p110α Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
|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, respectively. Phase 2.
|Selective||PI3Kα, IC50: 0.4 nM|
HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
|Selective||PI3Kα , IC50: 0.8 nM|
Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, and minimal effect on PI3Kβ/γ/δ. Phase 2.
|Selective||PI3Kα, IC50: 5 nM|
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.
|Selective||p110α, IC50: 5.8 nM|
A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.
|Selective||p110α, IC50: 32 nM|
YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue).
|Selective||p110α, IC50: 3.3 μM|
|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, respectively. Phase 1.
|Pan||p110α, Ki: 0.019 nM|
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.
|Pan||PI3Kα, IC50: 0.4 nM|
|S2802||BAY 80-6946 (Copanlisib)||
BAY 80-6946 (Copanlisib) is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM. Phase 2.
|Pan||PI3Kα, IC50: 0.469 nM|
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, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2.
|Pan||PI3Kα, Ki: 1.8 nM|
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.
|Pan||PI3Kα, IC50: 2 nM|
PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.
|Pan||p110α, IC50: 2 nM|
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.
|Pan||PI3Kα, IC50: 2.6 nM|
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). Phase 2.
|Pan||p110α, IC50: 3 nM|
|S1009||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, respectively. Inhibits ATR with IC50 of 21 nM, whileshown to be a poor inhibitor to Akt and PDK1. Phase 2.
|Pan||p110α, IC50: 4 nM|
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.
|Pan||PI3Kα, IC50: 4 nM|
|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, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus other PIKK family kinases. Phase 2.
|Pan||p110α, IC50: 5 nM|
PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ.
|Pan||PI3Kα, IC50: 11 nM|
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.
|Pan||PI3Kα, IC50: 14 nM|
ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM, mostly PI3Kδ. Phase1/2.
|Pan||PI3Kα, IC50: 16 nM|
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.
|Pan||PI3Kα, IC50: 19 nM|
|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, highly selective for PI3K δ/γ than other protein kinases. Phase 3.
|Pan||PI3Kα, Ki: 25900 pM|
XL147 is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM, less potent to PI3Kβ. Phase 1/2.
|Pan||PI3Kα, IC50: 39 nM|
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.
|Pan||PI3Kα, IC50: 39 nM|
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM.
|Pan||p110α, IC50: 39 nM|
|S2247||BKM120 (NVP-BKM120, Buparlisib)||
BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.
|Pan||p110α, IC50: 52 nM|
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, respectively.
|Pan||PI3Kα, IC50: 60 nM|
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.
|Pan||PI3Kα, IC50: 165 nM|
LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.
|Pan||p110α, IC50: 0.5 μM|
|S2226||CAL-101 (Idelalisib, GS-1101)||
CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.
|Pan||p110α, IC50: 820 nM|
AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ. Phase 1.
|Pan||PI3Kα, IC50: 870 nM|
AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.
|Pan||PI3Kα, IC50: 935 nM|
TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2.
|Pan||PI3Kα, IC50: 1.3 μM|
PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
|Pan||p110α, IC50: 2299 nM|
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.
|Pan||PI3Kα, IC50: 4.5 μM|
TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM, 1000-fold more selective for p110β than p110α.
|Pan||p110α, IC50: 5 μM|
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.
|Pan||p110α, IC50: 100 μM|
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