thiophene thiourea derivative with molecule weight 260.00 in free base form; There is no formal name yet, we temporally call this molecule as TPT-260.
    GY04084 S-2238(Thrombin Substrate) S-2238 is specific to thrombin, is a short peptide covalently bound to pNA (4-nitroaniline).
    GY04406 TIMTEC-BB SBB000972
    GY04407 MMT-CL
    GY04443 GSK3008348 GSK3008348 is a potent and selective inhibitor being developed as the first inhaled inhibitor of the αvβ6 integrin for the treatment of IPF.
    GY04123 SC-26196 A selective Δ6 desaturase inhibitor that displays selectivity over Δ5 and Δ9 desaturases
    GY04596 α-CHCA 4-Chloro-α-cyanocinnamic acid (α-CHCA) is a classic monocarboxylate transporters (MCT) inhibitor. α-cyano-4-hydroxycinnamate (CHC) has a 10-fold selectivity for MCT1 compared to other MCTs.
    GY04614 GC376 GC376 is a 3CLpro inhibitor; inhibits the replication of viruses TGEV, FIPV and PTV with IC50 values of 0.15, 0.2 and 0.15 μM.
    GY04689 ELN484228 ELN484228 is a blocker of α-synuclein which is a key protein in Parkinson’s disease.
    GY04705 Tafamidis Tafamidis(Fx1006A) is a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade.
    GY04715 Verucerfont (GSK561679) Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively.
    GY04726 Leonurine (SCM-198) Leonurine, a natural alkaloid extracted from Herba leonuri, has been proved to have anti-inflammatory effect.
    GY04732 PF-9366 PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC50 of 420 nM and a Kd of 170 nM.
    GY04487 PCO371 PCO371 is a novel, orally active small molecule that acts as a full agonist of PTHR1.
    GY04495 CAS1822358-25-7 A compound potently inhibits RNA polymerase I transcription in A375 Malignant Melanoma cell line, while has no effects on polymerase II.
    GY04516 GSK-2018682 GSK-2018682 is a sphingosine 1 phosphate receptor (S1PR)-1 agonist potentially for the treatment of multiple sclerosis.
    GY04598 VPS34 inhibitor (Compound80) A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines.
    GY04606 KG-501(NaphtholAS-Ephosphate) KG-501 is a small molecule inhibitor of Aldolase, Histochemical substrate for alkaline phosphatases.
    GY04619 Gea3162 Gea 3162 is a potent inhibitor of ADP-induced platelet aggregation in platelet rich plasma (PRP). GEA 3162 stimulates cGMP production in platelets, granulocytes, and polymorphonuclear leukocytes.
    GY04620 GYY4137 morpholine salt GYY4137 is a slow-releasing H2S compound with vasodilator and antihypertensive activity.
    GY04621 KYP-2047 KYP-2047 is a very potent, selective inhibitor of Prolyl oligopeptidase (POP), also known as prolyl endopeptidase (PEP or PE). Ki = .023nM (porcine).
    GY04628 Z-IETD-pNA (GRANZYMEBSUBSTRATEI) Z-IETD-pNA is a colorimetric caspase-8/granzyme B substrate containing the benzyloxycarbonyl (Z) moiety.
    GY04633 Velaresol Velaresol, also known as BW12C or BW12C79, is a oxyhaemoglobin stabilizer.
    GY04636 Adipamidoxime (NSC70868) Adipamidoxime(NSC 70868) is a new bioactive compoud.
    GY04637 Cosan-528 Cosan-528 is a bioactive chemical.
    GY04638 Sematilide HCl Sematilide, also known as CK-1752, is a class III antiarrhythmic.
    GY04643 O-Butyryltimolol Butyryltimolol is a lipophilic ester prodrug of timolol, a beta adrenergic blocer with antihypertensive and hemodynamic properties.
    GY04645 NSC191412 NSC 191412 is a bioactive compound.
    GY04646 U19963 U 19963 is a bioactive compound.
    GY04649 Probucol Disuccinate Probucol is an effective inhibitor of ABCA1-mediated cholesterol efflux without influencing scavenger receptor class B type I–mediated efflux.
    GY04653 NSC6038 NSC 6038 is a bioactive compound.
    GY04669 Tomatidine HCl Tomatidine hydrochloride is a steriodal alkaloid structurally sumilar to cyclopamine (sc-200929) but does not inhibit hedgehog pathway. It can be employed as a negative control for cyclopamine (sc-200929) and KAAD-cyclopamine.
    GY04680 Arecaidinebut-2-ynylestertosylate Arecaidine but-2-ynyl ester tosylate is a potent muscarinic agonist that shows 4.6-fold that is selectivity for mAChR M2 in the atrium versus those in the ileum.
    GY04681 AVex-73 AVex-73 is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease
    GY04684 Alovudine Alovudine is a DNA polymerase subunit gamma-1 (POLG) inhibitor, shows promise for treating AML.
    GY04697 NSC31205 NSC 31205 is a PIM2/1 inhibitor.
    GY04710 Thiambutosin Thiambutosine was a candidate for treatment of lepromatous leprosy.
    GY04714 LX-2761 LX2761 is a locally acting SGLT1 inhibitor that is highly potent in vitro and delays intestinal glucose absorption in vivo to improve glycemic control.
    GY04717 IT901 IT 901 is a c-Rel inhibitor (IC50 = 3 μM). Inhibits IL-2 expression in activated T-cells in vitro.
    GY05011 Methyl Cellulose  Methyl cellulose (or methylcellulose) is a chemical compound derived from cellulose. It is not digestible, not toxic, and not an allergen. Methyl cellulose is widely used in drug formuation for oral adminstration.
    GY07394 DSP-2230 DSP-2230 is a selective Nav1.7/Nav1.8 blocker.
    GY07395 MC180295 MC180295 (MC-180295, MC 180295) is a novel potent, highly selective CDK9 inhibitor with IC50 of 5 nM, displays >22-fold selectivity over other CDKs.
    GY05382 Deoxynyboquinone Deoxynyboquinone (NSC 165572).
    GY05383 BNC-1 BNC-1 is a small molecule modulator of Amyloid pathology by promoting phosphorylation and activation of Elk-1, a transcriptional repressor of presenilin-1 but not presenilin-2.
    GY05384 TDI-2760 TDI-2760 si a small molecule Aβ-aggregation inhibitor that not only shows a strong inhibitory efficacy toward the Aβ-fibrinogen interaction (IC50=1.67 uM) but also retains potency toward the Aβ42 aggregation inhibition process.
    GY05385 SEN 1269 SEN1269 is a novel potent Aβ aggregation inhibitor that binds to monomeric Aβ1-42 with Kd of 4.4 uM, protects neuronal cell lines against an Aβ1-42 insult with IC50 of 15 uM.
    GY05386 ACG-416B A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.13 uM, >385-fold selectivity over ChoKβ.
    GY05387 TRO 40303 TRO 40303 is a novel cardioprotective compound that delays mitochondrial permeability transition pore (mPTP) opening, binds specifically to TSPO at the cholesterol site (Ki=150 nM).
    GY05388 P11 PAFAH inhibitor P11 (P11) is a potent, selective platelet-activating factor acetylhydrolases PAFAH1b2 and PAFAH1b3 inhibitor with IC50 of 40 nM and 900 nM respectively.
    GY05389 MDL-72527 A polyamine oxidase (PAO) inhibitor that inhibits spermine oxidase and N1-acetylpolyamine oxidase with IC50 of 6.1 and 0.02 uM, respectively.
    GY05390 Visomitin Visomitin (SKQ1 bromide.
    GY05391 Meayamycin Meayamycin is an analogue of FR901464 that binds to the splicing factor 3b (SF3b) complex and inhibits pre-mRNA splicing, shows picomolar antiproliferative activity against various cancer cell lines and multidrug-resistant cells.
    GY05392 R 59022 A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM, inhibits the phosphorylation of OAG to OAPA with IC50 of 3.8 uM in intact platelets.
    GY05393 VJ115 A small molecule NADH oxidase ENOX1 inhibitor with IC50 of 10 uM.
    GY05395 ADX-102 ADX-102 (Reproxalap, NS-2) is a novel small molecule immunomodulator that covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal, which have been shown to mediate inflammatory pain.
    GY05398 iMDK iMDK is a small molecule inhibitor of the growth factor Midkine (MDK) that suppresses the endogenous expression of MDK but not other growth factors such as PTN or VEGF.
    GY05400 JNJ-26489112 JNJ-26489112 (JNJ26489112) is a broad-spectrum anticonvulsant that displays activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures.
    GY05401 RSM-932A A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.0 uM, 33-fold selectivity over ChoKβ.
    GY05402 GRF (1-44), human The parent molecule of several peptides recently extracted from pancreatic tumours associated with acromegaly.
    GY05403 p32 inhibitor M36 p32 inhibitor M36 is a novel small molecule inhibitor of p32 mitochondrial protein, binds directly to p32 and inhibits p32 association with LyP-1.
    GY05404 5-FAM The single isomer, 5-FAM, contains a carboxylic acid that can be used to react with primary amines via carbodiimide activation of the carboxylic acid. Fluorescein is the most common fluorescent derivatization reagent for labeling biomolecules. In addition to its relatively high absorptivity, excellent fluorescence quantum yield, and good water solubility, fluorescein has an excitation maximum that closely matches the 488 nm spectral line of the argon-ion laser.
    GY05405 Juniferdin Juniferdin is a small molecule, potent Protein disulfide isomerase (PDI) inhibitor with IC50 of 156 nM, inhibits PDI-mediated reduction of HIV-1 envelope glycoprotein gp120.
    GY05407 PDMP HCl A ceramide analog that inhibits glucosylceramide synthase (GCS), reduces the synthesis of sphingosine and its derivatives, increases cellular ceramide, and induces cell cycle arrest. .
    GY05408 Aβ polymerization stimulator O4 Aβ polymerization stimulator O4 is an orcein-related small molecule can drive polymerization of amyloid-β (Aβ).
    GY05409 D-Glutamic acid The one form of glutamic acid found in nature, is the most potent natural inhibitor of glutathione synthesis.
    GY05410 GW-4869 GW-4869 (GW4869, GW 4869) is a cell-permeable, potent, specific, non-competitive inhibitor of neutral sphingomyelinase (nSMase) with IC50 of 1 uM.
    GY05412 Perhexiline Perhexiline is a prophylactic antianginal agent that inhibits carnitine palmitoyltransferase (CPT1/CPT2).
    GY05413 Pyrimidinone 8 Pyrimidinone 8 is a novel allosteric, non-competitive divalent metal transporter-1 (SLC11A2/DMT1) inhibitor with Ki of 20 uM.
    GY05414 Adrafinil The prodrug of modafinil that is a mild central nervous system stimulant drug used to relieve excessive sleepiness and inattention.
    GY05415 E7107 E7107 (E-7107) is a derivative of pladienolide that targets the SF3b subunit of the spliceosome, shows significant antitumor activity in vitro and in vivo.
    GY05416 AZD5904 AZD5904 (AZD-5904) is a potent, selective irreversible, orally bioavailable myeloperoxidase (MPO) inhibitor with IC50 of 140 nM, similar potency in mouse and rat.
    GY05417 TRX-0237 TRX-0237 Methylate (Hydromethylthionine, Methylene blue) is a Tau aggregation inhibitor (TAI) with Ki of 0.12 uM for intracellular TAI activity.
    GY05419 L-Thyroxine sodium salt pentahydrate A manufactured form of the thyroid hormone thyroxine (T4) that typically used to treat hypothyroidism.
    GY05420 Tranilast A compound that exhibits anti-inflammatory and immunomodulatory effects by inhibiting lipid mediator and cytokine release from inflammatory cells and interfering with PDGF- and TGF-β1-induced proliferation and migration of vascular medial smooth muscle cells.
    GY05421 L-Thyroxine A manufactured form of the thyroid hormone thyroxine (T4) that typically used to treat hypothyroidism.
    GY05422 NAPQI A toxic byproduct, iminoquinone metabolite of acetaminophen that covalently binds to the active site of MIF.
    GY05424 GGTI 2417 GGTI 2417 is the methyl ester prodrug of GGTI-2418, a highly potent, competitive, and selective inhibitor of GGTase I.
    GY05426 DS44170716 A novel MPT (mitochondrial permeability transition) inhibitor of that inhibits Ca2+-induced MPT in rat liver isolated mitochondria.
    GY05427 5MPN 5MPN is a first-in-class, selective, competitive, orally available inhibitor of PFKFB4 with Ki of 8.6 uM, does not inhibit PFK-1 or PFKFB3.
    GY05577 T-025 T-025 is an orally available, potent inhibitor of Cdc2-like kinases (CLKs) with Kd of 4.8, 0.096, 6.5, and 0.61 nM for CLK1, CLK2, CLK3, and CLK4, also inhibits DYRK1A and DYRK1B with IC50 of 0.074 and 1.5 nM.
    GY05579 SAN9812 SAN9812 (Carnostatine) is a potent, highly selective, competitive inhibitor of Carnosinase 1 (CN1) activity with Ki of 11 nM.
    GY05580 RU-521 RU-521 (RU.521, RU-320521) is a potent, selective cyclic GMP-AMP synthase (cGAS) inhibitor with Kd of 36.2 nM.
    GY05585 PF-794 PF-794 (PF794) is a potent, specific and ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with IC50 of 39 nM in cell-free assays.
    GY05586 PF-06928215 PF-06928215 (PF06928215) is a high affinity Cyclic GMP-AMP synthase (cGAS) inhibitor with Kd of 200 nM, IC50 of 4.9 uM.
    GY05588 P053 P053 (P-053, CerS1 inhibitor P053) is a potent, selective, orally active inhibitor of ceramide synthase 1 (CerS1) with IC50 of 0.5 uM, displays >10-fold selectivity for inhibition of CerS2, CerS4, CerS5, and CerS6.
    GY05597 LV-320 LV-320 (LV320) is a novel potent, cell-active, allosteric inhibitor of the autophagy-related cysteine protease ATG4B with IC50 of 24.5 uM in ATG4B cleavage assays.
    GY05598 KuWal151 KuWal151 is a potent, selective cdc2-like kinase (CLK) inhibitor with IC50 of 88/510/28 nM for CLK1/2/4, respectively.
    GY05601 Karonudib Karonudib (TH1579) is an analogue of TH588, a potent, selective MTH1 inhibitor with good oral availability and demonstrates excellent pharmacokinetic and anti-cancer properties in vivo..
    GY05602 JTT-551 sodium JTT-551 sodium (JTT551, JTT 551) is a novel potent, selective inhibitor of protein tyrosine phosphatase 1B (PTP1B) with Ki of 0.22 uM, displays >45-fold and >136-fold selectivity over TCPTP, CD45 and LAR.
    GY05612 CWP-232228 CWP-232228 is a highly potent small-molecule Wnt/β-catenin signaling inhibitor that targets the β-catenin/Tcf4 interaction in the nucleus.
    GY05618 CLK2 inhibitor Indazole1 CLK2 inhibitor Indazole1 is a novel potent, selective inhibitor of CLK2 with IC50 of 2.7 nM, 60-fold selectivity over PKA and >600-fold selectivity over a panel of 34 kinases.
    GY05629 ARN-3261 ARN-3261 is a potent, selective, orally available salt inducible kinase SIK2 and SIK3 inhibitor with IC50 of 11 nM and 19 nM, respectively.
    GY05633 HCI-2389 A potent, specific, irreversible NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 16.65 nM.
    GY05634 XEN 602 A potent, specific divalent metal transporter 1 (DMT1) inhibitor that inhibits Mn incorporation in HEK293 cells with IC50 of 0.3 nM.
