Autophinib

Description: Autophinib is a novel and potent autophagy inhibitor, which inhibits starvation-induced or rapamyc induced autophagy. It acts by targeting the lipid kinase VPS34 with IC50 values of 90, 40 and 19 nM, respectively. Autophagy is a critical regulator of cellular homeostasis and metabolism. Interference with this process is considered a new approach for the treatment of disease, in particular cancer and neurological disorders. Therefore, novel small-molecule autophagy modulators such as autophinib are in high demand. Autophinib was identified by means of a phenotypic assay monitoring the formation of autophagy-induced puncta, indicating accumulation of the lipidated cytosolic protein LC3 on the autophagosomal membrane. Target identification and validation revealed that autophinib inhibits autophagy induced by starvation or rapamycin by targeting the lipid kinase VPS34.

References: Angew Chem Int Ed Engl. 2017 Jul 3; 56(28):8153-8157.