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    PI3K

    PI3K (Phosphoinositide 3-kinase), via phosphorylation of the inositol lipid phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), forms the second messenger molecule phosphatidylinositol (3,4,5)-trisphosphate (PI(3,4,5)P3) which recruits and activates pleckstrin homology domain containing proteins, leading to downstream signalling events crucial for proliferation, survival and migration. Class I PI3K enzymes consist of four distinct catalytic isoforms, PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ.There are three major classes of PI3K enzymes, being class IA widely associated to cancer. Class IA PI3K are heterodimeric lipid kinases composed of a catalytic subunit (p110α, p110β, or p110δ; encoded by PIK3CA, PIK3CB, and PIK3CD genes, respectively) and a regulatory subunit (p85).The PI3K pathway plays an important role in many biological processes, including cell cycle progression, cell growth, survival, actin rearrangement and migration, and intracellular vesicular transport.

    Products

    Catalog No. Name Description
    GY01245 Special Taselisib (GDC-0032) GDC-0032 is a potent β-sparing small molecule inhibitor of PI3K, with Ki values of 0.29 nM, 0.91 nM, 0.97 nM for PI3Kα, PI3Kβ and PI3Kγ, respectively.
    GY04284 Special 3-Methyladenine 3-Methyladenine is a potent inhibitor of autophagy and PI3K, blocking autophagy through its effect on PI3K, with IC50s of 25 μM and 60 μM for Vps34 and PI3Kγ, respectively.
    GY01012 Special LY294002 LY294002 is a broad-spectrum inhibitor of PI3K, with IC50 of 0.5/0.57/0.97 μM for PI3Kα/PI3Kδ/PI3Kβ, respectively, also potently inhibits CK2 with IC50 of 98 nM.
    GY01032 Special GDC-0941 (Pictilisib) GDC-0941 is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
    GY01045 Special Buparlisib (BKM120) NVP-BKM120 is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
    GY01056 Special BYL-719 BYL-719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM.
    GY01138 Special GSK2126458 GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively.
    GY01216 Special Duvelisib (IPI-145) Duvelisib is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
    GY01330 Special PF-04691502 PF-04691502 is a potent and selective inhibitor of PI3K and mTOR kinases with antitumor activity. PF-04691502 inhibits human and mouse PI3Kα with Ki of 1.8 and 1.2 nM, respectively, human PI3K isoforms β, δ, and γ with Ki of 2.1, 1.6, and 1.9 nM, respectively, and human mTOR with Ki of 16 nM.
    GY01344 Special GSK2636771 GSK2636771 is a potent, selective and orally bioavailable PI3Kβ inhibitor, sensitive to PTEN null cell lines.
    GY01388 Special TG100-115 TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.
    GY01504 Special NVP-BGT226 NVP-BGT226 is a potent pan-class I PI3K and mTOR catalytic inhibitor with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ.
    GY01536 Special PI3K inhibitor X PI3K inhibitor X is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.
    GY01571 Special VS-5584 VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC50s of 2.6 nM, 3.3 nM, 21 nM, 2.7 nM, 3 nM and 3.4 nM for PI3Kα, PI3Kα mt H1047R, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
    GY01586 Special PI3K-IN-1 PI3K-IN-1 is a potent inhibitor of PI3K, more information can be found in patent WO2012103524 A2 and WO2013147649 A2.
    GY01613 Special Pilaralisib (XL-147) XL147 is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
    GY01631 Special AS-252424 AS-252424 is a potent and selective PI3Kγ inhibitor with an IC50 of 30±10 nM.
    GY01707 Special PIK-90 PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
    GY01759 Special PIK-294 PIK-294 is a potent p110δ-selective inhibitor with an IC50 of 10 nM.
    GY02264 Special PQR309 PQR309 is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively.
    GY04277 Special CZC24832 CZC24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and >100-fold selectivity over PI3Kα and PI3Kδ.
    GY04450 Special Vps34-PIK-III Vps34-PIK-III is a potent and selective inhibitor of VPS34 with an IC50 of 18 nM.
    GY01628 Voxtalisib (SAR245409) SAR245409 is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM).
    GY01011 Dactolisib (BEZ235) BEZ235 is a dual pan-class I PI3K and mTOR kinase inhibitor with IC50 of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively.
    GY01115 BAY 80-6946 BAY 80-6946 is an ATP-competitive selective class-I PI3 kinases inhibitor, with IC50s of 0.5, 0.7, 3.7 and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, and much less active against mTOR (IC50=45 nM) and other PIKs (no inhibition at 1 μM).
    GY01125 Gedatolisib (PKI-587) PKI-587 is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively.
    GY01153 PI-103 PI-103 is a potent PI3K/Akt and mTOR inhibitor with IC50 values of 2 nM for recombinant PI3K isoform p110α and 30 nM for mTOR
    GY01239 Apitolisib (GDC-0980) GDC-0980 is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively, and also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases.
    GY01295 TGX-221 TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.
    GY01300 YYlxTYtXmNHGMFaUVdZ ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
    GY01338 Quercetin Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4±0.6 μM, 3.0±0.0 μM and 5.4±0.3 μM for PI3K γ, PI3K δ and PI3K β, respectively.
    GY01399 AS-605240 AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.
    GY01429 HS-173 HS-173 is a novel PI3K inhibitor, that is used for cancer treatment.
    GY01438 AZD8186 AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC5050=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
    GY01479 AZD 6482 AZD 6482 is a potent and selective p110β inhibitor with IC50 of 0.69 nM.