    GY05637 LOXO-292 A potent, selective, orally available RET kinase inhibitor with potential antineoplastic activity.
    GY05641 CCG 258748 A potent, selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 8 nM.
    GY05643 Nek2 inhibitor 72 A potent, ATP-competitive and relative selective Nek2 inhibitor with IC50 of 0.27 uM.
    GY05647 CS-11 A novel small molecule inhibitor that inhibits PP2A and β-catenin interaction by selectively engaging PR55α binding site (Kd=45 pM).
    GY05651 Fumarase-IN-1 A cell-permeable small molecule inhibitor of Fumarase (fumarate hydratase), an enzyme of the tricarboxylic acid cycle (TCA cycle).
    GY05655 CAT639 CAT639 is an improved analog of ATV399 that exhibits improved β-cell viability and insulin secretion in the rat insulin-producing INS1E cells and primary rat dispersed islet cells, inhibits dimerization of iNOS.
    GY05656 TiY TiY (TIC Fluorescent Probe TiY) is the first TIC (tumor initiating cell)-specific fluorescent chemical probe, target vimentin, a marker for epithelial-to-mesenchymal transition (EMT).
    GY05664 ERD03 ERD03 (EXOSC3-RNA disrupting compound 3) is a small molecule EXOSC3-RNA disrupting (ERD) compound that binds specifically to EXOSC3 (Kd=17 uM), induces a PCH1B-like phenotype in zebrafish.
    GY05665 DNS-pE2 DNS-pE2 is the first small molecule that can selectively label endogenous 3-phosphoglycerate dehydrogenase (PHGDH) from various mammalian cells.
    GY05666 DNS-pE DNS-pE (PHGDH Fluorescent Probe DNS-pE) is the first small molecule that can selectively label endogenous 3-phosphoglycerate dehydrogenase (PHGDH) from various mammalian cells.
    GY05674 SPM-242 racemate A potent, selective S1P3 antagonist with Ki of 0.25 nM.
    GY05675 GNF-351 A potent, pure aryl hydrocarbon receptor (AHR) antagonist (IC50=62 nM) devoid of partial agonist potential.
    GY06451 SCF-I2 An allosteric, sepecific inhibitor of substrate recognition by the SCFCdc4 ubiquitin ligase with IC50 of 6.2 uM in FP assyas.
    GY06452 Pexmetinib Pexmetinib (ARRY-614) is a potent, orally active, dual Tie-2/p38 MAPK inhibitor with IC50 of 1, 26 and 35 nM for Tie-2, p38α and p38β, respectively.
    GY06453 GAP-134 A potent, orally active gap-junction modifier.
    GY06454 GAP-134 HCl A potent, orally active gap-junction modifier.
    GY06455 Suplatast tosilate A Th2 cytokine inhibitor that attenuates IL-2, IL-5 and IL-13 production and has no effect on IFN-γ production.
    GY06457 ANI-7 A potent and selective (up to 263-fold) inhibitor of breast cancer cells with GI50 of 0.5 uM (MCF-7), via activation the aryl hydrocarbon receptor (AhR) pathway.
    GY06458 SPA70 SPA70 is a potent and selective hPXR antagonist (IC50=0.51 uM) that interacts with the ligand-binding domain (LBD) of hPXR, inhibits hPXR in human hepatocytes and mouse models and enhances the chemosensitivity of cancer cells.
    GY06459 GMI-1070 GMI-1070 (Rivipansel, PF-06460031) is a novel small molecule glycomimetic pan-Selectin antagonist with IC50 of 4.3 uM, 423 uM and 337 uM for E-selectin, P-selectin and L-selectin, respectively.
    GY06460 Gemigliptin A novel potent, selective, competitive and orally active DPP4 inhibitor with potential for the treatment of type 2 diabetes.
    GY06461 TAK-100 TAK-100 is a potent, selective and orally active inhibitor of DPP-4 with IC50 of 5.3 nM, shows no inhibition on DPP2/8/9.
    GY06464 Heclin A small molecule inhibitor of HECT-type ubiquitin ligase with IC50 of 6.8/6.3/6.9 uM for Smurf2/Nedd4/WWP1, respectively.
    GY06465 Mapracorat Mapracorat (ZK 245186) is a potent, selective and non-steroid glucocorticoid receptor (GR) agonist with binding Ki of 1.9 nM.
    GY06466 TG693 TG693 is an orally available, selective, ATP-competitive CLK1 inhibitor with IC50 of 112.6 nM.
    GY06467 GATA4 activator 7 A novel small molecule that activates GATA4/NKX2-5 transcriptional synergy with EC50 of 7 uM in cell reporter assay. .
    GY06468 Gosogliptin 2HCl A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.
    GY06469 Gosogliptin A potent, selective, competitive, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 13 nM.
    GY06470 SKF-89976A HCl A potent, selective and GABA transporter 1 (GAT1) inhibitor with IC50 of 0.13 uM for hGAT1.
    GY06471 MLS-0322825 MLS-0322825 is a novel potent low-molecular-weight protein tyrosine phosphatase (LMPTP) inhibitor with IC50 of 3.3 uM.
    GY06472 Lisinopril dihydrate A angiotensin-converting enzyme (ACE) inhibitor for treatment of hypertension, heart failure, and after heart attacks.
    GY06473 Loteprednol etabonate Loteprednol etabonate is an anti-inflammatory corticosteroid used in optometry and ophthalmology.
    GY06474 AA-861 AA-861 (Docebenone) is a potent, selective 5-Lipoxygenase (5-LO) inhibitor with IC50 of 0.8 uM.
    GY06478 MK-0974 A potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 0.77 nM.
    GY06480 Lisinopril A angiotensin-converting enzyme (ACE) inhibitor for treatment of hypertension, heart failure, and after heart attacks.
    GY06481 Ronacaleret A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR.
    GY06483 3-Bromo-7-Nitroindazole 3-Bromo-7-Nitroindazole is a more potent inhibitor of nNOS than 7-nitroindazole in vitro, is also potent against iNOS, inhibits rat nNOS, bovine eNOS, and rat iNOS with IC50 of 0.17, 0.86, and 0.29 uM.
    GY06484 NCI-83633 A small molecule inhibitor of PP2C that activates extensive 3' cleavage at a concentration 50-fold below that required by fluoride or CP.
    GY06485 CE-245677 CE-245677 is a potent, selective, orally active, dual Tie2/Trk kinase inhibitor with IC50 of 4.7 nM, 1 nM for Tie2 and TrkA/B, respectively.
    GY06487 NK150460 A potent and selective inhibitor of breast cancer cells via activation the aryl hydrocarbon receptor (AhR) pathway.
    GY06488 Ronacaleret HCl A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR.
    GY06489 BC-21 BC-21 (NSC 109268) is a novel small molecule inhibitor that effectively inhibits the β-catenin/Tcf4 interaction with Ki of 6.55 uM.
    GY06490 Ilepatril A potent, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 0.053 and 5.0 nM, respectively.
    GY06492 PTP1B-IN-1 A 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for design of protein tyrosine phosphatase-1B (PTP1B) inhibitor.
    GY06496 Tasisulam sodium Tasisulam (LY 573636) is a small molecule antitumor agent that induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death.
    GY06497 SP 4206 SP 4206 is a high-affinity (Kd=70 nM) small molecule that blocks blocks the binding of the IL-2α receptor (IL-2Rα) to IL-2.
    GY06498 Mocravimod A synthetic immunosuppressant that functions as a S1P1 receptor agonist.
    GY06499 Guanabenz Guanabenz (WY 8678) is an α2 adrenergic receptor agonist that is used as an antihypertensive agent.
    GY06500 Prednisolone Prednisolone is a glucocorticoid with the general properties of the corticosteroids. .
    GY06503 NSC117079 A selective protein phosphatase PHLPP inhibitor with IC50 of 4 uM for PP2C domain of PHLPP2.
    GY06504 RUNX1-IN-17 A potent, allosteric inhibitor of CBFβ-RUNX1 interaction with IC50 of 3.2 uM in FRET assays.
    GY06505 Pexacerfont A potent, selective and orally active CRF1 receptor antagonist with IC50 of 6.1 nM, >1,000-fold selectivity over CRF-binding protein and biogenic amine receptors.
    GY06508 NDT 9513727 NDT 9513727 is a potent, selective and orally bioavailable C5a receptor inverse agonist with IC50 of 11.6 nM in radioligand binding assay.
    GY06509 Elobixibat An orally available, potent and selective ileal bile acid transporter (IBAT) inhibitor for the treatment of constipation.
    GY06510 DT204 A novel SCFSkp2 inhibitor that reduces Skp2 binding to Cullin-1 and Commd1, synergistically enhances BTZ-induced apoptosis.
    GY06511 PD-146176 A potent, selective, non-competitve inhibitor of 15-lipoxygenase (15-LOX) with Ki of 197 nM.
    GY06512 W-54011 A potent and orally active non-peptide C5a receptor (CD88.
    GY06513 BN82002 A potent Cdc25 dual specificity phosphatase inhibitor with IC50 of 2-6 uM for Cdc25A/B/C.
    GY06514 ATV399 ATV399 (ATV-399) is a novel small molecule that dose-dependently reduces the cleaved caspase9 levels with IC50 of 3.3 uM, inhibits dimerization of iNOS.
    GY06515 Triptonide A key bioactive small molecule identified in Tripterygium wilfordii Hook F., has a broad spectrum of biological functions.
    GY06516 Carnosic acid Carnosic acid (Carnosate) is a naturally occurring phenolic compound with antioxidant, anti-inflammatory and antimicrobial properties, inhibits the BCL9/β-catenin interaction with Ki of 3.3 uM.
    GY06517 Leukadherin 1 Leukadherin 1 (LA1) is a small molecule allosteric agonist of integrin CD11b/CD18 (CR3), increases CD11b/CD18-dependent cell adhesion to fibrinogen (EC50=4 uM).
    GY06518 Phortress The L-lysylamide prodrug of 5F-203 (NSC703786), a potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway.
    GY06520 Sufugolix A highly potent and orally bioavailable non-peptide antagonist of luteinizing hormone-releasing hormone (LHRH) receptor with binding and functional IC50 of 0.1 and 0.06 nM for human LHRH, respectively.
    GY06522 SNAP-37889 A potent, selective galanin-3 receptor (Gal3) antagonist with Ki of 17.44 nM, displays highly selective for Gal3 over the Gal1 and Gal2 subtypes (both Ki >10 uM).
    GY06523 Ro5-3335 A benzodiazepine inhibitor that directly interacts with RUNX1 and CBFβ, represses RUNX1/CBFβ-dependent transactivation in reporter assays.
    GY06524 VX-148 VX-148 is a potent, uncompetitive, orally bioavailable IMPDH inhibitor with Ki of 6 nM against IMPDH type II enzyme.
    GY06525 OTX008 OTX008 (Calixarene 0118, PTX-008) is a is a calixarene derivative designed to bind the Galectin-1 (Gal1) amphipathic β-sheet conformation.
    GY06526 5F 203 A potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway.
    GY06527 SB 290157 A potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM.
    GY06528 5Z-7-Oxozeaenol A potent, selective TAK1 inhibitor with IC50 of 8 nM, displays >33-fold and >62-fold selectivity over MEKK1 and MEKK4 respectively.
    GY06530 Lopixibat chloride Lopixibat chloride (LUM-001, HP-625) is a potent, selectiove, oral inhibitor of sodium bile acid cotransporter and Ileal bile acid transporter (IBAT).
    GY06531 Rupintrivir Rupintrivir (AG-7088, AG7088) is a potent, irreversible inhibitor of human rhinovirus 3C protease, inhibits the replication of all HRV serotypes with EC50 of 23 nM and EC90 of 82 nM.
    GY06532 ZL0454 ZL0454 is a potent, highly selective small-molecule BRD4 inhibitor with IC50 of 49 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively.
    GY06533 ZL0420 ZL0420 is a potent, highly selective BRD4 inhibitor with IC50 of 27 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively.
    GY06535 Dynarrestin Dynarrestin is a novel inhibitor of cytoplasmic Dyneins 1 and 2, acts reversibly to inhibit cytoplasmic dynein 1-dependent microtubule binding and motility in vitro without affecting ATP hydrolysis.
    GY06536 Y08060 Y08060 is a potent and selective BET inhibitor with Kd of 306 nM for BRD4 BD1, displays excellent selectivity for BET subfamily over other non-BET family with the exception of moderate inhibition of CBP/EP300.
    GY06537 SJ830599 SJ830599 is a modest selective BRD2-BD2 inhibitor with IC50 of 0.61 uM, 3.3-fold selectivity over BRD2-BD1.
    GY06538 PMX53 PMX53 (Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)) is a potent C5a receptor (CD88) antagonist with IC50 of 20 nM, also is an agonist for Mas-related gene 2 (MrgX2) in human mast cells.
    GY06539 RMC-4550 RMC-4550 (RMC4550) is a potent, selective, allosteric inhibitor of SHP2 with IC50 of 0.58 nM (full-length SHP2 enzyme), suppresses pERK signaling in Calu-1 cells with IC50 of 7 nM.
    GY06540 BCX-1470 methanesulfonate A serine protease inhibitor that inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM).
    GY06542 SHP2-IN-2 SHP2-IN-2 is a selective, allosteric inhibitor of protein tyrosine phosphatase SHP2, preferentially inhibits SHP2 F285S over the PTP domain and allosteric site mutant.
    GY06543 ABBV-744 ABBV-744 (ABBV744) is a potent, BDII-selective BET bromodomain inhibitor, ABBV-744 is a potent, selective inhibitor of the AR transcription activity.
    GY06544 XDM-CBP A highly potent and selective inhibitor of CBP/p300 bromodomain with Kd of 0.23/0.47 uM respectively, with high selectivity over all other BD families, including the BET family.
    GY06545 LLS30 LLS30 is a potent, allosteric Galectin-1 (Gal-1) inhibitor, inhibits AR negative cells PC3, DU145, and AR positive cells, 22RV1 and CWR-R1 cells with IC50 of 10.4 μM, 5.3 μM, 3.3 μM and 5.9 μM, respectively.
    GY06546 LLS2 LLS2 is a novel potent Galectin-1 (Gal1) inhibitor that decreases membrane-associated H-Ras and K-Ras and contributed to the suppression of pErk pathway.
    GY06547 Mtphagy Dye Mtphagy Dye is a small-molecule fluorescent probe for visualizing mitophagy.
    GY06548 SJB7 SJB7 is a close analog of SPA70 and hPXR agonist, interacts with the ligand-binding domain (LBD) of hPXR.
    GY06549 WNK inhibitor 7 A potent, selectiive inhibitor of WNK1 kinase with IC50 of 95 nM, shows IC50 of 1.39 uM in the cellular OSR1 phosphorylation assay with reasonable aqueous solubility.
    GY06550 WNK inhibitor 11 WNK inhibitor 11 is a potent, selectiive and orally active inhibitor of WNK1 kinase with IC50 of 6 nM, 1,000-fold selectivity over WNK4 and 57-fold selectivity over WNK2.
    GY06551 WNK inhibitor 12 A potent, selectiive and orally active inhibitor of WNK1 kinase with IC50 of 6 nM, 1,000-fold selectivity over WNK4 and 57-fold selectivity over WNK2.
    GY06552 IMPDH2-IN-5 A potent, selective IMPDH2 inhibitor that covalently binds to Cys140 with IC50 of 620 nM (inhibition of NO production).
    GY06553 FL-411 FL-411 is a novel small-molecule inhibitor of BRD4, induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction and activating AMPK-mTOR-ULK1-modulated autophagic pathway in breast cancer cells.
