Description
FIPI, a derivative of halopemide, is a potent and selective phospholipase D (PLD) inhibitor with IC50 values of 20 and 25 nM for PLD2 and PLD1 respectively. It attenuate mercury-induced lipid signaling leading to protection against cytotoxicity in aortic endothelial cells. It rapidly blocks in vivo PA production with subnanomolar potency. It has good pharmacokinetic parameters in rats. It did not significantly inhibit p38 or ERK phosphorylation in bone marrow-derived macrophages stimulated with lipopolysaccharide. It prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis