Name | PI3KC2α-IN-1 |
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Description | PI3KC2α-IN-1 is a potent PI3KC2α inhibitor (IC50: 95 nM). PI3KC2α-IN-1 interacts with the ATP-binding site of PI3KC2α. PI3KC2α-IN-1 can be used in the research of thrombosis, diabetes and cancers[1]. |
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Related Catalog | |
Target |
PI3KC2α:95 nM (IC50) PI3KC2β:5700 nM (IC50) PI3KC2γ:860 nM (IC50) |
In Vitro | PI3KC2α-IN-1 (PITCOIN1, 30 nM-1 mM, HEK293T cell lysates) is highly selective in targeting PI3KC2α but no other human kinases (Kinobead profiling assay)[1]. PI3KC2α-IN-1 (100 μM, 20 h) shows no detectable cytotoxicity in HeLa cells[1]. PI3KC2α-IN-1 (6 h) blocks plasma membrane tubulation induced by eGFP–SNX9 in HeLa cells (EC50: 5 μM)[1]. PI3KC2α-IN-1 (20 μM, 6 h) results in impaired clathrin-mediated endocytosis of transferrin in Cos7 cells[1]. PI3KC2α-IN-1 (20 μM, 6 h) inhibits endosomal PI(3)P synthesis[1]. PI3KC2α-IN-1 (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). |
Molecular Formula | C19H16N6O2S2 |
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Molecular Weight | 424.50 |