1644443-47-9

Autophinib is a potent VPS34 inhibitor (IC50 = 19 nM). Inhibits starvation- and Rapamycin-induced autophagy (IC50 values = 40 and 90 nM, respectively).

Autophinib is an ATP-competitivepotent and selective PI3K type 3 lipid kinase vacuolar protein sorting 34 inhibitor (VPS34 IC50/[ATP] = 19 nM/10 μM & 51 nM/100 μM) th at shows significant inhibition against only 45 kinases among a panel of >460 with little or no potency toward mTORTBK1 and 12 other phosphatidylinositol kinases (=22% inhibition at 1 μM). Autophinib effectively prevents autophagy induction in MCF7 cells upon amino acid starvation or rapamycin treatment (IC50 = 40 nM and 19 nMrespectively) with similar potency as SAR405 (IC50 = 53 nM and 20 nMrespectively) and VPS34-IN1 (IC50 = 13 nM and 15 nMrespectively). Autophinib enhances MCF7 cell death under starvation condition (EC50 = 264 nM and 234 nM by cytotoxiciy and apoptosis detectionrespectively) by preventing autophagy-dependent cell survival.

Vps34: 19 nM (IC₅₀)

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