    GY06554 CLK inhibitor T3 CLK inhibitor T3 (T3) is a highly potent, selective, and cell-based stable CDC-like kinase (CLK) inhibitor with 0.67, 15 and 110 nM for CLK1,2 and 3, respectively.
    GY06555 GW274150 GW274150 is a potent and highly selective inhibitor of iNOS with IC50 of 1.4 uM, displays >200 fold selectivity over eNOS and nNOS (IC50>100 uM).
    GY06556 BAY 299 BAY 299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 and the second bromodomain of TAF1 with IC50 of 6 nM and 13 nM, respectively.
    GY06557 XMU-MP-2 XMU-MP-2 is a potent and selective BRK/PTK6 (breast tumor kinase) inhibitor with biochemical IC50 of 3.2 nM.
    GY06558 Merimepodib Merimepodib (VX-497, VI-21497, MMPD) is a potent, selective, reversible, uncompetitive IMPDH inhibitor with broad-spectrum antiviral activity.
    GY06559 MP07-66 A novel FTY720 analog that acts as PP2A activator, disrupts the SET/PP2A interaction devoid of immunosuppressive effects leads to the reactivation of PP2A.
    GY06560 GNE-049 GNE-049 is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively.
    GY06561 GMI-1271 A novel specific glycomimetic E-Selectin antagonist with Kd of 0.46 uM, IC50 of 1.75 uM.
    GY06563 K-7174 A selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2).
    GY06565 Danicopan Danicopan (ACH-4471.
    GY06567 AZD-9567 AZD-9567 (AZD9567) is a potent, selective, non-steroidal and orally available selective glucocorticoid receptor modulator (SGRM) for treatment of rheumatoid arthritis.
    GY06568 NI-42 A potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs.
    GY06569 β-catenin-IN-11a β-catenin-IN-11a is a β-catenin/CD44/Nanog axis inhibitor, docks into the β-catenin allosteric site and interferes β-catenin/TCF-4 complex.
    GY06570 TRIM24 inhibitor X TRIM24 inhibitor X is a potent TRIM24 bromodomain inhibitor for synthesis dTRIM24.
    GY06571 NI-57 NI-57 is a potent inhibitor of the bromodomain of the BRPFs and binds to BRPF1B, BRPF2 and BRPF3 and with KD of 31 nM,108 nM and 408 nM (ITC), respectively.
    GY06575 iCRT-5 iCRT-5 is a selective, cell-permeable β-catenin responsive transcription (CRT) inhibitor with IC50 of 18 nM.
    GY06576 MSI-1436 An non-competitive, allosteric inhibitor of PTP1B with Ki of 0.6 uM for PTP1B1-405.
    GY06578 NNC 05-2090 HCl NNC 05-2090 is a potent selective GABA transporter inhibitor of mGAT2 with Ki of 1.4 uM.
    GY06579 Dynein2-IN-37 Dynein2-IN-37 (Ciliobrevin analog 37) is a potent, selective cytoplasmic dynein 2 ATPase activity antagonist with IC50 of 11 uM, shows weak inhibition for dynein 2 (IC50=280 uM).
    GY06580 SMAP SMAP (DT-061, DT061) is an orally bioavailable small molecule activator of PP2A, inhibits KRAS-driven tumor growth.
    GY06581 Razuprotafib sodium Razuprotafib sodium is a potent protein tyrosine phosphatase β(HPTPβ) inhibitor.
    GY06582 GS-5734 GS-5734 (Remdesivir) is a monophosphoramidate prodrug of adenosine analogue that exhibits antiviral activity against multiple variants of EBOV (EC50=70-140 nM) and other filoviruses (EC50=0.019-1.48 uM) in cell-based assays.
    GY06583 SMAP-2 SMAP-2 (DT-1154) is an orally bioavailable small molecule activator of PP2A, binds to PP2A Aα scaffold subunit and inhibits KRAS-driven tumor growth both in vitro and in vivo.
    GY06584 P62-mediated mitophagy inducer P62-mediated mitophagy inducer (PMI) is a small molecule P62-mediated mitophagy inducer that activates mitophagy without recruiting Parkin or collapsing membrane potential and retains activity in cells devoid of a fully functional PINK1/Parkin pathway.
    GY06585 LP99 LP99 is the first potent and selective BRD7/9 bromodomain inhibitor with Kd of 99 nM for BRD9.
    GY06587 IACS-7e IACS-7e is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement).
    GY06588 E-7386 E-7386 (E7386) is a potent, orally active modulator of CBP/beta-catenin, disrupts the interaction and inhibits canonical Wnt signaling pathway /TCF reporter gene activity in LiCl-stimulated HEK-293 and MDA-MB-231 with IC50 of 55 and 73 nM, respectively.
    GY06589 PF-6689840 PF-6689840 (PF6689840) is a potent and selective Type II PTK6/Brk inhibitor with IC50 of 54 nM in biochemical assays.
    GY06590 PF-6683324 PF-6683324 (PF6683324) is a potent and selective Type II PTK6/Brk inhibitor with IC50 of 76 nM in biochemical assays.
    GY06593 Tecalcet HCl Tecalcet (R-568.
    GY06594 TCDD A potent AHR (aryl hydrocarbon receptor) agonist that induces degradation of AhR by the ubiquitin-proteasome pathway.
    GY06596 FICZ FICZ is a high affinity aryl hydrocarbon receptor (AhR) agonist with Kd of 70 pM.
    GY06597 GS-493 GS-493 is a novel potent, selective SHP2 inhibitor with IC50 of 71±15 nM in enzyme assay.
    GY06599 MS-402 A potent, selective inhibitor of the first bromodomain of BET (BRD4-BD1) with Ki of 77 nM.
    GY06600 BI 894999 BI 894999 is a novel potent, selective BET inhibitor with IC50 of 5 and 41 nM for BRD4-BD1 and BRD4-BD2 bromodomains, respectively.
    GY06601 INCB054329 INCB054329 is a novel potent, orally bioactive BET inhibitor that inhibits binding of BRD2, BRD3 and BRD4 to an acetylated histone H4 peptide with low nanomolar potency.
    GY06604 LLY-2707 LLY-2707 (LLY 2707, LLY2707) is a novel potent, selective, nonsteroidal glucocorticoid receptor antagonist with Ki of 2.13 nM.
    GY06605 Garvagliptin A potent, selective dipeptidyl peptidase-4 (DPP-4) inhibitor for treatment for type 2 diabetes.
    GY06606 Gemopatrilat A potent, orally available, dual ACE-neutral endopeptidase (vasopeptidase) inhibitor with IC50 of 12 and 63 nM, respectively.
    GY06607 INH154 INH154 is a novel small molecules disrupting Hec1/Nek2 interaction, inhibits HeLa and MDA-MB-468 cancer cells growth with IC50 of 0.20 and 0.12 uM, respectively.
    GY06608 GPR39 modulator 7 GPR39 modulator 7 is a Hedgehog pathway inhibitor that has high cellular potency (EC50=20 nM) in the reporter gene assay, activates the orphan receptor GPR39 and potently reduces of Gli1 and Ptch1 mRNA levels.
    GY06609 GPR39 modulator 3 GPR39 modulator 3 is a Hedgehog pathway inhibitor that has high cellular potency (EC50=5 nM) in the reporter gene assay, activates the orphan receptor GPR39 and potently reduces of Gli1 and Ptch1 mRNA levels.
    GY06610 SNAP 5114 A GABA transport inhibitor with IC50 of 5, 21, 388 and 140 uM for hGAT-3, rGAT-2, hGAT-1 and BGT-1, respectively.
    GY06611 Rostafuroxin Rostafuroxin (PST2238) is potent, selective, orally active Na-K-ATPase inhibitor, displaces 3H ouabain from dog kidney Na+,K+-ATPase with IC50 of 1.5 nM.
    GY06612 LB-102 A potent, selective serine/threonine protein phosphatase 2A (PP2A) inhibitor with IC50 of 0.4 uM.
    GY06613 BC-1215 A highly unique, selective E3 ligase F box component Fbxo3 inhibitor with IL1β IC50 of 0.9 ug/mL.
    GY06614 Relacorilant A potent, selective glucocorticoid receptor (GR) antagonist with Ki of 7.2 nM in the HepG2 TAT assay.
    GY06615 Tecalcet Tecalcet (R-568.
    GY06616 PF-05381941 A potent, dual TAK1/p38a inhibitor with IC50 of 156/186 nM respectively, with good kinome selectivity against 50 representative kinases.
    GY06617 Leucettamine B Leucettamine B is a potent inhibitor of CLK1 (IC50=15 nM), Dyrk1A (IC50=40 nM), and Dyrk2 (IC50=35 nM) and a moderate inhibitor of CLK3 (IC50=4.5 uM).
    GY06619 NNC-711 NNC-711 is a potent and selective inhibitor of GABA uptake by GAT-1 with IC50 of 0.04 uM.
    GY06620 SBI-425 SBI-425 is a potent, selective, orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor with IC50 of 16 nM, shows high selectivity over other alkaline phosphatases including IAP and PLAP.
    GY06621 TD-139 TD-139 (TD139) is a highly potent, selecitve inhibitor of Galectin-3 (Gal-3) carbohydrate binding domain with Ki of 14 nM.
    GY06622 BAY-826 BAY-826 (BAY826) is a novel selective, highly potent, orally available TIE-2 inhibitor (dissociation constant=1.6 nM).
    GY06623 TAI-95 A potent, orally abioavailable Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum (GI50=14.29-73.65 nM, breast cancer cell lines).
    GY06624 BR103 BR103 is a potent, metabolically stable and highly selective small molecule agonist of complement C3a receptor (C3aR) with EC50 of 22 ± 8  nM.
    GY06625 CPDA A potent SHIP2 inhibitor that enhances in vitro insulin signaling through the Akt pathway more efficiently than AS1949490, and ameliorates abnormal glucose metabolism in diabetic (db/db) mice.
    GY06628 Factor D inhibitor 7 Factor D inhibitor 7 is a potent and selective, orally bioavailable inhibitor of Factor D with IC50 of 50 nM.
    GY06630 TC-2153 TC-2153 is a specific, small moelcule inhibitor of neuron-specific tyrosine phosphatase STEP with IC50 of 24.6 nM.
    GY06631 MK-8825 MK-8825 is a highly potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 17 nM for rat CGRP.
    GY06632 FAS-IN-1 FAS-IN-1 is a potent inhibitor of fatty acid synthase (FAS) wtih IC50 of 10 nM.
    GY06633 Atogepant A potent, selective and orally available CGRP receptor antagonist for the prevention of migraine.
    GY06635 Ciliobrevin D Ciliobrevin D is a cell-permeable, reversible, specific inhibitor of cytoplasmic dynein, blocks dynein-dependent microtubule gliding and ATPase activity while sparing kinesin dependent cellular trafficking.
    GY06636 Nek2 inhibitor A potent and selective NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 22 nM, >200-fold selectivity over Plk1, Mps1, Aurora A and CDK2.
    GY06638 TAK1-IN-1 TAK1-IN-1 is a potent, selective, Type I (ATP-competitive, DFG-in) TAK1 inhibitor with Kd of 59 nM, a thienopyrimidine scaffold that serves as a good starting point for medicinal chemistry.
    GY06639 Avacopan A potent, selective, orally availale C5aR (CD88) inhibitor with IC50 of 0.1 nM.
    GY06640 Tolcapone A selective, potent and reversible nitrocatechol-type inhibitor of catechol-O-methyltransferase (COMT) for treatment of Parkinson's disease.
    GY06641 BRK inhibitor P21d BRK inhibitor P21d is a potent, selective, cell permeable inhibitor of breast tumor kinase (Brk, PTK6) with IC50 of 30 nM, shows no inhibitory activity against Aurora B and Lck (IC50>20 uM).
    GY06642 TAI-1 A potent, small molecule Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum (GI50=13.48 nM K562 cells).
    GY06643 CC-220 A potent, next-generation modulator of cereblon E3 ubiquitin ligase with IC50 of 60 nM.
    GY06645 Imigliptin 2HCl A novel potent, selective, orally available DPP-4 inhibitor with IC50 of 9 nM.
    GY06646 NQ301 NQ301 (CD45 inhibitor 211, Compound 211) is a potent antithrombotic agent that inhibits thromboxane A2 receptor and synthase activity, also is a potent, selective inhibitor of CD45 tyrosine phosphatase with IC50 of 200 nM, >100-fold selectivity over other related PTPs (LAR, PTP1B, PTP-σ, SHP-1 and MKPX).
    GY06647 BI-99179 BI-99179 is a potent and selective inhibitor of type I fatty acid synthase (FAS) with IC50 of 79 nM.
    GY06648 SR12813 A potent and efficacious pregnane X receptor (PXR) activator with EC50 of 200 and 700 nM for human and rabbit PXR.
    GY06649 Velcalcetide Velcalcetide (AMG-416, Velcalcetide, Etelcalcetide, KAI-4169) is a potent, peptide agonist of CaSR, dose-dependenty increases IP1 accumulation with EC50 of 25 uM in cell based assays.
    GY06650 Minnelide A water-soluble prodrug of triptolide that is highly effective in reducing pancreatic tumor growth and spread, and improving survival.
    GY06651 PBI-4050 sodium PBI-4050 (Setogepram, PBI4050) is a synthetic analog of a medium-chain fatty acid that displays agonist and antagonist ligand affinity toward GPR40 and GPR84, respectively.
    GY06652 AZD-5248 AZD-5248 is a potent, selective, first generation, oral inhibitor of dipeptidyl peptidase 1 (DPP1).
    GY06653 BCI-215 A potent, tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor.
    GY06654 BCI A small-molecule, allosteric inhibitor of DUSP6 (dual-specificity phosphatase 6) with IC50 of 12.3 uM.
    GY06655 BRPF1B TRIM24-IN-34 BRPF1B TRIM24-IN-34 is a selective BRPF1B/TRIM24 dual inhibitor that binds with KD of 137 and 222 nM, respectively.
    GY06656 Siponimod Siponimod (BAF312) is a potent, selective S1P1/S1P5 receptor modulator with EC50 of 0.39/0.0.98 nM, >1,000-fold selectivity over S1P2/3/4.
    GY06658 ML197 ML197 is a potent, selective small molecule inhibitor of Cdc2-like kinases (CLK) and DYRK with IC50 of 96/40/206 nM for CLK1/CLK4/Dyrk1A, respectively.
    GY06659 Evogliptin A potent, long acting, reversible and competitive DPP-4 inhibitor with IC50 of 0.9 nM.
    GY06662 Etrasimod Etrasimod (APD334) is a potent, selective, centrally available S1P1 receptor antagonist with β-arrestin EC50 of 6.1 nM, internalizes human S1P1 in CHO cells expressing HA tagged S1P1 with IC50 of 1.88 nM.
    GY06663 AS-1949490 A potent, selective SHIP2 inhibitor with IC50 of 0.34/0.62 uM for mouse/human SHIP2.
    GY06666 Rivipansel sodium Rivipansel sodium (GMI-1070, PF-06460031) is a novel small molecule glycomimetic pan-Selectin antagonist with IC50 of 4.3 uM, 423 uM and 337 uM for E-selectin, P-selectin and L-selectin, respectively.
    GY06667 DBPR108 DBPR108 is a potent, selective, orally bioavailable and long-acting inhibitor of DPP4 with IC50 of 15 nM, >3,000-fold selectivity over DPP8, DPP9, FAP and DPP-II.
