PI3K

PI3K Inhibitors (53)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1009 BEZ235 (NVP-BEZ235, Dactolisib) BEZ235 (NVP-BEZ235, Dactolisib) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.
  • Nature, 2012, 487(7408):505-9
  • Nat Med, 2015, 10.1038/nm.3855
  • Cancer Cell, 2012, 21(2):155-67
S1065 Pictilisib (GDC-0941) Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2.
  • Nature, 2014, 508(7494):118-22
  • Cell Stem Cell, 2012, 10(2):210-7
  • Cancer Discov, 2011, 1(7):608-25
S1105 LY294002 LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.
  • Nature, 2015, 10.1038/nature14412
  • Hepatology, 2014, 59(4):1262-72
  • Blood, 2014, 123(2):239-48
S2226 CAL-101 (Idelalisib, GS-1101) CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.
  • Nature, 2015, 517(7535):460-5
  • Nature, 2013, 496(7446):523-7
  • Cancer Discov, 2014, 4(9):1022-35
S2247 BKM120 (NVP-BKM120, Buparlisib) BKM120 (NVP-BKM120, Buparlisib) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.
  • Nat Med, 2015, 10.1038/nm.3855
  • Cancer Cell, 2012, 21(2):155-67
  • Cancer Discov, 2013, 4(2):232-45
S7646 Voxtalisib (XL765, SAR245409) Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
S7813 AMG319 AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
S7103 GDC-0032 GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
  • Cell, 2013, 153(4):840-54
  • Leukemia, 2013, 27(3):650-60
  • Leukemia, 2012, 26(5):927-33
S2638 NU7441 (KU-57788) NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 μM in cell-free assays.
  • Genes Dev, 2014, 28(8):875-87
  • Nucleic Acids Res, 2014, 42(12):7776-92
  • Nucleic Acids Res, 2014, 42(9):5616-32
S7694 AZD8186 AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.
S7675 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.
S7645 Pilaralisib (XL147) Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
S7798 GNE-317 GNE-317 is a potent, brain-penetrant PI3K inhibitor.
S7623 PI-3065 PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
S7356 HS-173 HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
S8002 GSK2636771 GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.
  • Blood, 2015, 10.1182/blood-2014-11-610329
S7016 VS-5584 (SB2343) 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. Phase 1.
S7018 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.
  • Anticancer Res, 2015, 35(5):2699-708
S7028 Duvelisib (IPI-145, INK1197) Duvelisib (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 in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3.
  • Int J Cancer, 2015, 10.1002/ijc.29579
S1352 TG100-115 TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2.
  • Exp Mol Med, 2015, 47:e143
  • Shock, 2013, 39(1):83-8
S2636 A66 A66 is a potent and specific p110α inhibitor with IC50 of 32 nM in a cell-free assay, >100 fold selectivity for p110α over other class-I PI3K isoforms.
  • Nature, 2015, 517(7535):460-5
  • Genes Dev, 2012, 26(14):1573-86
  • Cell Death Differ, 2013, 21(3):491-502
S1219 YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue).
S2682 CAY10505 CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM.
  • Br J Haematol, 2014, 166(4):529-39
S1360 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. Phase 1.
  • Nature, 2012, 486(7404):532-6
  • Nat Chem Biol, 2013, 9(11):708-14
  • Exp Mol Med, 2015, 47:e143
S2743 PF-04691502 PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2.
  • Blood, 2015, 10.1182/blood-2014-11-610329
  • Cell Rep, 2015, 11(3):446-59
  • Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268
S1205 PIK-75 PIK-75 is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.
  • Cell Death Differ, 2013, 21(3):491-502
  • Stem Cells, 2015, 10.1002/stem.1986
  • Mol Carcinog, 2012, 52(9):667-75
S1489 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.
  • Mol Cell Endocrinol, 2013, 372(1-2):86-95
  • PLoS One, 2015, 10(3):e0122753
S1410 AS-605240 AS-605240 selectively inhibits PI3Kγ with IC50 of 8 nM, over 30-fold and 7.5-fold more selective for PI3Kγ than PI3Kδ/β and PI3Kα in cell-free assays, respectively.
  • Blood, 2015, 10.1182/blood-2014-11-610329
  • J Pharmacol Exp Ther, 2013, 347(3):669-80
  • Exp Gerontol, 2014, 52:55-69
S2749 BGT226 (NVP-BGT226) BGT226 (NVP-BGT226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
  • Mol Cancer Ther, 2015, 14(8):1928-38
  • Cancer Lett, 2014, 348(1-2):38-49
  • PLoS One, 2014, 9(3):e90746
S1462 AZD6482 AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1.
