Product Categories

PI3K Phosphatidylinositol 3-kinase

PI3K Inhibitors (41)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
S1009 BEZ235 (NVP-BEZ235) BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively, and also inhibits ATR with IC50 of 21 nM.
S1105 LY294002 LY294002 is a PI3K inhibitor for p110α, p110δ and p110β with IC50 of 0.5 μM, 0.57 μM and 0.97 μM, respectively.
S1065 GDC-0941 GDC-0941 is a potent inhibitor of PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ with IC50 of 3 nM, 33 nM, 3 nM and 75 nM, respectively.
S2226 CAL-101 (GS-1101) CAL-101 is a selective PI3K class I inhibitor of p110δ with IC50 of 2.5 nM.
S2247 BKM120 (NVP-BKM120) BKM120 is a selective PI3K inhibitor of p110α, p110β, p110δ and p110γ with IC50 of 52-99 nM, 166 nM, 116 nM and 262 nM, respectively.
S7028 IPI-145 (INK1197) IPI-145 (INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM.
S2638 NU7441 (KU-57788) NU7441 is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 μM.
S2814 BYL719 BYL719 strongly and selectively inhibits PI3Kα.
S1038 PI-103 PI-103 is a potent, ATP-competitive PI3K inhibitor of DNA-PK, p110α, mTORC1, PI3KC2β, p110δ, mTORC2, p110β, and p110γ with IC50 of 2 nM, 8 nM, 20 nM, 26 nM, 48 nM, 83 nM, 88 nM and 150 nM, respectively.
S1169 TGX-221 TGX-221 is a potent, selective PI3K inhibitor for p110β with IC50 of 8.5 nM.
Cat.No. Product Name Information Product Citations Customer Reviews
S2758 Wortmannin Wortmannin is a multi-target inhibitor of MLCK and PI3K with IC50 of 170 nM and 3 nM, and also potentlt inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM (less sensitive to ATR with IC50 of 1.8 μM).
S2636 A66 A66 is a potent and specific p110α inhibitor with IC50 of 32 nM.
S1072 ZSTK474 ZSTK474 is a potent pan-class I PI3K inhibitor with IC50 of 37 nM.
S1118 XL147 XL147 (SAR245408) is a selective and reversible class I PI3K inhibitor for wild type and mutant p110α with IC50 of 40 nM and 40 nM, respectively.
S2767 3-Methyladenine 3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM, respectively.
S1268 IC-87114 IC-87114 is a selective inhibitor of PI3Kδ with IC50 of 0.5 μM.
S1410 AS-605240 AS-605240 is a novel, potent and selective PI3Kγ inhibitor with IC50 of 8 nM.
S2671 AS-252424 AS-252424 is a novel, potent and selective inhibitor of PI3Kγ with IC50 of 33 nM.
S1523 XL765 (SAR245409) XL765 is a dual inhibitor of mTOR/PI3k for mTOR, p110α, p110β, p110γ and p110δ with IC50 of 157 nM, 39 nM, 113 nM, 9 nM and 43 nM, respectively.
S2658 GSK2126458 GSK2126458 is a highly selective and potent inhibitor of p110α, p110β, p110γ, p110δ, mTORC1 and mTORC2 with Ki of 0.019 nM, 0.13 nM, 0.024 nM, 0.06 nM, 0.18 nM and 0.3 nM, respectively.
Cat.No. Product Name Information Product Citations Customer Reviews
S1205 PIK-75 PIK-75 is a selective and competitive inhibitor of p110α with IC50 of 5.8 nM and also potently inhibits DNA-PK with IC50 of 2 nM.
S2743 PF-04691502 PF-04691502 is an ATP-competitive, selective inhibitor of PI3K(α/β/δ/γ)/mTOR with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, also inhibits Akt phosphorylation on T308/S473 with IC50 of 7.5 nM/3.8 nM.
S1462 AZD6482 AZD6482 is an inhibitor of PI3Kβ with IC50 of 21 nM.
S2628 PF-05212384 (PKI-587) PKI-587 is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively.
S2696 GDC-0980 (RG7422) GDC-0980 (RG7422) is a potent, selective inhibitor of PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ with IC50 of 5 nM, 27 nM, 7 nM, and 14 nM, and also a mTOR inhibitor with Ki of 17 nM.
S1489 PIK-93 PIK-93 is a novel and potent inhibitor of PI3Kγ and PI4KIIIβ with IC50 of 16 nM and 19 nM, respectively.
S1187 PIK-90 PIK-90 is a potent and cell permeable inhibitor of p110α, p110β, p110γ and p110δ with IC50 of 11 nM, 350 nM, 18 nM and 58 nM, respectively.
S2802 BAY80-6946 BAY 80-6946 is a potent and highly selective reversible PI3K inhibitor for PI3Kα and PI3Kβ with IC50 of 0.469 nM and 3.72 nM, respectively.
S1352 TG100-115 TG100-115 is a potent and dual selective inhibitor for PI3Kγ and PI3Kδ with IC50 of 83 nM and 235 nM, respectively.
S1219 YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM.
Cat.No. Product Name Information Product Citations Customer Reviews
S1360 GSK1059615 GSK1059615 is a novel and dual inhibitor of PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR with IC50 of 0.4 nM, 0.6 nM, 2 nM, 5 nM and 12 nM, respectively.
S2227 PIK-294 PIK-294 is a highly potent and selective p110δ inhibitor with IC50 of 10 nM.
S2681 AS-604850 AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM.
S2699 CH5132799 CH5132799 exhibits a strong inhibitory activity especially against PI3Kα with IC50 of 14 nM and also inhibits mTOR with IC50 of 1.6 µM.
S2682 CAY10505 CAY10505 is a PI3Kγ inhibitor with IC50 of 30 nM.
S2749 NVP-BGT226 NVP-BGT226 is a novel dual PI3K/mTOR inhibitor with IC50 of 1 nM.
S2759 PI3K/HDAC InhibitorⅠ PI3K/HDAC Inhibitor I is a dual PI3K and HDAC inhibitor for PI3Kɑ, HDAC1, HDAC2, HDAC3 and HDAC10 with IC50 of 19 nM, 1.7 nM, 5 nM, 1.8 nM and 2.8 nM, respectively.
S2207 PIK-293 PIK-293 is a PI3-K inhibitor for p110α, p110β, p110δ and p110γ with IC50 of 100 μM, 25 μM, 0.24 μM and 10 μM, respectively.
S2739 PKI-402 PKI-402 is a potent dual PI3K/mTOR inhibitor targeting PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR with IC50 of 2 nM, 7 nM, 16 nM, 14 nM, and 3 nM, respectively.
S2870 TG 100713 TG 100713 is a PI3K inhibitor for PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.
Cat.No. Product Name Information Product Citations Customer Reviews
S8002 GSK2636771 GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor.
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All PI3K Inhibitors

