PIK-III

PIK-III (VPS34-IN2), 一种选择性VPS34酶活性的抑制剂，抑制细胞自噬以及LC3的重新脂化，稳定自噬底物。其对VPS34和 PI(3)Kδ的IC50值分别为0.018 μM和1.2 μM。 Information PIK-III (VPS34-IN2), which is a selective inhibitor of ​VPS34 enzymatic activity, inhibitsautophagyand de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively. Targets Vps34 (Cell-free assay); PI3Kδ (Cell-free assay) 0.018μM; 1.2μM In vitro VPS34 enzymatic function is essential for LC3 lipidation in mammalian cells and PIK-III is a robust inhibitor of autophagy and LC3 lipidation in mammalian cells.In H4 cells, PIK-III inhibits the formation of autolysosomes and increases the cytosolic signal of LC3 under basal conditions and when autophagy is induced with the mTOR inhibitor AZD8055.In a CCCP-induced mitophagy model, PIK-III inhibits the clearance of mitochondria.PIK-III treatment leads to an increase in the levels of LC3-I in H4 and PSN1 cells.In Panc10.05 cells, PIK-III increases the levels of LC3-II in parallel with LC3-I suggesting a cell type-specific response. Cell Research(from reference) Cell lines：H4 cells/ HeLa cells Concentrations：2.5μM in H4 cells/5μM in Hela cells Incubation Time：overnight for H4 cells/12h for Hela cells

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