    GY06668 ZL-006 ZL-006 (ZL 006, ZL006) is a brain penetrant small molecule inhibitor of PSD-95/nNOS interaction that prevents glutamate-induced excitotoxicity and cerebral ischemic damage in vivo.
    GY06669 ZTM000990 ZTM000990 is a small-molecule antagonist of the oncogenic Tcf4/β-catenin protein complex with IC50 of 0.64 uM.
    GY06671 WZ-4-49-8 WZ-4-49-8 is a potent, selective c-Fes protein-tyrosine kinase inhibitor with IC50 of 67 nM.
    GY06672 CI-966 CI-966 (PD 126141) is a potent, selective inhibitor of the GABA transporter GAT-1 with IC50 of 0.26 and 1.2 uM for human and rat GAT-1, respectively.
    GY06673 CI-966 HCl CI-966 is a potent, selective inhibitor of the GABA transporter GAT-1 with IC50 of 0.26 and 1.2 uM for human and rat GAT-1, respectively.
    GY06674 GRL-0617 GRL-0617 is a potent, noncovalent SARS-CoV papain-like protease (PLpro) inhibitor with IC50 of 0.6 uM, Ki of 0.49 uM.
    GY06675 Plpro-IN-6 A potent, noncovalent SARS-CoV papain-like protease (PLpro) inhibitor with IC50 of 2.6 uM.
    GY06676 BR111 BR111 is a potent, highly selective and orally active antagonist of complement C3a receptor (C3aR) with IC50 of 85 ± 40  nM (inhibition of hC3a induced Ca2+ release on human macrophages).
    GY06677 PF-04191834 PF-04191834 (PF-4191834) is a potent, non‐iron chelating, non‐redox, selective and competitive inhibitor of 5-lipoxygenase (5‐LO) with Ki of 10 nM.
    GY06679 Sappanone A A homoisoflavanone found in Caesalpinia sappan, a potent, selective IMPDH2 inhibitor that covalently binds to Cys140 with Kd of 3.944 nM, almost 10 times lower than the Kd of binding to IMPDH1.
    GY06680 BC-1382 A potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction with IC50 of 5 nM.
    GY06681 Microcystin-LR A potent, selective inhibitor of protein phosphatase 2A (PP2A) with IC50 of 0.04 nM.
    GY06682 Razuprotafib Razuprotafib is a potent protein tyrosine phosphatase β (HPTPβ) inhibitor.
    GY06683 PBI-4050 PBI-4050 (Setogepram, PBI4050) is a synthetic analog of a medium-chain fatty acid that displays agonist and antagonist ligand affinity toward GPR40 and GPR84, respectively.
    GY06684 Ractopamine A small molecule TAAR1 agonist and β adrenoreceptor agonist that stimulates β1 and β2 adrenergic receptors.
    GY06685 rac Pterosin B rac Pterosin B is a potent and specific SIK3 signaling inhibitor that suppresses SIK3 downstream cascades by up-regulating the phosphorylation levels in the SIK3 C-terminal regulatory domain.
    GY06686 KIN-1400 A potent RIG-I-like receptor (RLR) agonist that triggers IRF3-dependent innate immune antiviral genes and IFN-β expression.
    GY06687 Pterosin B Pterosin B is a potent and specific SIK3 signaling inhibitor that suppresses SIK3 downstream cascades by up-regulating the phosphorylation levels in the SIK3 C-terminal regulatory domain.
    GY06690 YKL-05-099 YKL-05-099 (YKL 05-099) is a novel potent, selective pan-SIK inhibitor with IC50 of 10, 40 and 30 nM for SIK1, 2 and 3, respectively.
    GY06691 KIN-1408 A small-molecule MAVS-dependent IRF3 agonist that shows antiviral activity against Flaviviridae, Filoviridae (Ebola virus), Orthomyxoviridae (influenza A virus), Arenaviridae (Lassa virus) and Paramyxoviridae (RSVs, Nipah virus).
    GY06692 ARN-3236 ARN-3236 is a novel potent, selective, and orally active SIK2 inhibitor with IC50 of <1 nM.
    GY06693 MRT 199665 MRT 199665 is a potent salt-inducible kinases (SIKs) inhibitor with IC50 of 110, 12, 43 nM for SIK1,2,3 respectively.
    GY06694 Cavosonstat A potent, orally bioavailable inhibitor of S-nitrosoglutathione reductase (GSNOR) and CFTR modulator.
    GY06695 RO 5263397 A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) partial agonist with EC50 of 17 nM, >1,000-fold selectivity over human adrenergic α2A receptor.
    GY06696 N6022 A potent and reversible S-Nitrosoglutathione reductase (GSNOR) inhibitor with IC50 of 20 nM.
    GY06698 RO 5166017 A potent, selective TAAR1 agonist with Ki of 1.9, 2.7, 31 and 24 nM for mouse, rat, cynomolgus monkey and human TAAR1 stably expressed in HEK293 cells.
    GY06699 RO 5203648 A potent and selective TAAR1 partial agonist with Ki of 0.5, 1.0, 6.8 and 2.6 nM for mouse, rat, human and monkey TAAR1, respectively.
    GY06700 RO 5073012 A potent, selective, orally active TAAR1 partial agonist with Ki of 6 nM, EC50 of 23 nM (hTAAR1), 140-fold selectivity over β2 adrenergic receptors.
    GY06701 FT-011 A novel anti-fibrotic agent that prevents TGF-beta-stimulated production of collagen in cultured renal mesangial cells (55-70% inhibition at 30 uM).
    GY06702 THPN A potent nuclear receptor TR3 (Nur77)-specific targeting compound that can induce melanoma autophagy through a mitochondrial signaling pathway.
    GY06703 BMS-986202 BMS-986202 (BMS-986202, AM-152) is a potent, selective, orally available antagonist of the Lysophosphatidic Acid 1 Receptor (LPA1 receptor) with IC50 of 18 and 9 nM in calcium mobilisation and β-arrestin assays; fully inhibits the response to LPA in calcium mobilisation, β-arrestin, cAMP, GTPγS and RhoA functional assays.
    GY06704 ABC99 ABC99 is a potent, selective inhibitor of the Wnt-deacylating enzyme serine hydrolase NOTUM with IC50 of 13 nM, shows excellent selectivity across the serine hydrolase family.
    GY07351 SGL5213 SGL5213 is a potent, low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor with IC50 of 29 nM/20 nM for hSGLT1/hSGLT2.
    GY06706 JBJ-16-111 JBJ-16-111 is a small molecule that inhibits dengue virus (DENV) by binding to its envelope protein E.
    GY07076 BAY-850 BAY-850 is a potent, isoform selective, cellularly active ATAD2 bromodomain inhibitor with binding IC50 of 166 nM in TR-FRET assay
    GY07078 Teslexivir A first-in-class, small molecule protein-protein inhibitor of the interaction between the E1 and E2 proteins of HPV types 6 and 11
    GY07079 PH-46A A potent, first-in-class, oral small-molecule agent for the treatment of inflammatory bowel diseases.
    GY07080 PH-46A N-Methyl-D-Glucamine salt A potent, first-in-class, oral small-molecule agent for the treatment of inflammatory bowel diseases.
    GY07088 trans-AUCB A potent, specific and orally bioavailable soluble epoxide hydrolase (sEH) inhibitor with IC50 of 1.3 nM
    GY07089 Sirt2-PROTAC-1 A novel SirReal-based PROTAC that induces isotype-selective Sirt2 degradation (IC50=0.25 uM).
    GY07091 HJB-97 A potent BET bromodomian inhibitor with IC50 of 3-7 nM for BRD2/3/4 BD1 and BD2.
    GY07092 N3-PEG3-CH2COOH A PEG3 linker for PROTAC.
    GY07093 VHL Ligand 3 A VHL ligand for PROTAC.
    GY07094 VH-032 VH-032 (VHL ligand 1) is a VHL ligand for PROTAC and potent, small molecule inhibitor of the VHL/HIF-1α interaction with Kd of 185 nM.
    GY07095 VHL-2 A VHL ligand for PROTAC.
    GY07096 VHL Ligand 4 A VHL ligand for PROTAC.
    GY07097 N3-PEG4-CH2COOH A PEG4 linker for PROTAC.
    GY07098 N3-PEG2-CH2COOH A PEG2 linker for PROTAC.
    GY07099 CC-885 CC-885 (CC 885, CC885) is a novel E3 ligase cereblon (CRBN) modulator with potent anti-tumour activity mediated through the degradation of GSPT1
    GY07100 dBRD9 dBRD9 is a PROTAC that bridge the BRD9 bromodomain and the cereblon E3 ubiquitin ligase complex
    GY07105 ONO-0300302 A novel potent, slow tight binding LPA1 receptor antagonist with IC50 of 86 nM, Kd of 0.34 nM
    GY07108 ENT1-IN-39 A potent adenosine transport activity of ENT-1 with IC50 of 26.9 nM
    GY07110 Divin A potent chelator of iron that arrests late stages of cytokinesis by blocking the physical process of constriction in dividing cells
    GY07111 Sulfotransferase-IN-1 The first selective, cell-permeable inhibitor of GAG sulfotransferases with IC50 of 2.0-2.5 uM
    GY07115 HMCEF A novel P-selectin inhibitor that directly binds to P-selectin
    GY07116 Shield-1 A cell-permeable FKBP ligand that is designed to protect an otherwise unstable protein domain from degradation
    GY07117 PK-11195 An isoquinoline carboxamide that binds selectively to PBR (TSPO) with Ki of 3.1 nM in cerebellum, 4.1 nM in spinal cord
    GY07118 2-D08 A cell permeable, mechanistically unique inhibitor of protein sumoylation
    GY07119 Ro5-4864 A potent, selective ligand for the mitochondrial translocator protein 18kDa (TSPO/PBR)
    GY07120 HLY-78 An activator of the Wnt/β-catenin signaling pathway that targets the DIX domain of Axin
    GY07121 ABO dihydrochloride A small molecule ANXA7 GTPase activity inhibitor, induces mouse ESCs differentiation to VECs
    GY07123 PF-00446687 hydrochloride PF-00446687 hydrochloride (PF-446687) is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 nM
    GY07124 PF-00446687 PF-00446687(PF-446687) is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 nM
    GY07125 BMS-470539 A potent, selective, full agonist of human and murine MC1R with EC50 of 16.8 and 11.6 nM, respectively
    GY07128 CK-2127107 CK-2127107(CK-107, Reldesemtiv) is a novel orally active fast skeletal troponin activator, selectively activates fast skeletal myofibrils with EC50 of 3.4 uM
    GY07129 PF-DcpSi A potent inhibitor of the mRNA decapping scavenger enzyme (DcpS) with IC50 of 0.11 nM
    GY07130 Synta-66 A potent, selective CRAC channel Orai1 blocker with IC50 of 3 uM
    GY07132 CCT-367766 CCT-367766 (CCT367766) is a novel heterobifunctional PROTAC that binds and degrades the putative transcription factor regulator Pirin in cells.
    GY07133 LY3104607 A potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM
    GY07140 GPR30 inhibitor G15 G-15 (GPR30 inhibitor G15, G15) is a potent, selective GPER/GPR30 antagonist with Ki of 20 nM
    GY07141 GPR30 inhibitor G36 A potent, selective, cell-permeable GPER/GPR30 antagonist that inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 with IC50 of 112 nM and 165 nM, respectively
    GY07142 GPR30 inhibitor G1 A potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM
    GY07144 BI-0252 A potent, highly selective, orally active MDM2-p53 interaction inhibitor with IC50 of 4 nM
    GY07145 DS-3032b DS-3032b is a potent, selective, orally available MDM2-p53 inhibitor with potential antineoplastic activity
    GY07146 RO-2468 A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 6 nM
    GY07147 RO-5353 A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 7 nM
    GY07148 GNE-781 GNE-781 is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays
    GY07149 GNE-207 A novel potent, selective, orally active CBP/p300 bromodomain with IC50 of 1.0 nM
    GY07150 GB-88 GB-88 is a selective, orally available PAR2 antagonist that inhibits PAR2 activated Ca(2+) release with IC50 of 2 uM
    GY07151 GB-110 GB-110 is a potent, non-peptidic agonist of PAR2 that selectively induces PAR2-mediated intracellular Ca(2+) release in HT29 cells with EC50 of 0.28 uM
    GY07152 AZ-8838 AZ-8838 (AZ8838) is a potent, and selective PAR2 antagonist with Kd of 125 nM
    GY07154 THAL-SNS-032 THAL-SNS-032 is a novel CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN)
    GY07158 UE2343 UE2343 (UE-2343, Xanamem) is a potent, orally bioavailable, brain penetrant 11β-HSD1 inhibitor with IC50 of 24 nM in cell-free assays, with no activity for isozyme 11β-HSD2
    GY07163 PQ-912 A potent glutaminyl cyclase (QC) inhibitor that inhibits human, rat, and mouse QC with Ki of 20-65 nM
    GY07166 AX-000 A hit compound that inhibits the proliferation of human peripheral blood T cells stimulated with anti-CD3 with IC50 of <10 nM, inhibits TCR-Nck interaction.
    GY07167 APX-115 freebase APX-115 (Ewha 18278) is a first-in-class, orally active, pan-NADPH oxidase (Nox) inhibitor with Ki of 1.08, 0.57, 0.63 nM for Nox1, Nox2, and Nox4, respectively
    GY07168 APX-115 APX-115 (Ewha 18278) is a first-in-class, orally active, pan-NADPH oxidase (Nox) inhibitor with Ki of 1.08, 0.57, 0.63 nM for Nox1, Nox2, and Nox4, respectively
    GY07171 NU-8231 A small molecule inhibitor of MDM2-p53 protein-protein interaction with IC50 of 5.3 uM in ELISA assay
    GY07172 NU-8165 A small molecule inhibitor of MDM2-p53 protein-protein interaction with IC50 of 16 uM.
    GY07173 TDP-665759 A small molecule inhibitor of HDM2-p53 interaction with FP IC50 of 0.7 uM
    GY07176 AM-8735 A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.4 nM), cellular potency (SJSA-1 EdU IC50=25 nM), and favorable pharmacokinetic properties
    GY07177 RO-5963 A potent, dual MDM2/MDMX-p53 interaction inhibitor with IC50 of 17 and 24 nM, respectively
    GY07183 SP 141 A novel specific MDM2 inhibitor that promotes MDM2 auto-ubiquitination and degradation
    GY07186 DS-5272 A potent and orally active p53-MDM2 interaction inhibitor with IC50 of 2.4 nM
    GY05431 Cotylimide-VI Cotylimide-VI (CTL-VI) is a small molecule that perturbs plant hormone strigolactone accumulation and inhibits hypocotyl growth.
    GY05432 BIO 8898 BIO 8898 is a synthetic, CD40-CD154 co-stimulatory interaction inhibitor that inhibits the TNF family cytokine CD40L binding to CD40-Ig with a potency of IC50=25 uM.
    GY05433 UK-396082 UK-396082 is a potent and selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (activated TAFI.
    GY05434 AA147 AA147是转录因子ATF6的特异性小分子激动剂,其激活ATF6并影响干细胞的分化。AA147 is a specific, small molecule agonist of transcription factor ATF6, activates ATF6 and influences differentiation of stem cells.
    GY05435 Spliceostatin A Spliceostatin A is a methylated derivative of FR-901464 that inhibits pre-mRNA splicing.
    GY05437 Adrenosterone A steroid hormone with a weak androgenic effect, and an intermediate/prohormone of 11-ketotestosterone.
    GY05438 MPO-IN-28 A novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM.
    GY05439 VPC-18005 VPC-18005 (VPC18005) is a novel small molecule ERG (ETS-related gene) antagonist that inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, disrupts the ERG binding to DNA (Kd=250 uM).
