PI3KC2α-IN-3

PI3KC2α-IN-3 is a potent and highly selective PI3KC2α inhibitor (IC50: 126 nM). PI3KC2α-IN-3 interacts with the ATP-binding site of PI3KC2α. PI3KC2α-IN-3 impairs endocytic membrane dynamics and membrane remodeling. PI3KC2α-IN-3 can be used in the research of thrombosis, diabetes and cancers[1].

Research Areas >> Cancer

Research Areas >> Cardiovascular Disease

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

Research Areas >> Metabolic Disease

PI3KC2α:126 nM (IC50)

PI3KC2β:>10 μM (IC50)

PI3KC2γ:>10 μM (IC50)

PI3KC2α-IN-3 (PITCOIN3, 30 nM-1 mM, HEK293T cell lysates) is highly selective in targeting PI3KC2α but no other human kinases (Kinobead profiling assay)[1]. PI3KC2α-IN-3 (100 μM, 20 h) shows no detectable cytotoxicity in HeLa cells[1]. PI3KC2α-IN-3 (6 h) blocks plasma membrane tubulation induced by eGFP–SNX9 in HeLa cells (EC50: 4.6 μM)[1]. PI3KC2α-IN-3 (20 μM, 6 h) results in impaired clathrin-mediated endocytosis of transferrin in Cos7 cells[1]. PI3KC2α-IN-3 (20 μM, 6 h) inhibits endosomal PI(3)P synthesis[1]. PI3KC2α-IN-3 (20 μM, 6 h) impairs platelet membrane and thrombus formation in mouse resting platelets[1]. Cell Viability Assay[1] Cell Line: Cos7 cells Concentration: 20 μM Incubation Time: 6 h Result: Reduced endosomal PI(3)P, and reduced endosomal membrane recruitment of the PI(3)P-binding effector early endosomal antigen 1 (EEA1).