    GY01533 LY3023414 LY3023414 potently and selectively inhibits class I PI3K isoforms, mTORC1/2, and DNA-PK with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 165 nM and 4.24 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, mTOR and DNA-PK, respectively.
    GY01566 GSK1059615 GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
    GY01589 Vps34-IN-1 Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO/2012085815 A1, compound example 16a; has an IC50 of 4 nM.
    GY01636 AZD8835 AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively.
    GY01799 PF-4989216 PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.
    GY01834 CAY10505 CAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in neurons.
    GY01913 AMG319 AMG319 is a potent and selective PI3Kδ kinase inhibitor with IC50 of 18 nM.
    GY02195 PI3Kγ inhibitor 1 PI3Kγ inhibitor 1 is a PI3Kδ and PI3Kγ inhibitor extracted from patent WO2014004470A1, Compound 168 in Table 4, has IC50s of <100 nM.
    GY02199 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
    GY02257 PF-04979064 PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
    GY02285 PI3Kα inhibitor 1 PI3Kα inhibitor 1 is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .
    GY02286 740 Y-P 740 Y-P (PDGFR 740Y-P) is a potent and cell permeable PI3K activator.
    GY02310 GSK2269557 free base GSK2269557 free base is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.
    GY02334 Serabelisib (MLN1117) MLN1117 is a selective p110α inhibitor with an IC50 of 15 nM.
    GY02346 GDC-0326 GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
    GY02368 NVP-BKM120 HCl NVP-BKM120 Hydrochloride is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
    GY02386 PI3kδ inhibitor 1 PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM.
    GY02504 ON 146040 ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
    GY02556 CAL-130 CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
    GY02557 CAL-130 HCl CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
    GY02642 SAR405 SAR405 is a PIK3C3/Vps34 inhibitor with an IC50 of 1.2 nM. SAR405 also is a proximal inhibitor of the autophagy machinery.
    GY02645 Umbralisib (TGR-1202) TGR-1202 is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Also active against CK1ε, with an EC50 value of 6.0 μM.
    GY02646 Umbralisib (TGR-1202) R-enantiomer TGR-1202 R-enantiomer is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
    GY02751 Tenalisib Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.
    GY02772 NSC-781406 NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
    GY02780 IPI549 IPI549 is a potent and selective PI3Kγ Inhibitor with an IC50 of 16 nM.
    GY02791 PI3Kδ-IN-2 PI3Kδ-IN-2 is a potent and selective inhibitor of PI3Kδ extracted from patent WO 2015055071 A1, compound 10; has an IC50 of 6.4 nM.
    GY03002 GDC-0077 GDC-0077 is an orally available PI3K inhibitor with potential antineoplastic activity. GDC-0077 is extracted from patent WO 2017001645 A1, formula I.
    GY03213 PI-103 HCl PI-103 hydrochloride is a potent PI3K/Akt and mTOR inhibitor with IC50 values of 2 nM for recombinant PI3K isoform p110α and 30 nM for mTOR.
    GY03287 CAL-130 Racemate CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor.
    GY03596 NVP-BAG956 NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
    GY03760 Pictilisib (GDC-0941) dimethanesulfonate GDC-0941 dimethanesulfonate is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
    GY03814 MDK34597 (PI3K inhibitor) MDK34597 is a PI3K inhibitor.MDK34597 is an analog of PI-103 and acts as a dual PI3K/mTOR Inhibitor.
    GY03843 VPS34 inhibitor 1 VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
    GY04716 PQR530 PQR530 is a selective, orally bioavailable, potent dual PI3K/mTORC1/2 inhibitor.
    GY05638 IPI-443 A potent, selective, orally active p110δ/γ PI3K dual inhibitor with cellular IC50 of 0.29 and 7.1 nM, respectively.
    GY05871 SF-1126 SF-1126 is a pan PI3K/BRD4 inhibitor, RGDS-conjugated LY294002 prodrug that exhibits increased solubility and binds to specific integrins.
    GY05942 ST-168 ST-168 is a novel potent, orally available MEK/PI3K bifunctional inhibitor with IC50 of 182, 69.2, 1482, 2293, and 41.7 nM for MEK1, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively.
    GY05943 AS2541019 AS2541019 is a novel potent, selective, orally active PI3Kδ inhibitor with IC50 of 20.1 nM, >100-fold selectivity over other PI3K isoforms.
    GY05964 PI3Kδ inhibitor 52 A potent, selective, and efficacious PI3Kδ inhibitor with IC50 of 1.7 nM, >100-fold selectivitity over PI3Kγ/α/β.
    GY05973 PI3Kβ and δ inhibitor 20a A potent, highly selective PI3Kβ/δ inhibitor with IC50 of 7.8/5.3 nM respectively, with liitle to no activity on PI3Kα/γ (IC50=850/>10,000 nM).
    GY06043 Seletalisib Seletalisib (UCB-5857) is a potent, ATP-competitive, and selective PI3Kδ inhibitor with IC50 of 12 nM.
    GY06046 Leniolisib A novel potent and selective PI3Kδ inhibitor with biochemical IC50 of 11 nM.
    GY06063 GSK-2292767 GSK-2269557 is a highly potent and selective inhibitor of PI3Kδ (pKi=10.1).
    GY06066 SN-32976 SN-32976 is a novel, potent and selective class I PI3K and mTOR inhibitor with IC50 of 15.1/461/110/134/194 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR, respectively.
    GY06093 GNE-490 GNE-490 is a potent, selective, orally available class I PI3K inhibitor with IC50 of 3.5/25/5.2/15 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ.
    GY06145 ST-162 ST-162 is a potent, bifunctional MAPK/PI3K antagonist with IC50 of 191 nM and 398 nM for PI3Kα and MEK1, respectively.
    GY07005 BL-140 A novel specific p110β inhibitor with IC50 of 5.74 nM
    GY07015 LAS191954 A potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 of 2.6 nM
    GY06961 INCB040093 A novel potent, selective, orally available PI3Kδ inhibitor with IC50 of 31 nM.