  • Blood, 2014, 125(5):881-8
  • Diabetologia, 2013, 56(6):1339-49
  • Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268
S1523 Voxtalisib (SAR245409, XL765) 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.
  • Cell Rep, 2015, 11(3):446-59
  • Endocrinology, 2013, 154(3):1247-59
  • Mol Cancer Res, 2014, 12(5):703-13
S2814 Alpelisib (BYL719) Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.
  • Blood, 2015, 10.1182/blood-2014-11-610329
  • J Thorac Oncol, 2015, 10(12):1736-44
  • Br J Haematol, 2014, 165(1):89-101
S2759 CUDC-907 CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. Phase 1.
  • Am J Transl Res, 2014, 6(5):471-493
S1268 IC-87114 IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β.
  • Cancer Cell, 2015, 27(1):97-108
  • Cancer Discov, 2012, 2(5):425-33
  • Oncogene, 2014, 33(23):3043-53
S2658 Omipalisib (GSK2126458, GSK458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Phase 1.
  • Proc Natl Acad Sci USA, 2013, 110(10):4015-20
  • Mol Cancer Ther, 2015, 14(2):429-39
  • J Pharmacol Exp Ther, 2013, 347(3):669-80
S2870 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.
  • MedChemComm, 2013, 10.1039/c3md00301a
S2628 Gedatolisib (PF-05212384, PKI-587) Gedatolisib (PF-05212384, 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 in cell-free assays, respectively. Phase 2.
  • Cell Rep, 2015, 11(3):446-59
  • Mol Cancer Ther, 2015, 14(2):429-39
  • Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268
S2699 CH5132799 CH5132799 inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines. Phase 1.
  • Am J Transl Res, 2014, 6(5):471-493
  • Biochimie, 2014, 105:182-91
S2739 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.
S2802 BAY 80-6946 (Copanlisib) BAY 80-6946 (Copanlisib) is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.
S1169 TGX-221 TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α.
  • Cancer Cell, 2015, 27(1):97-108
  • Blood, 2014, 123(2):239-49
  • Oncogene, 2015, 10.1038/onc.2015.173
S1118 XL147 analogue XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
  • Autophagy, 2012, 8(6):903-14
  • Cancer Res, 2014, 74(18):5184-94
  • Oncogene, 2015, 10.1038/onc.2015.143
S1187 PIK-90 PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ.
  • J Cell Biol, 2012, 198(2):185-94
  • J Biol Chem, 2014, 10.1074/jbc.M114.554162
  • Exp Mol Med, 2015, 47:e143
S2207 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.
S2227 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.
  • Mol Cell Biol, 2012, 32(12):2268-78
S2767 3-Methyladenine (3-MA) 3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation.
  • Cell Death Dis, 2016, 7(6):e2247
  • Cell Physiol Biochem, 2016, 38(6):2401-13
  • Am J Cancer Res, 2015, 5(1):125-139
S2391 Quercetin Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Phase 4.
S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.
  • Nature, 2015, 10.1038/nature14412
  • Cancer Res, 2014, 74(10):2846-56
  • Cell Rep, 2015, 10.1016/j.celrep.2015.01.014
S1072 ZSTK474 ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2.
  • J Cell Sci, 2014, 127(Pt 4):788-800
  • Biochem J, 2014, 459(3):513-24
  • J Cell Mol Med, 2015, 19(9):2244-52
S2671 AS-252424 AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.
  • Blood, 2014, 123(2):239-51
  • Cell Death Differ, 2014, 21(3):491-502
  • Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268
S2681 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.
  • J Biol Chem, 2014, 289(46):32109-20
S2696 Apitolisib (GDC-0980, RG7422) Apitolisib (GDC-0980, RG7422) 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. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Phase 2.
