PITCOIN3 (HB-05-160) is a potent, highly selective, cell-permeable inhibitor of PI3KC2α catalytic activity with IC50 of 126 nM.
PITCOIN3 displays high selectivity over other PI3Ks and to PI3K-like protein kinases such as mTOR.
PITCOIN3 impair PI(3,4)P2 synthesis and endocytosis in HeLa cells, dose-dependently blocks plasma membrane tubule formation induced by constitutively active enhanced green fluorescent protein (eGFP)-SNX9 with EC50 of 4.6 uM.
PITCOIN3 is nontoxic for in a variety of different cell types, for example, Cos7, HEK293 and HepG2 cells, also has no effect on the Golgi pool of PI(4)P, which is mainly synthesized by PI 4 kinase IIIβ.
Pharmacological blockade of PI3KC2α by PITCOIN3 (20 uM for 6 h) reduces endosomal PI(3)P levels in Cos7 cells.|
PITCOIN3 (20 uM for 6 h) impairs platelet membrane remodeling and thrombus formation in mouse resting platelets, causes a pronounced and highly significant reduction in the prothrombotic capacity of platelets, displays antithrombotic activity in mouse blood.