| 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. |
Pan |
hsVps34, IC50: 320 nM |
| 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 |
hVps34, IC50: 978 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 |
Vps34, IC50: 2.4 μM |
| S1118 |
XL147 |
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 |
Vps34, IC50: 6.975 μM |
| S2767 |
3-Methyladenine (3-MA) |
3-Methyladenine is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. |
Pan |
Vps34, IC50: 25 μM |