    GY05440 6-FITC 6-Fluorescein isothiocyanate(6-FITC) is a derivative of fluorescein used in wide-ranging applications including flow cytometry.
    GY05442 6-FAM The single isomer, 6-FAM, contains a carboxylic acid that can be used to react with primary amines via carbodiimide activation of the carboxylic acid. Fluorescein is the most common fluorescent derivatization reagent for labeling biomolecules. In addition to its relatively high absorptivity, excellent fluorescence quantum yield, and good water solubility, fluorescein has an excitation maximum that closely matches the 488 nm spectral line of the argon-ion laser.
    GY05443 RH01687 RH01687 is a small molecule that protect pancreatic β cells against endoplasmic reticulum stress-induced cell death.
    GY05444 RH01386 RH01386 is a small molecule that protect pancreatic β cells against endoplasmic reticulum stress-induced cell death.
    GY05445 Naxillin Naxillin is the first non-auxin-like molecule that promotes root branching, activates a subset of auxin-induced transcripts, including AUX/IAA, SAUR and PIN families.
    GY05446 4-CPPC 4-CPPC is the first reversible and selective inhibitor of pro-inflammatory protein macrophage migration inhibitory factor-2 (MIF-2) with Ki of 33 uM, 13-fold selectivity for human MIF-2 versus human MIF-1.
    GY05447 7DG 7DG (7-Desacetoxy-6,7-dehydrogedunin) is a selective inhibitor of protein kinase R (PKR) that directly interact with the C-terminal of PKR.
    GY05448 Teglicar Teglicar (ST-1326) is a potent, selective and reversible inhibitor of liver carnitine palmitoyl-transferase 1 (L-CPT1) with IC50 of 0.68 uM, Ki of 0.36 uM.
    GY05449 Laquinimod Laquinimod (ABR-215062) is an immunoregulator derived from Linomide, has been shown to completely inhibit the development of murine acute experimental autoimmune encephalomyelitis (EAE).
    GY05450 Difluprednate A FDA approved topical corticosteroid indicated for the treatment of inflammation and pain associated with ocular surgery.
    GY05452 JI051 JI051(JI-051) is a specific compound that inhibits the cancer-associated transcription factor Hes1 via the PHB2 chaperone, blocks Hes1-mediated transcriptional repression.
    GY05453 KSC-34 KSC-34 (PDIA1 inhibitor KSC-34) is a potent, selective protein disulfide isomerase A1 (PDIA1) inhibitor, 30-fold selectivity for the A-site over the A' site.
    GY05454 Olesoxime Olesoxime (TRO 19622) is a cholesterol-like compound that binds directly to two components of the mitochondrial permeability transition pore: the voltage-dependent anion channel and TSPO (or PBR).
    GY05455 K-604 K-604 is a potent, selective and competitive ACAT-1 inhibitor with IC50 of 0.45 uM for human ACAT-1, displays 229-fold selectivity over ACAT-2.
    GY05456 Ipfencarbazone A substance being developed for the control of weeds such as watergrass in rice.
    GY05457 RX-055 A tailored WOBE437-derived diazirine-containing photoaffinity probe that irreversibly blocks membrane transport of both endocannabinoids.
    GY05458 EML-633 A small-molecule inhibitor of Spindlin1 (SPIN1) with Kd of 2 uM.
    GY05459 EML-631 A small-molecule inhibitor of Spindlin1 (SPIN1) with Kd of 4 uM.
    GY05460 PNPLA4-IN-1 PNPLA4-IN-1 is a potent, selective, and irreversible PNPLA4 inhibitor with IC50 of 1.8 uM (separated membrane proteome fraction), shows in-cell inhibition of PNPLA4 with IC50 of 11.7 uM.
    GY05462 PF-6808472 PF-6808472 (XO44) is a sulfonyl fluoride chemical probe that covalently labels a broad swath of the intracellular kinome with high efficiency.
    GY05463 Sudemycin K Sudemycin K is a synthetic antitumor splicing inhibitor with IC50 of 15 nM (MCL1 alternative splicing regulation), shows cytotoxicity in HeLa cells with IC50 of 2.3 nM.
    GY05464 CCG 258001 A potent, relatively selective G protein-coupled receptor kinase GRK2 inhibitor with IC50 of 280 nM.
    GY05466 MN58b MN58b is a potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.4 uM, >30-fold selectivity over ChoKβ and does not affect MAPKs, PI3Ks, and other enzymes involved in the regulation of phospholipid metabolism.
    GY05467 JCR 795b JCR 795b is a competitive, small molecule inhibitor of choline kinase (ChoK) with in vitro IC50 of 3.5 uM.
    GY05468 Lin28-IN-1 Lin28-IN-1 is a small-molecule inhibitor of the Lin28/let-7 interaction with IC50 of 4.03 uM.
    GY05471 PAT-1251 PAT-1251 (PAT 1251, PAT1251) is a potent, selective and orally bioavailable lysyl oxidase-like 2 (LOXL2) inhibitor with IC50 of 0.71 uM in human whole blood assays, with high selectivity over LOX (400-fold) and other amine oxidases.
    GY05472 JHU-083 JHU-083 is an orally available prodrug of the glutaminase inhibitor 6-diazo-5-oxo-L-norleucine (DON), blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.
    GY05473 YPC-22026 YPC-22026, a metabolically stable derivative of YPC-21661, is a novel small molecule inhibitor of the transcription factor Zinc-finger protein 143 (ZNF143), inhibits the binding of ZNF143 to DNA.
    GY05475 AKR1C3 inhibitor KV-37 AKR1C3 inhibitor KV-37 is a potent, isoform selective and metabolically stable inhibitor of Aldo-keto reductase 1C3 (AKR1C3) with IC50 of 66 nM, displays 109-fold selectivity over AKR1C2.
    GY05476 GRK2-IN-115h HCl A highly potent and selective GRK2 inhibitor with IC50 of 18 nM.
    GY05478 TES-1025 TES-1025 (TES1025) is a potent, selective inhibitor of human ACMSD (α-Amino-β-carboxymuconate-ε-semialdehyde decarboxylase) with IC50 of 13 nM, increases NAD+ levels in cellular systems.
    GY05479 EB-3D EB-3D is a novel potent and selective choline kinase ChoKα inhibitor with IC50 of 1.0 uM (purified ChoKα1), strongly impairs cell proliferation in a variety of different cancer cell lines.
    GY05480 ML404 ML404 is a small molecule inhibitor of mtPTP, inhibits mitochondrial swelling with EC50 of 4.9 nM, shows no effect on mitochondrial coupling at >100 uM.
    GY05481 H3B-8800 H3B-8800 is an orally available splicing modulator that targets spliceosome SF3b complex containing either WT or mutant SF3B1 (binding IC50 of 0.3-2 nM).
    GY05482 SBE-β-CD A sulfobutylether β-cyclodextrin derivative, it is an excipient or a formulating agent used to increase the solubility of poorly soluble drugs. .
    GY05483 CU-3 CU-3 (DGKα inhibitor CU-3) is a is a novel potent, selective diacylglycerol kinase α (DGKα) inhibitor with IC50 of 0.6 uM, targets the catalytic region, but not the regulatory region.
    GY05486 CBR-096-4 A derivative of the antifungal drug itraconazole (ITA) as an inhibitor of MFB cell fate in resident fibroblasts derived from multiple murine and human tissues.
    GY05487 KG-548 KG-548 is an ARNT/TACC3 disruptor (IC50=25 uM) that selectively bind within the ARNT PAS (Per-ARNT-Sim) domain that recruits TACC3.
    GY05488 MN30 MN30 (Methyl-3,4-dephostatin.
    GY05489 CD38 inhibitor 78c CD38 inhibitor 78c is a potent, specific, reversible CD38 inhibitor with Ki of 14.5 nM for recombinant human CD38.
    GY05491 Hemicholinium-3 Hemicholinium-3 (HC-3) is a competitive, small molecule inhibitor of choline kinase (ChoK) with ex vivo IC50 of 500 uM, also bolcks the sodium and chloride-dependent transport system and affects choline acetyltransferase.
    GY05492 DS-2330 DS-2330 is a phosphorous lowering agent for treating hyperphosphatemia in chronic kidney disease.
    GY05493 JAS239 JAS239 is a novel carbocyanine dye that binds and competitively inhibits choline kinase (ChoK) intracellularly, prevents choline phosphorylation and induces cell death in breast cancer cell lines.
    GY05494 ARN 726 ARN726 is a potent, selective, orally bioavailable N-acylethanolamine acid amidase (NAAA) inhibitor with IC50 of 63 nM (r-NAAA) and 27 nM (h-NAAA).
    GY05495 TD-1 Hemoglobin modulator TD-1 (TD-1) is a novel allosteric effector of hemoglobin that increases hemoglobin oxygen affinity and reduces SS erythrocyte sickling.
    GY05498 IACS-010759 IACS-010759 (IACS010759) is a small molecule inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), targets complex I of the mitochondrial electron transport chain.
    GY05499 BMT-090605 BMT-090605 (BMT 090605, BMT090605) is a potent, selective adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50 0.6 nM.
    GY05500 BMT-046091 BMT-046091 (BMT046091) is a potent and selective AAK1 inhibitor with IC50 of 2.8 nM.
    GY05501 SB-204990 SB-204990 is the cell-penetrant, orally active gamma-lactone prodrug of the potent ATP citrate-lyase (ACLY) inhibitor SB-201076.
    GY05502 NCT-502 NCT-502 is a small molecule 3-phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3.7 uM) that reduces the production of glucose-derived serine in cells and suppress the growth of PHGDH-dependent cancer cells.
    GY05503 Fulacimstat Fulacimstat (BAY 1142524, BAY1142524) is a potent, orally available chymase inhibitor with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively.
    GY05507 LP-935509 LP-935509 is a potent, selective and brain-penetrant adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50 of 3.3 nM.
    GY05508 Rovazolac An novel anti-inflammatory agent.
    GY05509 PF-06282999 A potent, highly selective and irreversible inhibitor of myeloperoxidase (MPO) with Kinact/KI of 116000 M-1s-1.
    GY05510 Isobutyl-deoxynyboquinone Isobutyl-deoxynyboquinone (IB-DNQ) is a selective substrate for NAD(P)H:quinone oxidoreductase (NQO1), produces ROS, and induces cytotoxicity in cancer cells in an NQO1-dependent manner.
    GY05511 CCG-203586 A potent, CNS-active Glucosylceramide synthase (GCS) inhibitor with IC50 of 27 nM.
    GY05512 Herboxidiene Herboxidiene (GEX1A.
    GY05513 Pitstop 2 A small molecule inhibitor of clathrin terminal domain and inhibits clathrin-mediated endocytosis.
    GY05514 Lucerastat A galactose analogue that is an UDP-glucose ceramide glucosyltransferase (UGCG/GCS) inhibitor (IC50=41.4 uM).
    GY05516 PE859 PE859 is a novel, orally active tau aggregation inhibitor that inhibits the heparin-induced aggregation of both 3RMBD and full length tau with IC50 of 0.81 uM and 2.23 uM, respectively.
    GY05518 PF-03382792 PF-03382792 (PF-3382792) is a clinical compound under phase 1 investigation for an unknown indication.
    GY05519 Setafrastat Setafrastat is a small molecule hair growth stimulator.
    GY05520 ZINC-3573 racemate ZINC-3573 racemate is a potent, selective agonist of the atypical opioid receptor MRGPRX2 (EC50=3 uM), showing little activity against 315 other GPCRs and 97 representative kinases.
    GY05521 ARN 077 ARN077 is the first potent, selective N-acylethanolamine acid amidase (NAAA) inhibitor with IC50 of 7 nM on both rat NAAA and human NAAA.
    GY05523 trans Ned-19 trans Ned-19 is a cell-permeant chemical probe for the Ca(2+)-releasing second messenger NAADP, blocks NAADP signaling (IC50=6 nM, inhibition of Ca2+ release).
    GY05524 R 283 A potent, irreversible inhibitor of human tissue transglutaminase (hTG2).
    GY05525 L 682777 A potent, irreversible inhibitor of human tissue transglutaminase (hTG2).
    GY05526 ATR-101 ATR-101 (PD-132301, Nevanimibe) is a selective and potent inhibitor of ACAT1 with IC50 of 52 nM.
    GY05528 Pitstop 1 A potent, selective inhibitor of clathrin-independent endocytosis with IC50 of 18 uM (inhibition of clathrin TD-amphiphysin B/C complex formation).
    GY05529 Thioflavin S A homogenous mixture of compound that is used to stain amyloid plaques, binds to amyloid fibrils but not monomers and gives a distinct increase in fluorescence emission.
    GY05530 RU-505 RU-505 is an effective inhibitor of the Aβ42-fibrinogen interaction with IC50 of 2.72 uM in FP assays.
    GY05531 Padsevonil Padsevonil (UCB-0942, UCB0942) is a potential anti-seizure agent that functions as a pre- and post-synaptic inhibitor.
    GY05532 TMP-153 TMP-153 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor with IC50 of 5-10 nM for the hepatic and intestinal ACAT from various animals.
    GY05533 N-acetyl lysyltyrosylcysteine amide N-acetyl lysyltyrosylcysteine amide (KYC) is a potent, tripeptide inhibitor of myeloperoxidase (MPO), inhibits MPO-mediated hypochlorous acid (HOCl) formation (IC50=7 uM) and nitration/oxidation of LDL.
    GY05535 ACT-389949 ACT-389949 is a novel potent and selective formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX) agonist with EC50 of 3 nM, shows potential for the treatment of inflammatory disorders.
    GY05536 KP-1019 A ruthenium complex anticancer agent that is useful for metastatic tumors and cis-platin resistant tumors.
    GY05537 EXEL-0346 EXEL-0346 (EXEL0346) is a novel potent, orally active Glucosylceramide synthase (GCS) inhibitor with IC50 of 2 nM.
    GY05538 TRX-0237 Methylate TRX-0237 Methylate (LMTX) is a Tau aggregation inhibitor (TAI) with Ki of 0.12 uM for intracellular TAI activity.
    GY05539 GNX-865 GNX-865 is a potent mitochondrial permeability transition pore (mPTP) inhibitor with EC50 of 105 uM (mitochondrial swelling).
    GY05540 LQB-118 An orally active pterocarpanquinone that exhibits antitumoral and antileishmanial activity both in vitro and in vivo.
    GY05542 R-59949 A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 0.01-10 uM in isolated platelet membranes and in intact platelets.
    GY05543 Sudemycin E Sudemycin E is an alternative splicing inhibitor that binds to the U2 small nuclear ribonucleoprotein (snRNP) component SF3B1, causes a rapid change in alternative pre-messenger RNA splicing.
    GY05544 Nexinhib 20 Nexinhib 20 is a novel small molecule neutrophil exocytosis inhibitor (IC50=0.33 uM) that specifically inhibits Rab27a-JFC1 binding (IC50=2.6 uM) but does not interfere with the interaction of other Rab GTPases and effectors.
    GY05546 Emixustat HCl Emixustat (ACU-4429) is a first in class small-molecule inhibitor of the visual cycle isomerase (RPE65) with IC50 of 4.4 nM.
    GY05547 Emixustat Emixustat (ACU-4429) is a first in class small-molecule inhibitor of the visual cycle isomerase (RPE65) with IC50 of 4.4 nM.
    GY05549 BCI-137 BCI-137 is a chemical compound able to compete with Argonaute 2 miRNAs binding, binds to Ago2 with Kd of 126 uM.
