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Abmole Inhibitor Catalog 2017

PI3K Phosphoinositide 3-kinases


Cat.No.  Name Information
M6175 Serabelisib Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase.
M6152 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
M6084 IPI549 IPI549 is a potent and selective PI3Kγ Inhibitor with IC50 of 16 nM.
M5344 VPS34-IN1 Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.
M5343 Voxtalisib Analogue Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
M5337 PI-3065 PI-3065 is a novel potent and selective PI3K p110δ inhibitor with IC50 of 15 nM; exhibits > 100 fold selectivity against p110α, p110β, p110γ, DNA-PK and mTOR
M5335 PF-4989216 PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.
M5314 AZD-8835 AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).
M5268 TGR-1202 TGR-1202, a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively.
M5255 GDC-0326 GDC-0326 is Inhibitor of the class I phosphoinositide 3-kinase (PI3K) isoform PI3Kα which has received substantial attention for their potential use in cancer therapy.
M5231 GSK2269557 Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).
M4803 AZD8186 AZD8186 is a novel potent small molecule that targets the lipid kinase PI3Kβ with selectivity vs PI3Kα.
M3902 Quercetin Quercetin is a PI3K inhibitor with IC50 of 2.4-5.4 μM that has been shown to cause potent reversible inhibition of fatty-acid synthase.
M3880 Acalisib Acalisib (GS-9820) is an inhibitor of the beta and delta isoforms of the 110 kDa catalytic subunit of class IA phosphoinositide-3 kinases (PI3K) with potential immunomodulating and antineoplastic activities.
M3765 NVP-QAV-572 NVP-QAV-572 is a potent PI3K kianse inhibitor with IC50 of 10 nM.
M3730 CNX-1351 CNX-1351 is a selective covalent Inhibitor of PI3Kα.
M3682 PX-866 PX-866 is a ring-opened analog of wortmannin that potently and irreversibly inhibits PI3K (IC50 = 0.1-88 nM).
M3679 AMG 511 AMG 511, a potent and selective pan class I PI3K inhibitor exhibiting IC50 values of 8, 11, 2, and 6 nM against the PI3K α, β, δ, and γ isoforms respectively.
M3531 PIK-294 PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively.
M3474 PIK-93 PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM.
M3450 PIK-293 PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively.
M3368 AS-604850 AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα.
M3367 CAY10505 CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM.
M3304 YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue).
M3230 D-87503 D-87503 inhibits PI3K and Erk2 with IC50 of 62 nM and 760 nM, respectively.
M3218 PKI-402 PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R.
M3063 TG100713 TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.
M3007 SF1126 SF1126 is a soluble, vascular targeted pan-PI3K inhibitor.
M2609 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.
M2567 VS-5584 VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.
M2436 BAY 80-6946 BAY 80-6946 is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM.
M2296 3-Methyladenine 3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM, respectively.
M2295 AZD6482 AZD6482 is an inhibitor of PI3Kβ with IC50 of 21 nM.
M2220 GDC-0941 Bimesylate GDC-0941 Bimesylate is the orally bioavailable bismesylate salt of a potent inhibitor of the class I phosphatidylinositol 3 kinase (PI3K).
M2135 GDC-0032 GDC-0032 is a potent, next generation PI3-kinase inhibitor.
M2104 BYL719 BYL719 is the first oral PI3K inhibitor that strongly and selectively inhibits the PI3K alpha isoform of PI3K.
M2073 IPI-145 IPI-145 is a potent, oral inhibitor of phosphoinositide-3-kinase (PI3K)-delta and PI3K-gamma.
M2053 Wortmannin Wortmannin is a specific, covalent inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) with IC50 of 3 nM.
M2050 GSK2636771 GSK2636771 is a potent, orally available and specific PI3K p110β (PI3K beta, PI3Kβ) inhibitor.
M1984 PF-04691502 PF-04691502 is a potent and selective, ATP-competitive PI3K/mTOR inhibitor with IC50 of 7.5 nM and 3.8 nM of AKT T308 and AKT S473, respectively.
M1978 GSK1059615 GSK1059615 is a potent, ATP-competitive inhibitor of PI 3-kinase alpha (PI3Kα) with IC50 of 2 nM.
M1945 CAL-101 CAL-101 (GS-1101) is an oral PI3Kδ-specific inhibitor that has shown preclinical and clinical activity in non-Hodgkin lymphoma and chronic lymphocytic leukemia.
M1933 GNE-493 GNE-493 is a potent, selective and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitor for the treatment of cancer.
M1931 GSK2126458 GSK2126458 is a highly potent inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) with low picomolar to subnanomolar activity.
M1925 LY294002 LY294002 is a highly selective PI3K inhibitor with IC50 values of 0.31, 0.73, 1.06 and 6.60 μM for PI3Kβ, PI3Kα, PI3Kδ and PI3Kγ respectively.
M1896 PIK-90 PIK-90 is a novel and potent PI3K inhibitor with IC50 values of 11 nM, 350 nM, 18 nM and 58 nM for p110α, p110β, p110γ and p110δ respectively.
M1886 TG100-115 TG100-115 is a selective PI3K γ/δ inhibitor with IC50 values of 83 and 235 nM respectively.
M1879 XL147 XL147 (SAR245408) is an orally bioavailable, selective small molecule Class I PI3K kinase family inhibitor.
M1878 ZSTK474 ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3-kinase (PI3K), induces G1 arrest of the cell cycle in vivo.
M1849 XL765 XL765 is a PI3K/mTOR dual kinase inhibitor with IC50 values of 157 nM, 39 nM, 113 nM, 9 nM and 43 nM for mTOR, p110α, p110β, p110γ and p110δ, respectively.

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