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PI3KC2α-IN-3 is a highly selective and potent PI3KC2α inhibitor with an IC50 value of 126 nM. PI3KC2α-IN-3 interacts with the ATP binding site of PI3KC2α and impairs endocytic membrane kinetics and membrane remodelling. PI3KC2α-IN-3 can be used to study thrombosis, diabetes and cancer.