    GY05550 Z62954982 Z62954982 is a potent, specific Rac1 inhibitor, reduces the intracellular levels of Rac1-GTP in a concentration-dependent manner with IC50 of 12 uM, 4 times more effective than NSC23766 (IC50=50 uM).
    GY05552 FR-900359 A specific, membrane-permeable inhibitor of Gq signaling.
    GY05553 ML359 ML359 is a small molecule, specific inhibitor of Protein disulfide isomerase (PDI) with IC50 of 250 nM.
    GY05554 CXL017 CXL017 is a small molecule that has selective cytotoxicity toward MDR cancer cell lines in vitro, through inhibition of the sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA) with IC50 of 15 uM.
    GY05555 5S rRNA modificator 2 A novel chemical probe that enable selective 2’-hydroxyl acylation for accurate RNA structural analysis in living cells.
    GY05557 ALZ-801 ALZ-801 is an orally available, valine-conjugated prodrug of tramiprosate, a small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor for the treatment of Alzheimer's disease.
    GY05558 Z-DON A potent, irreversible and cell permeable inhibitor of tissue transglutaminase with IC50 of 20 nM.
    GY05560 CK-37 A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site.
    GY07344 Sephin1 Sephin1(IFB-088) is a selecitive PPP1R15A inhibitor, but not the related regulatory phosphatase PPP1R15B.
    GY07190 F3406 A novel small-molecule arenaviruse inhibitor that exhibits strong anti-LCMV activity (IC50<1 uM) without cell toxicity
    GY07202 Dihydromunduletone Dihydromunduletone is a rotenoid derivative that selectively inhibits GPR56 (IC50=21 uM) and GPR114/ADGRG5, but not GPR110 or Class A GPCRs
    GY07203 PF-06678419 PF-06678419 (PF06678419) is a potent, selective inhibitor of the Na+/citrate transporter NaCT (SLC13A5) that shows inhibition of citrate uptake in the HEKNaCT cells with IC50 of 0.44 uM
    GY07204 PF-06649298 A potent, selective inhibitor of the Na+/citrate transporter NaCT (SLC13A5) that shows inhibition of citrate uptake in the HEKNaCT cells with IC50 of 0.41 uM
    GY07207 GWJ-A-23 GWJ-A-23 (GWJ-23, GWJ23) is a potent, selective autotaxin inhibitor with Ki of 18 nM, an analog of the known ATX inhibitor S32826 and has improved aqueous solubility compared with the parent compound
    GY07208 ZQ-16 A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM
    GY07209 IND-114338 A novel antiprion compound with EC50 of 68 nM, significantly increases monoglycosylated/diglycosylated PrPSc.
    GY07232 IRAK4-IN-28 A novel potent, selective IRAK4 inhibitor with IC50 of 51 nM
    GY07237 SNIPER(ABL)-062 SNIPER(ABL)-062 is a novel, potent SNIPER molecule that tethers BCR-ABL inhibitor to a ligand of IAP, causes potent BCR-ABL degradation
    GY07238 MZ-242 A novel potent, selective Sirt2 inhibitor with IC50 of 0.118 uM
    GY07239 SirReal1 A novel potent, selective Sirt2 inhibitor with IC50 of 3.745 uM
    GY07241 GPR120 agonist 4x A potent, selective, orally bioavailable GPR120 agonist with EC50 of 42 nM in calcium flux assays
    GY07242 Ischemin A cell permeable CBP bromodomain inhibitor with Kd of 19 uM
    GY07246 SCB-4380 The first potent, selective inhibitor for PTPRZ (protein tyrosine phosphatase receptor-type Z) with IC50 of 0.4 uM against human Z-ICR-catalyzed hydrolysis
    GY07248 PAT-505 PAT-505 (PAT 505, PAT505) is a potent, selective, noncompetitive, and orally active autotaxin inhibitor with IC50 of 2.0 nM against the lysoPLD activity of human ATX
    GY07249 PAT-048 PAT-048 (PAT048) is a potent, selective, noncompetitive autotaxin inhibitor with IC50 of 1.1 nM against the lysoPLD activity of human ATX
    GY07254 A-1048400 A-1048400(A 1048400) is a novel potent, selective, orally active N-type and T-type calcium channel blocker with IC50 of 1.4 and 1.2 uM, respectively
    GY07255 BETd-260 BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL
    GY07256 BETd-260 trifluoroacetate BETd-260 trifluoroacetate (ZBC260, BETd 260 TFA) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL
    GY07257 MPK-09 A highly potent, selective mutant p53 (R175H, R249S, R273H, R273C) reactivator
    GY07258 LY2922470 LY2922470 (LY-2922470) is a potent, selective, orally available GPR40 agonist with EC50 of 7 nM
    GY07259 LY2922083 A potent, selective, orally available GPR40 agonist with EC50 of 9 nM
    GY07260 LY2881835 A potent, selective, orally available GPR40 agonist with EC50 of 8 nM
    GY07262 TBK1 PROTAC 1 A novel potent, selective TBK1 PROTAC with DC50 of 12 nM, selectively degrades TBK1 with excellent selectivity against a related kinase IKKε
    GY07263 OSU-03013 A novel potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 of 2 uM
    GY07269 SPM-242 A potent, selective S1P3 antagonist with Ki of 0.25 nM
    GY07270 CM11 A homo-PROTAC, bivalent small-molecule dimerizer of the VHL E3 ubiquitin ligase to induce self-degradation.
    GY07274 IND125 A novel brain penetrant antiprion compound with EC50 of 57 nM, prevents both PrP(Sc) accumulation and astrocytic gliosis in the cerebrum
    GY07276 Ischemin sodium A cell permeable CBP bromodomain inhibitor with Kd of 19 uM
    GY06707 SALL4 peptide FFW SALL4 peptide FFW (RRKFAKFQWI, FFW peptide) is a potent therapeutic SALL4 peptide antagonist of SALL4-NURD (nucleosome remodeling deacetylase) interaction with target affinity of 23 nM
    GY06708 RTI-13951-33 RTI-13951-33 is a potent, selective, brain-penetrant agonist of the orphan receptor GPR88 with EC50 of 25 nM in in vitro cAMP functional assay
    GY06709 MS645 MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ), shows12- to 28-fold gain in affinity for binding to the tandem BD1-BD2 over the single BD1 or BD2
    GY06710 BTK PROTAC 9 BTK PROTAC 9 is a novel potent PROTAC for BTK with DC50 of 5.9 nM in cultured Ramos cells, requires simultaneous engagement of BTK and CRBN to effectively degrade BTK
    GY06711 BTK PROTAC 10 BTK PROTAC 10 is a novel potent PROTAC for BTK with DC50 of 1.1 nM in cultured Ramos cells
    GY06713 CR6086 CR6086 (CR-6086) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM
    GY06714 CDK12 inhibitor 2 CDK12 inhibitor 2 is a potent, selective, non-covalent CDK12 inhibitor with IC50 of 52 nM, displays >192-fold selectivity over CDK2/7/8/9
    GY06716 MAI-400 MAI-400 (MAI400) is a novel peptide inhibitor of APC-Asef interaction with Kd of 12 nM and IC50 of 0.25 uM
    GY06717 RORγt inverse agonist 32 RORγt inverse agonist 32 is a potent, orally bioavailable inverse agonist of RORγt with IC50 of 9 nM in SPA binding assays
    GY06718 CCR6 inhibitor 35 CCR6 inhibitor 35 is a potent and selective CCR6 inhibitor with IC50 of 6.0 nM (hCCR6)
    GY06720 Cyclophilin inhibitor C31 Cyclophilin inhibitor C31 (SMCypI C31) is a small-molecule cyclophilin (CypA) inhibitor (SMCypI) with PPIase inhibition IC50 of 0.1 uM, displays anti-HCV activity (HCV Gt1b replicon EC50=0.4 uM) and disrupts the CypA-NS5A interaction
    GY06721 RAS inhibitor Abd-7 RAS inhibitor Abd-7 is a potent RAS-binding compound (Kd=51 nM) that interacts with RAS in cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signalling
    GY06722 AM9405 AM9405 (AM-9405) is novel potent, peripherally active cannabinoid type 1 (CB1) and 5-HT3 receptor agonist, inhibits the EFS-induced twitch contraction of the ileum and the colon with IC50 of 0.076 and 45.71 nM, respectively
    GY06723 KRAS inhibitor Cmpd2 KRAS inhibitor Cmpd2 is a small-molecule compound that blocks biochemical and cellular functions of KRASG12V with IC50 of 0.8 uM in vitro
    GY06724 VERU-111 analogue 13f VERU-111 analogue 13f is a novel potent colchicine binding site inhibitor (CBSI) in tubulin with potential anticancer activities
    GY06725 MB 07811 MB 07811 (MB07811) is an orally bioavailable, liver-targeted prodrug of MB07344, which is a thyroid hormone receptor-beta agonist (TRβ) agonist, efficiently converted to MB07344 by liver microsomes in vivo
    GY06726 MP-HJ-1b MP-HJ-1b is a novel potent inhibitor of microtubule and tumor cell growth, binds the colchicine pocket at the intra-dimer interface, depolymerizes microtubules and affects spindle formation
    GY06727 NTCP binder peptide WL4 NTCP binder peptide WL4 is a macrocyclic peptide, pan-genotypic inhibitor of HBV cellular entry via targeting the cell-surface receptor for HBV, sodium taurocholate cotransporting polypeptide (NTCP, Kd=42 nM), reduces HBs antigen levels in culture supernatants with IC50 of 0.66 uM
    GY06728 NTCP binder peptide WD1 NTCP binder peptide WD1 is a macrocyclic peptide, pan-genotypic inhibitor of HBV cellular entry via targeting the cell-surface receptor for HBV, sodium taurocholate cotransporting polypeptide (NTCP, Kd=15 nM), reduces HBs antigen levels in culture supernatants
    GY06729 Brusatol Brusatol (NSC 172924, (+)-Brusatol) is a quassinoid extracted from Brucea Esters, can inhibit HIF-1 signaling pathway, also is a potent Nrf2 inhibitor
    GY06730 GSK3004774 GSK3004774 (GSK-3004774) is a potent, nonabsorbable, gastrointestinally-restricted agonist of calcium-sensing receptor (CaSR) with pEC50 of 7.3.
    GY06731 mutant EGFR inhibitor B30 mutant EGFR inhibitor B30 is a potent, selective, next-generation EGFR mutants inhibitor with IC50 of 1.1 and 7.2 nM for EGFRL858R and EGFRL858R/T790M/C797S, respectively
    GY06732 WY-135 WY-135 (WY135) is a novel potent inhibitor of ALK and ROS1 with IC50 of 1.2 and 0.48 nM, respectively
    GY06733 MF-094 MF-094 (MF094) is a potent, highly selective inhibitor of ubiquitin specific protease 30 (USP30) with IC50 of 0.12 uM, demonstrates <30% inhibitory activity for a panel of 22 USPs assays at 10 uM
    GY06734 A12B4C3 A12B4C3 (hPNKP inhibitor A12B4C3) is a specific, noncompetitive inhibitor of the human DNA repair enzyme polynucleotide kinase/phosphatase (hPNKP) with IC50 of 60 nM, displays no inhibition of calcineurin and protein phosphatase-1 or APTX.
    GY06735 VXc-486 VXc-486 (VXc486) is a novel inhibitor of gyrase B, potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis in vitro with MICs of 0.03-0.30 μg/ml and 0.08-5.48 μg/ml, respectively
    GY06736 ATH686 ATH686 (ATH-686) is a potent and selective, second-generation inhibitor of mutant FLT3 protein kinase
    GY06737 AAE871 AAE871 (AAE-871) is a potent type I kinase inhibitor of FLT3 with IC50 of 34 nM, potently inhibits proliferation of FLT3-ITD- and D835Y-expressing cells (IC50<10 nM) through selective inhibition of FLT3 kinase activity.
    GY06738 TAK-615 TAK-615 (TAK615) is a potent, selective, negative allosteric modulator (NAM) of the LPA1 receptor, partially inhibits the LPA response with IC50 of 91 nM (60% at 10 uM) in calcium mobilisation assays.
    GY06739 SAR-100842 SAR-100842 (SAR100842) is a potent, selective, orally available antagonist of the Lysophosphatidic Acid 1 Receptor (LPA1 receptor) with IC50 of 31 nM in β-arrestin assays
    GY06740 LY900009 LY900009 (LY-900009) is an orally active small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein, inhibits Notch signalling in tumour cell lines and endothelial cells with IC50 of 0.005-20 nM
    GY06741 NIK inhibitor 4f NIK inhibitor 4f is a highly potent and selective NF-κB-inducing kinase (NIK) inhibitor with Ki of 0.23 nM, shows an IC50 of 34 nM in NF-κB reporter assays
    GY06742 UCB9608 UCB9608 (UCB-9608) is a potent, selective, orally bioavailable PI4KIIIβ inhibitor with IC50 of 11 nM
    GY06743 Tianeptinaline Tianeptinaline is a class I HDAC-selective, brain penetrant analogue of tianeptine with IC50 of 0.24, 0.12 and 0.155 uM for HDAC1, 2 and 3 respectively, does not inhibit HDAC6
    GY06744 Tianeptinostat Tianeptinostat is a class I HDAC inhibitor with IC50 of 28, 33 and 51 nM for HDAC1, 2 and 3, respectively, also inhibits HDAC6 (IC50=1.6 nM) but not HDAC5 (IC50>80 uM)
    GY06745 HDAC6 degrader 9c HDAC6 degrader 9c (dHDAC6 9c) is a bifunctional molecule (dHDAC6) that could selectively degrade HDAC6, by conjugating non-selective HDAC inhibitor to a thalidomide-type E3 ligase ligand
    GY06746 HAMI3379 HAMI3379 (HAMI-3379) is a potent and selective antagonist of cysteinyl leukotriene 2 (CysLT(2)) receptor, inhibits LTD4- and LTC4-induced intracellular calcium mobilization withIC50 of 3.8 nM and 4.4 nM respectively
    GY06747 MPT0G211 MPT0G211 is a novel potent, selective HDAC6 inhibitor with IC50 of 0.291 nM, displays >1,000-fold selectivity over other HDAC isoforms
    GY06748 UCT943 UCT943 (UCT-943) is a potent, selective, next generation Plasmodium falciparum PI4K inhibitor with IC50 of 23 nM
    GY06749 BU09059 BU09059 is a potent, selective, short-acting kappa-opioid receptor antagonist with Ki of 1.72 nM, displays 15- and 616-fold selectivity over μ- and δ-receptors respectively
    GY06750 RasGRP3 ligand 96 RasGRP3 ligand 96 is a potent, selective ligand of Ras guanine-releasing protein 3 (RasGRP3) with Ki of 1.75 nM, showed 73-fold and 45-fold selectivity relative to PKCα and PKCε for in vitro binding activity resepctively
    GY06752 MPT0E028 MPT0E028 is a potent HDAC inhibitor that inhibits nuclear HDAC activity with IC50 of 11.1 nM in HeLa cells, 9-30 times more potent than SAHA
    GY06753 sPLA2-X inhibitor 31 sPLA2-X inhibitor 31 is a potent, selective secreted phospholipase A2 type X (sPLA2-X) with IC50 of 26 nM, displays 12-fold and 80-fold selectivity over sPLA2-Iia and sPLA2-V, respectively
    GY06754 MB725 MB725 is a small-molecule p53 mutant Y220C stabilizer, induces selective viability reduction in several p53-Y220C cancer cell lines (Huh7 cell IC50=10 uM)
    GY06755 MB710 MB710 is a small-molecule p53 mutant Y220C stabilizer, binds tightly to the Y220C pocket and stabilizes p53-Y220C in vitro.
