Autophinib

Autophinib is a potent, selective autophagy inhibitor with IC₅₀s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC₅₀ of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34^[1]. IC50 & Target: IC50: 19 nM (VPS34), 40 nM (Rapamycin-induced autophagy), 90 nM (starvation-induced autophagy)^[1] In Vitro: Autophinib (0.01-1 μM) inhibits LC3 lipidation to form LC3-II in a dose-dependent manner in starved MCF7-LC3 cells. Consistent with inhibition of autophagic flux, Autophinib also inhibits p62 degradation by autophagy dose-dependently in MCF7-LC3 cells^[1].
Autophinib enhances cell death (EC₅₀ of 264 nM) of starved cells as compared to fed cells, which occurred via the induction of apoptosis (EC₅₀ of 234 nM) in MCF7 cells^[1].