  • Cancer Discov, 2014, 4(5):554-63
  • Mol Cancer Ther, 2015, 14(8):1928-38
  • Breast Cancer Res, 2014, 16(4):406

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1009 BEZ235 (NVP-BEZ235, Dactolisib) <1 mg/mL 0.01 mg/mL <1 mg/mL
S1065 Pictilisib (GDC-0941) <1 mg/mL 44 mg/mL <1 mg/mL
S1105 LY294002 <1 mg/mL 36 mg/mL 21 mg/mL
S2226 CAL-101 (Idelalisib, GS-1101) <1 mg/mL 83 mg/mL 23 mg/mL
S2247 BKM120 (NVP-BKM120, Buparlisib) <1 mg/mL 82 mg/mL 2 mg/mL
S7646 Voxtalisib (XL765, SAR245409) <1 mg/mL 54 mg/mL <1 mg/mL
S7813 AMG319 <1 mg/mL 77 mg/mL 77 mg/mL
S7103 GDC-0032 <1 mg/mL 70 mg/mL <1 mg/mL
S1038 PI-103 <1 mg/mL 24 mg/mL <1 mg/mL
S2638 NU7441 (KU-57788) <1 mg/mL 3 mg/mL <1 mg/mL
S7694 AZD8186 <1 mg/mL 91 mg/mL 35 mg/mL
S7675 PF-4989216 <1 mg/mL 76 mg/mL 7 mg/mL
S7645 Pilaralisib (XL147) <1 mg/mL 100 mg/mL <1 mg/mL
S7798 GNE-317 <1 mg/mL 47 mg/mL <1 mg/mL
S7623 PI-3065 <1 mg/mL 50 mg/mL <1 mg/mL
S7356 HS-173 <1 mg/mL 84 mg/mL <1 mg/mL
S8002 GSK2636771 <1 mg/mL 28 mg/mL <1 mg/mL
S7016 VS-5584 (SB2343) <1 mg/mL 71 mg/mL 3 mg/mL
S7018 CZC24832 <1 mg/mL 5 mg/mL <1 mg/mL
S7028 Duvelisib (IPI-145, INK1197) <1 mg/mL 83 mg/mL <1 mg/mL
S1352 TG100-115 <1 mg/mL 9 mg/mL <1 mg/mL
S2636 A66 <1 mg/mL 79 mg/mL 1 mg/mL
S1219 YM201636 <1 mg/mL 35 mg/mL <1 mg/mL
S2682 CAY10505 <1 mg/mL 58 mg/mL <1 mg/mL
S1360 GSK1059615 <1 mg/mL 2 mg/mL <1 mg/mL
S2743 PF-04691502 <1 mg/mL 14 mg/mL <1 mg/mL
S1205 PIK-75 <1 mg/mL 3 mg/mL <1 mg/mL
S1489 PIK-93 <1 mg/mL 78 mg/mL <1 mg/mL
S1410 AS-605240 <1 mg/mL 0.4 mg/mL <1 mg/mL
S2749 BGT226 (NVP-BGT226) <1 mg/mL 30 mg/mL <1 mg/mL
S1462 AZD6482 <1 mg/mL 82 mg/mL 10 mg/mL
S1523 Voxtalisib (SAR245409, XL765) Analogue <1 mg/mL 12 mg/mL <1 mg/mL
S2814 Alpelisib (BYL719) <1 mg/mL 88 mg/mL 2 mg/mL
S2759 CUDC-907 <1 mg/mL 102 mg/mL <1 mg/mL
S1268 IC-87114 <1 mg/mL 0.66 mg/mL <1 mg/mL
S2658 Omipalisib (GSK2126458, GSK458) <1 mg/mL 100 mg/mL <1 mg/mL
S2870 TG100713 <1 mg/mL 2 mg/mL <1 mg/mL
S2628 Gedatolisib (PF-05212384, PKI-587) <1 mg/mL 2 mg/mL <1 mg/mL
S2699 CH5132799 <1 mg/mL 12 mg/mL <1 mg/mL
S2739 PKI-402 <1 mg/mL 0.4 mg/mL <1 mg/mL
S2802 BAY 80-6946 (Copanlisib) 0.002 mg/mL 0.002 mg/mL 0.01 mg/mL
S1169 TGX-221 <1 mg/mL 12 mg/mL <1 mg/mL
S1118 XL147 analogue <1 mg/mL 3 mg/mL <1 mg/mL
S1187 PIK-90 <1 mg/mL 0.28 mg/mL <1 mg/mL
S2207 PIK-293 <1 mg/mL 80 mg/mL <1 mg/mL
S2227 PIK-294 <1 mg/mL 98 mg/mL <1 mg/mL
S2767 3-Methyladenine (3-MA) 20 mg/mL 3 mg/mL 4 mg/mL
S2391 Quercetin <1 mg/mL 61 mg/mL 10 mg/mL
S2758 Wortmannin <1 mg/mL 85 mg/mL <1 mg/mL
S1072 ZSTK474 <1 mg/mL 21 mg/mL <1 mg/mL
S2671 AS-252424 <1 mg/mL 61 mg/mL <1 mg/mL
S2681 AS-604850 <1 mg/mL 57 mg/mL 5 mg/mL
S2696 Apitolisib (GDC-0980, RG7422) <1 mg/mL 20 mg/mL <1 mg/mL
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