    GY06756 STING inhibitor C-178 STING inhibitor C-178 is a covalent, small-molecule inhibitor of STING, blocks palmitoylation (PMA)-induced clustering of STING
    GY06757 STING inhibitor C-176 STING inhibitor C-176 (C-176) is a covalent, in vivo-active, small-molecule inhibitor of STING, attenuates STING-associated autoinflammatory disease in mice.
    GY06758 STING inhibitor H-151 STING inhibitor H-151 (H-151) is a highly potent, selective, covalent small-molecule antagonist of STING that has noteworthy inhibitory activity both in human cells and in vivo.
    GY06759 S-C025 S-C025 is a highly potent antagonist of oxoeicosanoid receptor (OXE receptor) with IC50 of 0.12 nM
    GY06760 S-230 S-C025 is a highly potent antagonist of oxoeicosanoid receptor (OXE receptor) with IC50 of 0.12 nM, inhibits 5-oxo-ETE-induced calcium mobilization in human neutrophils.
    GY06761 TLR7 and 8 modulator 31 TLR7 and 8 modulator 31 is a potent, orally active, dual TLR7 and 8 agonist with LEC values of 0.15 and 0.16 uM, respectively
    GY06762 SW063058 SW063058 is a small molecule that selectively disrupt Beclin 1/Bcl-2 binding as compared to Bax/Bcl-2 and Bim/Bcl-2 binding and induces autophagic flux at concentrations with minimal cytotoxicity.
    GY06763 SW076956 SW076956 is a small molecule that selectively disrupt Beclin 1/Bcl-2 binding as compared to Bax/Bcl-2 and Bim/Bcl-2 binding and induces autophagic flux at concentrations with minimal cytotoxicity.
    GY06766 JMS-17-2 JMS-17-2 is a potent and selective antagonist of CX3CR1 with IC50 of 0.32 nM, displays significant selectivity for CX3CR1 over other chemokine receptors such CXCR2, CXCR1, and CXCR4 (IC50>1 uM)
    GY06767 Flavokawain B Flavokawain B is a natural chalcone that can induce apoptosis in androgen receptor-negative, hormone-refractory prostate cancer cell lines (IC50=3-50 uM), via up-regulation of death-receptor 5 and Bim expression
    GY06769 CCG-222740 CCG-222740 (CCG222740) is a pharmacological inhibitor of MRTF/SRF signalling, shows greater inhibitory effect on MRTF/SRF target genes than MRTF-A inhibitor CCG-203971, with IC50 of 5 uM in fibroblast-mediated collagen contraction assay
    GY06770 EC-359 EC-359 (EC359) is a first-in-class, orally available inhibitor of leukemia inhibitory factor (LIF), blocks LIF-LIFR interaction and binds to LIFR with affinity of 81 nM in SPR assay
    GY06771 CPSI-1306 CPSI-1306 (CPSI1306) is an orally available small-molecule MIF antagonist, protects against UVB-induced squamous cell carcinoma, reduces the severity of animal model of multiple sclerosis.
    GY06772 SGN-2FF SGN-2FF is an orally bioavailable small molecule inhibitor of glycoprotein fucosylation, demonstrates encouraging preclinical antitumor activity in mouse models
    GY06773 LTX-401 LTX-401 (LTX401) is an oncolytic amino acid derivative with potential immunogenic properties, selectively destroys the structure of the Golgi apparatus
    GY06774 LTX-401 dihydrochloride LTX-401 dihydrochloride (LTX401) is an oncolytic amino acid derivative with potential immunogenic properties, selectively destroys the structure of the Golgi apparatus
    GY06775 Tucidinostat Tucidinostat (Chidamide, HBI-8000, CS055) is a novel histone deacetylase (HDAC) inhibitor with IC50 of 95/160/67/733/78/432 nM for HDAC1/2/3/8/10/11, respectively
    GY06776 Azosemide Azosemide (Azosemidum) is a potent Na-K-Cl Cotransporter NKCC1 with IC50 of 0.246 and 0.197 uM for hNKCC1A and NKCC1B, being about 4-times more potent than bumetanide
    GY06777 DDR inhibitor X DDR inhibitor X is a potent discoidin domain receptor (DDR) inhibitor with IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
    GY06779 JH-VIII-157-02 JH-VIII-157-02 is a potent, orally active, CNS-permeable, second-generation inhibitor of ALK G1202R mutant with IC50 of 2 nM, also shows high potency against a variety of other frequently observed mutants (G1269A, S1206Y, F1174L and C1156Y)
    GY06780 RO1138452 RO1138452 is a potent, selective antagonist of prostacyclin receptor (IP receptor), inhibits carbaprostacylin-stimulated c-AMP accumulation in human SH-SY5Y neuroblastoma cells with pKb of 8.8
    GY06781 YW3-56 YW3-56 is a potent peptidylarginine deiminase (PAD) inhibitor with inhibitory activity against PAD2 (IC50=0.5-1 uM) and PAD4 (IC50=1-2 uM), inhibits U2OS cancer cell growth with IC50 of 2.5 uM
    GY06783 Foretinib-Based PROTAC 7 Foretinib-Based PROTAC 7 is a VHL-recruiting PROTAC that induces the degradation of c-Met in a dose- and time-dependent fashion in MDA-MB-231 cells.
    GY06784 Gefitinib-based PROTAC 3 Gefitinib-based PROTAC 3 is a VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R).
    GY06786 AGN192836 AGN192836 (AGN 192836) is a potent, selective α2 adrenergic (alpha 2-adrenoceptor) agonist with EC50 of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively
    GY06787 BAY-320 BAY-320 (BAY320) is a potent, selective, ATP-competitive inhibitor of Bub1 kinase with IC50 of 680 nM
    GY06788 BAY-524 BAY-524 (BAY524) is a potent, selective, ATP-competitive inhibitor of Bub1 kinase with IC50 of 450 nM
    GY06790 GLX351322 GLX351322 (GLX-351322) is a novel potent inhibitor of NADPH oxidase 4 (Nox4), inhibits hydrogen peroxide production from tetracycline inducible NOX4-overexpressing cells with IC50 of 5 uM
    GY06791 H3B-5942 H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo
    GY06792 Lipofermata Lipofermata (CB16.2 aka) is a specific fatty acid transport (FATP) inhibitor, blocks human FATP2-mediated fatty acid uptake (IC50=4.84 uM in Caco-2 cells) without impacting other cellular functions
    GY06793 Tesirine Tesirine ( SG3249) is a cathepsin B-cleavable valine-alanine pyrrolobenzodiazepine (PBD) dimer as antibody-drug conjugate (ADC) payload
    GY06794 LY500307 LY500307 (LY-500307, Erteberel, SERBA-1) is a potent, selective Estrogen Receptor β (ERβ) agonist with Ki/EC50 of 0.19/0.66 nM, 12-fold higher affinity than ERα and exhibits 32-fold more functional potency
    GY06796 ZLDI-8 ZLDI-8 (IAC-8) is a novel Notch signaling pathway inhibitor for Notch activating/cleaving enzyme ADAM-17, significantly decreases the level of NICD and accumulation of NICD in the nucleus
    GY06797 EGFR-HER2 Ex20Ins inhibitor 1a EGFR-HER2 Ex20Ins inhibitor 1a is a highly potent, broadly effective EGFR and HER2 Exon 20 insertion mutant inhibitor with biochemical IC50 of <0.5 nM (wtEGFR, 100 uM ATP)
    GY06799 SOD1-Derlin-1 inhibitor 56-59 SOD1-Derlin-1 inhibitor 56-59 is a cell-permeable, small molecule inhibitor of SOD1-Derlin-1 interaction, target SOD1 DBR and clearly attenuates the interactions of Derlin-1 with 122 types of SOD1mut in the cell-based co-immunoprecipitation assay
    GY06800 KY-226 KY-226 (KY226) is a potent, allosteric, orally active inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 uM (human PTP1B), does not exhibit PPARγ agonist activity
    GY06801 OUL35 OUL35 (NSC39047) is a potent and selective inhibitor of mono-ADP-ribosyltransferase PARP10/ARTD10 with IC50 of 330 nM, displays remarkable selectivity towards ARTD10 over other enzymes in the human protein family
    GY06802 Tecovirimat Tecovirimat (ST-246) is a potent, orally bioavailable, first-in-class inhibitor of orthopoxvirus egress with EC50 of 0.01-0.6 uM against a panel of Orthopoxviruses
    GY06803 EMD-281014 EMD-281014 is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels
    GY06804 EMD-281014 hydrochloride EMD-281014 hydrochloride is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels
    GY06805 FTBMT FTBMT is a novel selective GPR52 agonist of GPR52, increases intracellular cAMP levels in CHO cells expressing human, mouse, or rat GPR52, with pEC50 of 7.03, 6.85, and 6.87M, respectively
    GY06806 IK1 inhibitor PA-6 IK1 inhibitor PA-6 is an efficient, specific inhibitor of inward rectifier current (IK1), blocks KIR2.x currents of human and mouse with IC50 of 12-15 nM
    GY06808 JG-231 JG-231 is an allosteric inhibitor that disrupts the Hsp70-BAG3 interaction (Ki=0.11 uM), inhibits breast cancer cells MCF-7 and MDA-MB-231 with IC50 of 0.12 and 0.25 uM, respectively
    GY06809 SOS1 activator 17 SOS1 activator 17 is a small molecule activator of guanine nucleotide exchange factor SOS1 with EC50 of 0.8 uM, modulates RAS signaling in vitro
    GY06810 GlyT1 inhibitor 46 GlyT1 inhibitor 46 is a novel potent, selective, orally available inhibitor of glycine transporter-1 (GlyT1) with IC50 of 38 and 21 nM for rat and human GlyT1, respectively
    GY06811 TCASK10 TCASK10 is a potent, highly specific inhibitor of ASK1 with IC50 of 14 nM, 30-fold selectivity over ASK2 (IC50=510 nM) and no activity against MEKK1, TAK1, IKKβ, ERK1, JNK1, p38α, GSK-3β, PKCθ and B-raf
    GY06812 QCA570 QCA570 is a novel, highly potent efficacious BET degrader (PROTAC)
    GY06813 QCA276 QCA276 is a novel potent BET proteins inhibitor with IC50/Ki of 10/.3 nM, QCA276 is the BET ligand for PROTAC QCA570
    GY06814 BET inhibitor CF53 BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1)
    GY06816 Omidenepag Isopropyl Omidenepag Isopropyl (OMDI) is the prodrug of Omidenepag, which is a potent, selective agonist human EP2 receptor
    GY06817 SR2211 SR2211 (SR-2211) is a potent, selective RORγ inverse agonist (Ki=105 nM, IC50=320 nM) that potently inhibits production of IL-17 in cells
    GY06818 MRL-871 MRL-871 (MRL871) is a potent, selective inhibitor of RORγt via allosteric inverse agonism, inhibits coactivator binding with IC50 of 7 nM
    GY06819 ASS234 ASS234 (ASS-234) is a multitarget, potent, and CNS permeable inhibitor with IC50 of 5.2, 43, 350 and 460 nM for MAO-1, MAO-B, EeAChE and eqBuChE, respectively.
    GY06820 IGS-1.76 IGS-1.76 is a small molecule inhibitor of human NCS-1/Ric8a interaction with affinity of 1.25 uM (hNCS-1)
    GY06822 RORγt inverse agonist 22 RORγt inverse agonist 22 is a potent, subtype selective RORγt inverse agonist with binding IC50 of 18 nM, displays >192-fold selectivity over RORα and RORβ
    GY06823 Desmethyl dabrafenib Desmethyl dabrafenib (GSK2167542, Dabrafenib metabolite M8) is the desmethyl- metabolic byproduct of Dabrafenib, ameliorates developmental pathologies of Kabuki Syndrome in vivo.
    GY06824 ClpP inhibitor M21 ClpP inhibitor M21 is a noncompetitive inhibitor of ClpP with IC50 of 41.42 uM, inhibits ClpP cleavage of SUc-LY-AMC substrate in a peptidase assay
    GY06825 MALT1 paracaspase inhibitor 3 MALT1 paracaspase inhibitor 3 is a potent, specific, covalent inhibitor of MALT1 paracaspase with Ki of 10 nM, exhibits 10-and 100-fold improved potency in vitro and in vivo compared with Z-VRPR-fmk
    GY06826 SINCRO SINCRO is a novel anti-cancer compound that can activate the cytosolic DNA-sensing STING signaling pathway leading to the induction of type I interferon (IFN) genes
    GY06827 UniPR1331 UniPR1331 (UniPR-1331) is a selective, orally available antagonist of Eph/ephrin interaction with pIC50 of 5.45, IC50 of 2.9 uM
    GY06830 Cenupatide Cenupatide is an urokinase plasminogen activator receptor (uPAR) inhibitor for treating disorders associated altered cell migration, such as cancer.
    GY06832 Coblopasvir Coblopasvir (KW136, KW-136) is a novel HCV NS5A inhibitor under development for treatment of HCV infection.
    GY06833 Dersimelagon Dersimelagon is a melanocortin receptor agonist.
    GY06835 Exicorilant Exicorilant (CORT125281, CORT-125281) is a potent, selective glucocorticoid receptor (GR) antagonist, exhibits no cross-reactivity for the PR and AR receptors.
    GY06838 GR3027 GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC
    GY06840 Neluxicapone Neluxicapone is a potent, selective inhibitor of catechol-O-methyltransferase (COMT).
    GY06841 Soticlestat Soticlestat is a potent, selective cholesterol 24-hydroxylase inhibitor.
    GY06842 Taniborbactam Taniborbactam is a novel beta-lactamase inhibitor for the treatment of bacterial infections.
    GY06843 Tildacerfont Tildacerfont is a novel corticotropin releasing factor (CRF) CRF1 receptor antagonist.
    GY06845 TRPM8 antagonist 14 TRPM8 antagonist 14 is a potent, selective TRPM8 antagonist with IC50 of 0.2 nM in calcium influx assays, shows no activity on TRPV1.
    GY06846 PF-06764427 PF-06764427 (PF06764427) is a potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 55 nM, has no measurable agonist or PAM activity at the M2-M5 receptors at 10 uM.
    GY06847 VU0453595 VU0453595 (VU453595) is a potent, selective M1 positive allosteric modulator (PAM) with EC50 of 3.2 uM (rM1).
    GY06848 PF-06827443 PF-06827443 (PF06827443) is a potent, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with EC50 of 47 nM, shows no activity against M2-M5 at 10 uM.
    GY06849 KRM-II-81 KRM-II-81 is a potent, selective α1/α2/α3 GABAA receptors positive allosteric modulator with EC50 of 937 nM for α1β3γ2, negligible efficacy at α4/α5/α6 GABAA receptors.
    GY06850 HZ-166 HZ-166 (HZ166) is a GABAA receptor subtype-selective benzodiazepine site ligand with preferential activity at α2- and α3-GABA(A) receptors.
    GY06851 GAT-211 GAT-211 (GAT211) is a selective cannabinoid 1 receptor (CB1R) positive allosteric modulator with pKb of 7.26, Arrestin2 EC50 of 775 nM.
    GY06852 VU6004256 VU6004256 (VU 6004256) is a highly potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 155 nM (mouse M1), significant selectivity over M2-M5 (EC50>30 uM).
    GY06853 VU0418506 VU0418506 (VU 0418506) is a potent and selective mGlu4 positive allosteric modulator (PAM) with EC50 of 68 nM (hmGlu4).
    GY06854 GAT-100 GAT-100 (GAT100) is a potent, selective CB1R negative allosteric modulator (NAM) with cAMP EC50 and β-arr EC50 of 174 nM and 2.1 nM, does not exhibit inverse agonism.
