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    CDK

    CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. In fact, yeast cells can proliferate normally when their CDK gene has been replaced with the homologous human gene. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase.There are around 20 Cyclin-dependent kinases (CDK1-20) known till date. CDK1, 4 and 5 are involved in cell cycle, and CDK 7, 8, 9 and 11 are associated with transcription.CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKs of S. pombe (Cdc2), S. cerevisia (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs).

    Products

    Catalog No. Name Description
    GY04207 New Bohemine Bohemine is a synthetic, cell-permeable, cyclin-dependent kinase inhibitor
    GY01444 Special AZD5438 AZD-5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It also inhibits GSK3β, but is less potent to CDK5/6.
    GY02689 Special THZ1 THZ1 is a selective and potent covalent CDK7 inhibitor with IC50 of 3.2 nM.
    GY01080 Special LY2835219 (Abemaciclib) mesylate LY2835219 a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
    GY01010 Special Palbociclib (PD 0332991) HCl Palbociclib hydrochloride is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases.
    GY01037 Special LEE011 LEE011 is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
    GY01058 Special Palbociclib isethionate Palbociclib (isethionate) is a highly selective inhibitor of CDK4/6 with IC50s of 11 nM/16 nM, and shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. 
    GY01163 Special SNS-032 SNS-032 is a selective inhibitor of cyclin-dependent kinase (CDK), inhibiting CDK2/7/9 with IC50s of 38 nM/62 nM/4 nM.
    GY01221 Special Ro-3306 Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
    GY01237 Special AT7519 AT7519 as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
    GY01340 Special PHA-793887 PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
    GY01368 Special K03861 K03861 is a type II CDK2 inhibitor with Kd of 8.2 nM.
    GY01721 Special ON123300 ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8.
    GY01775 Special Kenpaullone (NSC-664704) Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively.
    GY02276 Special LY2835219 (Abemaciclib) LY2835219 free base is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
    GY02490 Special BS-181 HCl BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
    GY03541 Special RGB-286638 free base RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
    GY03734 Special SB1317 SB1317 is a potent inhibitor of CDK2, JAK2, and FLT3 for the treatment of cancer, with IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.
    GY03935 THZ1 HCl THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with IC50 of 3.2 nM.
    GY01071 Roscovitine (Seliciclib, CYC202) Roscovitine is a potent and selective CDK inhibitor with IC50 of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
    GY01082 Flavopiridol (Alvocidib) Flavopiridol is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
    GY01261 PHA-767491 PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
    GY01280 Flavopiridol HCl Flavopiridol Hydrochloride is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
    GY01282 PHA-848125 PHA-848125 is a potent, dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
    GY01365 LDC000067 LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.
    GY01440 R547 R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM.
    GY01497 XL413 HCl XL413 hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.
    GY01530 BMS-265246 BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively.
    GY01697 Purvalanol A Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
    GY01729 SU9516 SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC50s of 40, 200 nM, respectively.
    GY01844 AMG 925 AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 2.4 nM and 1.5 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell, extracted form Patent WO 2012129344 A1, example 5.
    GY01892 ML167 ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1, Clk2, Clk3 and Dyrk1A/1B.
    GY02022 NU6300 NU6300 is a non-covalent ATP-competitive CDK2 inhibitor (IC50 = 0.16 mM).
    GY02122 CYC065 CYC065 is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK 9 kinases.
    GY02139 BS-181 BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
    GY02194 XL413 XL413 is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.
    GY02246 LEE011 HCl LEE011 hydrochloride is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
    GY02329 NVP-2 NVP-2 is a CDK9 inhibitor with an IC50 of 0.5 nM.
    GY02338 CDK-IN-2 CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4.
    GY02420 KH-CB19 KH-CB19 is a potent and highly specific inhibitor of the CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4).
    GY02442 Senexin A Senexin A is a CDK8 inhibitor with an IC50 of 280 nM.
    GY02453 LEE011 succinate LEE011 succinate is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
    GY02454 Ribociclib (LEE011) succinate hydrate LEE011 succinate hydrate is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
    GY02514 BAY-1143572 BAY 1143572 is a highly selective, potent and orally available inhibitor of PTEFb/CDK9; inhibits the proliferation of AML cell lines with a median IC50 of 385 nM.