Phosphatidylinositol 3-kinases (PI3Ks) are a family of lipid kinases whose biological function is to phosphorylate the 3-hydroxyl group of phosphoinositide. It is proved that PI3K-dependent signaling pathway contributes to many cellular processes such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which might be involved in oncogenesis under certain situation[1]. When a growth factor or ligand binds to the tyrosine kinase receptors (RTK), the PI3K is activated by G protein-coupled receptors[2]. PI3Ks family is generally divided into Class I, Class II, and Class III according to their primary structure, regulation, and in vitro lipid substrate specificity[2]. Class I PI3Ks are heterodimeric molecules composed of a regulatory subunit (p85) and a catalytic subunit (p110). The regulatory subunit of PI3K could be further divided in to six subtypes: p85-α, p85-β, p55-γ, p150,p101 and p87. P85α is the most highly expressed regulatory subunit than the others. And the catalytic subunit could also further divided into four subtypes: p110-α, p110-β, p110-γ and p110-δ. The α and β isoforms of p110 are expressed in all kinds of cells, whereas δ is only found in leukocytes. The regulatory subunit p101 and catalytic subunit p110γ comprise a complex which is classified as Class IB PI3K. Other collocations of regulatory and catalytic subunits are called Class IA PI3Ks. However, class II is structurally different from Class I. There are three catalytic isoforms of Class II PI3Ks: PI3K-C2α, -C2β, and -C2γ, but no regulatory subunit. Class III is structurally similar to Class I for the reason that it is composed of a catalytic (Vps34) and a regulatory subunit (p150). Functionally, class I PI3Ks catalyze the production of phosphatidylinositol 3-phosphate (PtdIns-3,4-P), phosphatidylinositol (3,4)-bisphosphate (PtdIns-3,4-P2), and phosphatidylinositol (3,4,5)-triphosphate (PtdIns-3,4,5-P3). Class II is related to the production of PtdIns-3-P and PtdIns-3,4-P2, while class III specifically catalyzes the production of PtdIns-3,4-P2 [3-5].

References

[1] Cantley, L.C., The phosphoinositide 3-kinase pathway. Science, 2002. 296(5573): p. 1655-7.
[2] Leevers, S.J., B. Vanhaesebroeck, and M.D. Waterfield, Signalling through phosphoinositide 3-kinases: the lipids take centre stage. Curr Opin Cell Biol, 1999. 11(2): p. 219-25.
[3] Stokoe, D., The phosphoinositide 3-kinase pathway and cancer. Expert Rev Mol Med, 2005. 7(10): p. 1-22.
[4] Vanhaesebroeck, B., et al., Signalling by PI3K isoforms: insights from gene-targeted mice. Trends Biochem Sci, 2005. 30(4): p. 194-204.
[5] Engelman, J.A., J. Luo, and L.C. Cantley, The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism. Nat Rev Genet, 2006. 7(8): p. 606-19.

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