    GY06855 VU0467154 VU0467154 (VU 0467154) is a potent, selective M4 mAChR positive allosteric modulator with EC50 of 17.7 nM.
    GY06856 D-520 D-520 is a potent, multifunctional D2/D3 agonist with Ki of 41.8 /0.35 nM, modulates aggregation of alpha-synuclein (αSN) and reduces toxicity of preformed aggregates of αSN.
    GY06857 HS94 HS94 (DAPK3 inhibitor HS94) is a selective DAPK3 inhibitor with Ki of 126 nM, >20-fold selectivity over Pim kinases.
    GY06858 HS148 HS148 (DAPK3 inhibitor HS148) is a selective DAPK3 inhibitor with Ki of 119 nM, >10-fold selectivity over Pim kinases.
    GY06859 Wnt-p53 inhibitor compound 2 Wnt-p53 inhibitor compound 2 is a novel inhibitor targets both Wnt signaling and ATM/p53, potently inhibits Wnt transcription (IC50=11 nM) and p53 transcription (EC50=1.9 nM).
    GY06860 CFM-4.16 CFM-4.16 is a CARP-1 functional mimetic (CFM) compound bind with CARP-1, stimulates CARP-1 expression and apoptosis.
    GY06862 RCM-1 RCM-1 (FOXM1 inhibitor RCM-1) is a nontoxic, small molecule that inhibits FOXM1 activity in vitro and in vivo, inhibits GFP-FOXM1 in U2OS cells with EC50 of 0.72 uM.
    GY06863 JAK2 inhibitor G5-7 JAK2 inhibitor G5-7 is a small molecule, allosteric JAK2 inhibitor that selectively inhibits JAK2-mediated phosphorylation and activation of EGFR and STAT3 by binding to JAK2.
    GY06865 GPR40 AgoPAM AP5 GPR40 AgoPAM AP5 is a potent, selective GPR40 AgoPAM (full agonist with positive allosteric modulation) with hIP1 EC50 of 0.8 nM, high selectivity over the GPR120 receptor (EC50>30 uM).
    GY06866 NBI-59159 NBI-59159 (NBI59159) is a potent EAAT3-preferring inhibitor.
    GY06867 WAY-213613 WAY-213613 is a selective GLT-1/EAAT2 inhibitor.
    GY06868 PF-06885249 PF-06885249 (PF06885249) is a potent, direct AMPK activator with EC50 of 7.0 and 27 nM for α1β1γ1 and α2β1γ1, respectively.
    GY06869 AZ084 AZ084 (AZ-084) is a potent, selective, allosteric, orally available CCR8 antagonist with Ki of 0.9 nM.
    GY06872 Roxyl-WL Roxyl-WL is a highly potent and selective inhibitor of IDO1 with IC50 of 1 nM.
    GY06873 Qstatin Qstatin is a potent SmcR inhibitor in V. vulnificus. with IC50 of 208.9 nM, shows pan-QS (quorum sensing) inhibitor activity in diverse Vibrio species.
    GY06874 RB-005 RB-005 (RB-005) is a potent, selective inhibitor of sphingosine kinase SphK1 (SK1) with IC50 of 3.6 uM, displays 15-fold selectivity over SphK2.
    GY06875 MID-1 MID-1 (ChemBridge5655896) is a specific small molecule MG53-IRS-1 interaction disruptor (MID), but not MG53-FAK and-Cav-3 interaction.
    GY06876 AST-3424 AST-3424 (OBI-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent.
    GY06877 MLS6585 MLS6585 is a novel positive allosteric modulator of the D1 dopamine receptor, potentiatse dopamine-stimulated G-protein- and β-arrestin-mediated signaling and increase the affinity of dopamine for the D1 receptor with low micromolar potencies.
    GY06878 HX600 HX600 (HX-600) is a synthetic agonist of RXR-Nurr1 heterodimer complex, also selectively activate NGFI-B/RXR heterodimers.
    GY06879 VCE-004.3 VCE-004.3 (VCE004.3) is a novel semi-synthetic cannabidiol derivative behaving as a dual PPARγ/CB2 agonist and CB1 receptor modulator, binds and activates PPARγ (IC50=3.5 uM) and CB2 receptors (pKi=6.69) and antagonizes CB1 receptor (pKi=5.61).
    GY06880 AF64394 AF64394 is a potent, selective GPR3 inverse agonist with pIC50 of 7.3, displays >100-fold selectivity over GPR6 and GPR12.
    GY06881 NFEPP NFEPP is a novel potent, selective pH-dependent μ-opioid receptor (MOR) agonist with a low pKa, shows significantly lower affinity compared with fentanyl at pH 7.4.
    GY06882 ASP7657 ASP7657 is a novel, potent, and selective prostaglandin EP4 receptor antagonist and exhibits high affinity for rat and human EP4 receptors with Ki of 6.02 nM and 2.21 nM, respectively.
    GY06884 S44819 S44819 (S 44819, Egis-13529) is a novel potent, competitive, selective antagonist of the α5-GABAAR with Kd of 221 nM, IC50 of 585 nM (α5β2γ2).
    GY06885 STING CDN agonist IFM Therapeutics STING CDN agonist IFM Therapeutics is a synthetic cyclic dinucleotide (CDN) agonist of STING, stimulates potent immunity against cancer.
    GY06886 Amgen 16 Amgen16 is a highly potent inhibitor of NF-κB inducing Kinase (NIK), example 294 in patent WO 2009158011 A1.
    GY06888 AM-0216 AM-0216 (Amgen16) is a highly potent inhibitor of NF-κB inducing Kinase (NIK) with Ki of 2 nM, selectively decrease viability of MMCLs in which NFkB activity is NIK-dependent.
    GY06889 ABX-1431 hydrochloride ABX-1431 (ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL).
    GY06890 GSK4027 GSK4027 (GSK 4027, GSK-4027) is a potent, selective, cell-penetrant chemical probe of PCAF/GCN5 bromodomain with pKi of 8.9 for both.
    GY06891 PF-4778574 PF-4778574 (PF4778574) is a brain penetrant, positive allosteric modulator (potentiator) of AMPA receptor with Ki of 85 nM, increases S-AMPA-evoked responses in rat primary cortical neurons with EC50 of 45-919 nM.
    GY06892 GNE-6468 GNE-6468 (GNE6468) is a potent and selective RORc inverse agonist (EC50=2 nM) with >1,000-fold selectivity for RORc over PPARγ.
    GY06893 APX2009 APX2009 (APX-2009) is a novel potent inhibitor of reduction-oxidation factor 1-apurinic/apyrimidinic endonuclease 1 (Ref-1/APE1) with IC50 of 0.45 uM for redox EMSA inhibition.
    GY06894 APX2014 APX2014 (APX-2014) is a novel potent inhibitor of reduction-oxidation factor 1-apurinic/apyrimidinic endonuclease 1 (Ref-1/APE1) with IC50 of 0.2 uM for redox EMSA inhibition.
    GY06895 AP14145 AP14145 (AP-14145) is a potent, selective negative allosteric modulator of KCa2.2 and KCa2.3 with equal potency (IC50=1.1±0.3 uM).
    GY06896 UoS12258 UoS12258 (UoS-12258) is a selective, positive allosteric modulator of the AMPA receptor with pEC50 of 5.6.
    GY06898 CZh226 CZh226 hydrochloride (CZh-226) is a potent, selective inhibitor of p21-activated kinase 4 (PAK4) with Ki of 9 nM, displays 346-fold selectivity over PAK-1.
    GY06899 NGI-1 derivative C-19 NGI-1 derivative C-19 is a specific, small-molecule inhibitor of oligosaccharyltransferase (OST) catalytic subunit STT3B, without effect on STT3A.
    GY06901 INU-101 INU-101 (INU101) is a highly potent, selective, orally acitve 11β-HSD1 inhibitor with IC50 of 26.2 nM, 37 nM and 0.6 nM for mice, rats, and human 11β-HSD1, respectively.
    GY06902 HSD-016 HSD-016 (HSD016) is a potent, selective, and efficacious 11β-HSD1 inhibitor with IC50 of 149 and 530 nM for mouse and human 11β-HSD1, respectively.
    GY06903 INCB13739 INCB13739 (INCB-13739) is a potent, selective, oral 11βHSD1 inhibitor (IC50=1.1 nM) with high seelctivity over other dehydrogenases, glucocorticoid and mineralocorticoid receptors.
    GY06904 TAK-071 TAK-071 (TAK071) is a novel potent, selective, low cooperativity (α-value) positive allosteric modulator of muscarinic M1 receptor with inflection point of 2.7 nM in Ca2+ flux assays in CHO-K1 cells.
    GY06906 MFN2 agonist B-A l MFN2 agonist B-A/l is a mall-molecule mimics of the peptide-peptide interface of MFN2, allosterically activates MFN2 and promotes mitochondrial fusion with EC50 of 3 nM.
    GY06907 NP161 NP161 is a potent and selective inhibitor of extracellular TRX (Thioredoxin 1) in vitro with IC50 of 0.54 uM.
    GY06908 MAI-150 MAI-150 is a peptidomimetic inhibitor of APC-Asef interaction, blocks colorectal cancer migration.
    GY06909 BAY-8002 BAY-8002 is a novel potent, selective, orally available monocarboxylate transporter 1 (MCT1) inhibitor (Kd=7.9 nM), inhibits cellular lactate uptake in DLD-1 cells with IC50 of 8 nM.
    GY06911 PF-06747711 PF-06747711 (PF06747711) is a potent, selective, orally bioavailable RORC2 (RORγt) inverse agonist with IC50 of 4.1 nM.
    GY06912 VERU-111 VERU-111 is a novel, oral α and β tubulin inhibitor that would be a therapeutic option for hormone sensitive and castrate resistant advanced prostate cancer.
    GY06913 T1551 T1551 is a novel selective PRMT5 inhibitor with IC50 of 34.1 uM, decreases cell viability of A549 cell with IC50 of 5.8 uM (72h).
    GY06914 LIT-927 LIT-927 (LIT927) is the first selective, locally and orally active CXCL12 neutraligand with Ki of 267 nM for CXCL12-TR binding inhibition.
    GY06915 JNJ-55511118 JNJ-55511118 (JNJ55511118) is a selective, orally available AMPA receptor containing TARP-γ8 negative modulator with Ki of 26 nM, displays no significant activity against other TARP-less AMPARs and AMPARs coexpressed with other TARPs or CNIH2.
    GY06917 KB-141 KB-141 (KB141) is a potent, selective thyroid hormone receptor TRβ agonist (IC50=1.1 nM), binds to hTRβ with a 14-fold higher affinity than to hTRα.
    GY06918 PHY34 PHY34 is a potent autophagy inhibitor with cytotoxic effects by inhibiting autophagy at a late stage (MDA-MB-435 IC50=23 nM, MDA-MB-231 IC50=5.2 nM).
    GY06920 UAB30 UAB30 (9cUAB30) is a novel synthetic rexinoid that binds selectively to the retinoid X receptor (RXR) leading to activation of genes involved in induction of differentiation and apoptosis.
    GY06922 Nelonicline Nelonicline (ABT-126) is a potent, selective α7 nicotinic receptor (nAChR) partial agonist for the treatment of cognitive impairment with schizophrenia.
    GY06923 XL-001 XL-001 (XL001) is a novel specific CB2 inverse agonist with Ki of 0.5 nM.
    GY06925 Casein Kinase inhibitor A86 Casein Kinase inhibitor A86 (CKIα inhibitor A86) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=1-10 nM, CKIα Kd=9.8 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19.
    GY06926 BTX161 BTX161 is a thalidomide analog that mediates degradation of CKIα better than lenalidomide in human AML cells and activates DDR and p53, while stabilizing the p53 antagonist MDM2.
    GY06927 Amt-87 Amt-87 is a HIV latency-reversal agent that reactivates latent HIV at the transcriptional level, promotes phosphorylation of CDK9 T-loop at Thr186.
    GY06928 iCDK9 iCDK9 (i-CDK9) is a potent, highly selective CDK9 inhibitor (IC50<0.4 nM, CDK9-CycT1 kinase), exhibits >600-fold selectivity toward CDK1-CycB, CDK2-CycA, CDK4-CycD1, CDK7-CycH-MAT1 and CDK8-CycC.
    GY06929 IITZ-01 IITZ-01 (Autophagy inhibitor IITZ-01) is a novel potent lysosomotropic autophagy inhibitor, exhibits >10-fold potent autophagy inhibition along with 12- to 20-fold better cytotoxic action than Chloroquine.
    GY07295 TP0438836 TP0438836 is a potent, low-absorbable sodium-dependent SGLT1 inhibitor with IC50 of 28 nM, and also inhibits SGLT2 with IC50 of 7 nM.
    GY07299 GNE-8505 GNE-8505 is a dual leucine zipper kinase inhibitor with Ki of 4 nM.
    GY07355 EML-405 EML-405 (EML405) is a small-molecule inhibitor of Spindlin1 (SPIN1) with Kd of 14 uM.
    GY07361 NVS-ZP7-4 NVS-ZP7-4 is the first reported chemical tool to probe the impact of modulating ER zinc levels.
    GY07363 Compound 69 Compound 69 (PFKFB3 inhibitor) is a potent PFKFB3 inhibitor with IC50 of 14 nM and shows inhibition in HCT116 cells with IC50 of 0.49 μM.
    GY07372 MIDD0301 MIDD0301 is an allosteric GABAAR agonist with binding affinity of 72 nM.
    GY07375 (S)-DO271 (S)-DO271 is an inactive control of DO264.
    GY07377 EML741 EML741 is a novel chemotype of histone lysine methyltransferase EHMT1/2 (GLP/G9a) inhibitor with IC50 23 nM.
    GY07381 JNJ-64326067 JNJ-64326067 is a potent and selective binder to aggregated tau and would be a new promising tau positron emission tomography (PET) imaging tracer.
    GY07383 JNJ4796 JNJ4796 is an orally active inhibitor of influenza A HA and neutralizes influenza A group 1 viruses by inhibiting hemagglutinin-mediated fusion.
    GY07384 NLX-204 NLX-204 is a novel high selective 5-HT1A receptor-biased agonist with pKi of 10.19.
    GY07385 NV-5138 NV-5138 is the first selective Brain mTORC1 activator and binds to Sestrin2 with Kd of 1.5 µM.
    GY07386 GSK8612 GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0.
    GY07387 VU6019278 VU6019278 is a potent mGlu7 NAM inhibitor with IC50 of 501 nM and shows favorable plasma protein binding, low predicted hepatic clearance and high CNS penetration.
    GY07388 NPD2381 NPD2381 is a novel and selective cancer-stemness inhibitor that targets mitochondrial metabolism.
    GY07389 DS21360717 DS21360717 is a FER tyrosine kinase inhibitor with IC50 of 0.49 nM.
    GY07390 RK-287107 RK-287107 is a potent TNKS/TNKS2 inhibitor with IC50 of 14.3 nM/10.6 nM and shows >7,000-fold selectivity against the PARP1.
    GY07391 YKL-5-124 YKL-5-124 is a potent, selective and covalent CDK7 inhibitor with IC50 of 9.7 nM, which shows no inhibition to CDK12/CDK13.
    GY01980 ML390 ML390 exerts its potent differentiation effect on multiple leukemia models.
    GY02042 CDK2 CDK2 is a member of the eukaryotic S/T protein kinase family and its function is to catalyze the phosphoryl transfer of ATP γ-phosphate to serine or threonine hydroxyl (denoted as S0/T0) in a protein substrate.