Autophinib 是一种选择性细胞自噬抑制剂，通过靶向VPS34来抑制饥饿或雷帕霉素诱导的细胞自噬，对于饥饿和雷帕霉素诱导的自噬，IC50值分别为 90 nM 和 40 nM。它还是 ATP 竞争性VPS34抑制剂，其IC50值为 19 nM。

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.

Autophinib targets VPS34 but not other lipid kinases, mTOR and TBK1. Autophinib appears to be ATP-competitive, targets VPS34 in cell lysate and induces cellular phenotypes consistent with VPS34 inhibition. Autophinib inhibits the accumulation of autophagosomes under fed as well as starved conditions, but does not affect the number of autolysosomes. Thus it is not a late stage autophagy inhibitor but an inhibitor of autophagosome formation.

Cell lines: HeLa cellsConcentrations: 30 μMIncubation Time: 18 hMethod:

1644443-47-9

C14H11ClN6O3

346.73

H2O:<1 mgml
DMSO:64 mg/mL (184.6 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years