    GY02536 CDKI-73 CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).
    GY02558 AT7519 trifluoroacetate AT7519 trifluoroacetate as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
    GY02596 Senexin B Senexin B is a potent and selective CDK8/19 inhibitor.
    GY02690 THZ2 THZ2 is a potent and selective CDK7 inhibitor with IC50 of 13.9 nM.
    GY02691 CCT-251921 CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.
    GY02697 (+)-BAY-1251152 (+)-BAY-1251152 is a CDK9 inhibitor extracted from patent WO 2014076091 A1, example 1.
    GY02699 NU2058 NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1.
    GY02710 CC-671 CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively.
    GY02711 LY2857785 LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
    GY02714 THZ1-R THZ1-R is an inhibitor of CDK7, with an IC50 of 146 nM.
    GY02723 LY3177833 LY3177833 is an CDC7 and pMCM2 inhibitor extracted from patent US 20140275131and patent WO 2014143601 A1 compound example 4; has IC50 values of 3.3 nM and 290 nM, respectively.
    GY02790 THZ531 THZ531 is a covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.
    GY02897 MSC2530818 MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC50 of 2.6 nM for CDK8.
    GY02960 Trilaciclib HCl Trilaciclib hydrochloride is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.
    GY03032 NG 52 NG 52 (Compound 52 ) is a potent, cell-permeable, reversible, selective, and ATP-compatible inhibitor of the cell cycle-regulating kinase, Cdc28p (IC50 = 7 μM), and the related Pho85p kinase (IC50 = 2 μM).
    GY03033 Purvalanol B Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively.
    GY03431 Wogonin Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
    GY03540 RGB-286638 RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
    GY03742 PHA-767491 HCl PHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
    GY03774 AZD2098 AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor, used for asthma research.
    GY04699 Voruciclib Voruciclib is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with potential antineoplastic activity.
    GY05627 AZD5576 AZD5576(AZD 5576) is a potent, highly selective, and orally bioavailable inhibitor of CDK9 with IC50 of < 5 nM, decreases phosphorylation of Ser2-RNAPII in cells with an IC50 of 96 nM.
    GY06243 NU-6102 A potent CDK1 and CDK2 inhibitor with IC50 of 9.5 nM and 5.4 nM against CDK1/cyclinB and CDK2/cyclinA3 respectively.
    GY06255 HSD992 HSD992 is a potent, selective CDK2/3 inhibitor with moderate CDK9 inhibition with IC50 of 18 nM, 57 nM and 49 nM for CDK3/cyclin E, CDK2/cyclin A1 and CDK2/cyclin E, respecively.
    GY06257 IIIM-290 IIIM-290 is a potent, orally active cyclin-dependent kinase (CDK) inhiitor with IC50 of 1.9 and 16 nM for Cdk-9/T1 and Cdk-2/A, respectively.
    GY06259 Compound 919278 Compound 919278 is a specific inhibitor of lymphotoxin β receptor (LTβR, IC50=0.169 uM), and TNF receptor superfamily member 12A (FN14)-dependent nuclear translocation of p52 (IC50=0.167 uM) via inhibiting CDK12/CCNK, does not inhibit the TNF-α-mediated nuclear translocation of p65 (RelA).
    GY06261 BI-1347 BI-1347 is a potent, selective inhibitor of CDK8/cyclinC with IC50 of 1 nM.
    GY06275 AZD-4573 AZD-4573 (AZD4573) is a potent and selective inhibitor of CDK9, with fast-off binding kinetics and high selectivity versus other kinases, including other CDK family kinases.
    GY06284 YKL-1-116 YKL-1-116 is a potent, selective and covalent inhibitor of CDK7 that does not inhibit other CDKs.
    GY06294 ICEC 0942 ICEC 0942 (CT7001) is a potent, selective, orally active CDK7 inhibitor with IC50 of 41 nM, displays 15-fold selectivity over CDK2 (IC50=578 nM).
    GY06295 ICEC 0942 HCl ICEC 0942 (CT7001) is a potent, selective, orally active CDK7 inhibitor with IC50 of 41 nM, displays 15-fold selectivity over CDK2 (IC50=578 nM).
    GY06322 Trilaciclib A novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 4 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.
    GY06326 BAY-958 BAY-958 (BAY958, LDC526) is a potent, selective PTEFb/CDK9 inhibitor with IC50 of 5 nM against CDK9/CyclinT1.
    GY06327 TAK-931 TAK-931 is a potent, selective, ATP competitive and orally bioavailable inhibitor of Cdc7 with IC50 of <0.3 nM.
    GY06335 Roniciclib A novel potent, orally active, pan-CDK inhibitor with IC50 of 7/9/11 nM for CDK1/2/4 respectively, inhibits transcriptional CDK9/7 with IC50 of 5-25 nM.
    GY06337 VMY-1-103 A novel dansylated analog of purvalanol B, and a CDK inhibitor that inhibits cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B.
    GY07164 G1T38 A novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively
    GY07165 G1T38 dihydrochloride A novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively
    GY07189 CDK12 inhibitor E9 racemate A clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux
    GY07261 Fascaplysin chloride A potent CDK4/cyclin D1 with IC50 of 0.35 uM, 10-fold less potent for significantly for CDK6/cyclin D1 and does not inhibit other Cdks and tyrosine kinases
    GY07367 GSK3186899 GSK3186899 is an inhibitor of cdc-2-related kinase 12 (CRK12), with an EC50 of 1.4 μM for L. donovani in an intra-macrophage assay.