Bestatin

An aminopeptidase inhibitor; inhibits aminopeptidase B (IC50 = 0.05 µg/ml), aminopeptidase N (IC50 = 16.9 µM), leucine aminopeptidase (IC50 = 0.01 µg/ml), and the aminopeptidase activity of leukotriene A4 (LTA4) hydrolase (Kapp = 172 nM); selective for these aminopeptidases over aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, and thermolysin; inhibits LTB4 production in erythrocytes at 70 µM; increases the expression of Akt, inhibits proliferation, migration, and invasion, and induces autophagy and apoptosis in 5637 bladder cancer cells; decreases serum levels of LTB4 and reduces tumor growth in a PDX mouse model of colorectal cancer at 5 and 15 mg/kg