PI3K

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1009 Dactolisib (BEZ235, NVP-BEZ235) <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 Idelalisib (CAL-101, GS-1101) <1 mg/mL 83 mg/mL 23 mg/mL
S2247 Buparlisib (BKM120, NVP-BKM120) <1 mg/mL 82 mg/mL 2 mg/mL
S8596 Autophinib <1 mg/mL 69 mg/mL <1 mg/mL
S8581 Serabelisib (INK-1117,MLN-1117,TAK-117) <1 mg/mL 16 mg/mL <1 mg/mL
S8330 IPI-549 <1 mg/mL 100 mg/mL 8 mg/mL
S8589 SF2523 <1 mg/mL 29 mg/mL 7 mg/mL
S8157 GDC-0326 <1 mg/mL 76 mg/mL 19 mg/mL
S7682 SAR405 <1 mg/mL 88 mg/mL 88 mg/mL
S8194 TGR-1202 <1 mg/mL 100 mg/mL 7 mg/mL
S8456 VPS34 inhibitor 1 (Compound 19, PIK-III analogue) <1 mg/mL 78 mg/mL <1 mg/mL
S7937 GSK2269557 <1 mg/mL 88 mg/mL 8 mg/mL
S7865 740 Y-P (PDGFR 740Y-P) 1 mg/mL -1 mg/mL -1 mg/mL
S8163 GDC-0084 <1 mg/mL 8 mg/mL <1 mg/mL
S7966 AZD8835 <1 mg/mL 93 mg/mL <1 mg/mL
S1038 PI-103 <1 mg/mL 24 mg/mL <1 mg/mL
S2638 NU7441 (KU-57788) <1 mg/mL 4 mg/mL <1 mg/mL
S1169 TGX-221 <1 mg/mL 12 mg/mL <1 mg/mL
S1268 IC-87114 <1 mg/mL 0.66 mg/mL <1 mg/mL
S2758 Wortmannin <1 mg/mL 85 mg/mL <1 mg/mL
S1118 XL147 analogue <1 mg/mL 3 mg/mL <1 mg/mL
S1072 ZSTK474 <1 mg/mL 21 mg/mL <1 mg/mL
S2814 Alpelisib (BYL719) <1 mg/mL 88 mg/mL 2 mg/mL
S1410 AS-605240 <1 mg/mL 0.4 mg/mL <1 mg/mL
S1205 PIK-75 HCl <1 mg/mL 4 mg/mL <1 mg/mL
S2767 3-Methyladenine (3-MA) 10 mg/mL 3 mg/mL 4 mg/mL
S2636 A66 <1 mg/mL 79 mg/mL 1 mg/mL
S1523 Voxtalisib (SAR245409, XL765) Analogue <1 mg/mL 12 mg/mL <1 mg/mL
S1489 PIK-93 <1 mg/mL 78 mg/mL <1 mg/mL
S2658 Omipalisib (GSK2126458, GSK458) <1 mg/mL 100 mg/mL <1 mg/mL
S1187 PIK-90 <1 mg/mL 0.28 mg/mL <1 mg/mL
S1462 AZD6482 <1 mg/mL 82 mg/mL 10 mg/mL
S2743 PF-04691502 <1 mg/mL 14 mg/mL <1 mg/mL
S2696 Apitolisib (GDC-0980, RG7422) <1 mg/mL 20 mg/mL <1 mg/mL
S1360 GSK1059615 <1 mg/mL 2 mg/mL <1 mg/mL
S7028 Duvelisib (IPI-145, INK1197) <1 mg/mL 83 mg/mL <1 mg/mL
S2628 Gedatolisib (PF-05212384, PKI-587) <1 mg/mL 2 mg/mL <1 mg/mL
S1352 TG100-115 <1 mg/mL 9 mg/mL <1 mg/mL
S2671 AS-252424 <1 mg/mL 61 mg/mL <1 mg/mL
S2749 BGT226 (NVP-BGT226) <1 mg/mL 30 mg/mL <1 mg/mL
S2759 CUDC-907 <1 mg/mL 102 mg/mL <1 mg/mL
S2227 PIK-294 <1 mg/mL 98 mg/mL <1 mg/mL
S2681 AS-604850 <1 mg/mL 57 mg/mL 5 mg/mL
S8002 GSK2636771 <1 mg/mL 28 mg/mL <1 mg/mL
S2802 Copanlisib (BAY 80-6946) 0.002 mg/mL 0.002 mg/mL 0.01 mg/mL
S1219 YM201636 <1 mg/mL 35 mg/mL <1 mg/mL
S2699 CH5132799 <1 mg/mL 12 mg/mL <1 mg/mL
S2682 CAY10505 <1 mg/mL 58 mg/mL <1 mg/mL
S2207 PIK-293 <1 mg/mL 80 mg/mL <1 mg/mL
S2739 PKI-402 <1 mg/mL 0.4 mg/mL <1 mg/mL
S2870 TG100713 <1 mg/mL 2 mg/mL <1 mg/mL
S7016 VS-5584 (SB2343) <1 mg/mL 71 mg/mL 3 mg/mL
S7103 Taselisib (GDC 0032) <1 mg/mL 70 mg/mL <1 mg/mL
S7018 CZC24832 <1 mg/mL 5 mg/mL <1 mg/mL
S7813 AMG319 <1 mg/mL 77 mg/mL 77 mg/mL
S7938 GSK2292767 <1 mg/mL 100 mg/mL <1 mg/mL
S7356 HS-173 <1 mg/mL 84 mg/mL <1 mg/mL
S2391 Quercetin <1 mg/mL 61 mg/mL 10 mg/mL
S7646 Voxtalisib (XL765, SAR245409) <1 mg/mL 54 mg/mL <1 mg/mL
S7798 GNE-317 <1 mg/mL 47 mg/mL <1 mg/mL
S8322 LY3023414 <1 mg/mL 47 mg/mL 61 mg/mL
S7980 VPS34-IN1 <1 mg/mL 85 mg/mL 85 mg/mL
S7683 PIK-III <1 mg/mL 63 mg/mL 63 mg/mL
S7623 PI-3065 <1 mg/mL 50 mg/mL <1 mg/mL
S7645 Pilaralisib (XL147) <1 mg/mL 100 mg/mL <1 mg/mL
S7675 PF-4989216 <1 mg/mL 76 mg/mL 7 mg/mL
S7694 AZD8186 <1 mg/mL 91 mg/mL 35 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1009

Dactolisib (BEZ235, NVP-BEZ235)

Dactolisib (BEZ235, NVP-BEZ235) 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.

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.

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.

S2226

Idelalisib (CAL-101, GS-1101)

Idelalisib (CAL-101, 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.

S2247

Buparlisib (BKM120, NVP-BKM120)

Buparlisib (BKM120, NVP-BKM120) 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.

S8596New

Autophinib

Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.

S8581New

Serabelisib (INK-1117,MLN-1117,TAK-117)

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.

S8330New

IPI-549

IPI-549 is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM.

S8589New

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.

S8157New

GDC-0326

GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays.

S7682New

SAR405

SAR405 is a low-molecular-mass kinase inhibitor of Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR.

S8194New

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.

S8456New

VPS34 inhibitor 1 (Compound 19, PIK-III analogue)

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.

S7937New

GSK2269557

Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).

S8163New

GDC-0084

GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR.

S7966New

AZD8835

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).

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.

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.

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.

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.

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.

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.

S1072

ZSTK474

ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2.

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.

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.

S1205

PIK-75 HCl

PIK-75 HCl 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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

S8002

GSK2636771

GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines.

S2802

Copanlisib (BAY 80-6946)

Copanlisib (BAY 80-6946) 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.

S1219

YM201636

YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue).

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.

S2682

CAY10505

CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM.

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.

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.

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.

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.

S7103

Taselisib (GDC 0032)

Taselisib (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.

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.

S7813

AMG319

AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.

S7938

GSK2292767

GSK2292767 is a potent and selective PI3Kδ inhibitor.

S7356

HS-173

HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.

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.

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.

S7798

GNE-317

GNE-317 is a potent, brain-penetrant PI3K inhibitor.

S8322

LY3023414

LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.

S7980

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.

S7683

PIK-III

PIK-III, which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates.

S7623

PI-3065

PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.

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.

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.

S7694

AZD8186

AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.

S7865New

740 Y-P (PDGFR 740Y-P)

740 Y-P is cell-permeable phosphopeptide activator of PI3K.

Catalog No. Information Product Use Citations Product Validations
S1009

Dactolisib (BEZ235, NVP-BEZ235)

Dactolisib (BEZ235, NVP-BEZ235) 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.

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.

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.

S2226

Idelalisib (CAL-101, GS-1101)

Idelalisib (CAL-101, 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.

S2247

Buparlisib (BKM120, NVP-BKM120)

Buparlisib (BKM120, NVP-BKM120) 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.

S8596New

Autophinib

Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.

S8581New

Serabelisib (INK-1117,MLN-1117,TAK-117)

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.

S8330New

IPI-549

IPI-549 is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM.

S8589New

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.

S8157New

GDC-0326

GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays.

S7682New

SAR405

SAR405 is a low-molecular-mass kinase inhibitor of Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR.

S8194New

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.

S8456New

VPS34 inhibitor 1 (Compound 19, PIK-III analogue)

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.

S7937New

GSK2269557

Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).

S8163New

GDC-0084

GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR.

S7966New

AZD8835

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).

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.

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.

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.

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.

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.

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.

S1072

ZSTK474

ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2.

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.

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.

S1205

PIK-75 HCl

PIK-75 HCl 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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

S8002

GSK2636771

GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines.

S2802

Copanlisib (BAY 80-6946)

Copanlisib (BAY 80-6946) 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.

S1219

YM201636

YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue).

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.

S2682

CAY10505

CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM.

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.

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.

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.

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.

S7103

Taselisib (GDC 0032)

Taselisib (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.

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.

S7813

AMG319

AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.

S7938

GSK2292767

GSK2292767 is a potent and selective PI3Kδ inhibitor.

S7356

HS-173

HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.

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.

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.

S7798

GNE-317

GNE-317 is a potent, brain-penetrant PI3K inhibitor.

S8322

LY3023414

LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.

S7980

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.

S7683

PIK-III

PIK-III, which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates.

S7623

PI-3065

PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.

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.

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.

S7694

AZD8186

AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.

Catalog No. Information Product Use Citations Product Validations
S7865New

740 Y-P (PDGFR 740Y-P)

740 Y-P is cell-permeable phosphopeptide activator of PI3K.

Tags: PI3K inhibition | PI3K cancer | PI3K activation | PI3K signaling pathway | PI3 kinase pathway | PI3K activity | PI3K phosphorylation | PI3K assay | PI3K inhibitor cancer | PI3K inhibitor drugs | PI3K targets | PI3K inhibitors ic50 | PI3K inhibitors in clinical trials | PI3K inhibitor review