Bestatin

Bestatin is an aminopeptidase inhibitor originally isolated from S. olivoreticuli. It 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). It is selective for these aminopeptidases over aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, and thermolysin. Bestatin inhibits the production of LTB4 (Cay-20110) in erythrocytes when used at a concentration of 70 µM. It increases the expression of Akt, inhibits proliferation, migration, and invasion, and induces autophagy and apoptosis in 5637 bladder cancer cells. Bestatin (5 and 15 mg/kg) decreases serum levels of LTB4 and reduces tumor growth in a patient-derived xenograft (PDX) mouse model of colorectal cancer.Formal Name: N-[(2S,3R)-3-amino-2-hydroxy-1-oxo-4-phenylbutyl]-L-leucine. CAS Number: 58970-76-6. Synonyms: NK 421, NSC 265489. Molecular Formula: C16H24N2O4. Formula Weight: 308.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: PBS (pH 7.2): 0.16 mg/mL. SMILES: CC(C)C[C@@H](C(O)=O)N([H])C([C@@H](O)[C@H](N)CC1=CC=CC=C1)=O. InChi Code: InChI=1S/C16H24N2O4/c1-10(2)8-13(16(21)22)18-15(20)14(19)12(17)9-11-6-4-3-5-7-11/h3-7,10,12-14,19H,8-9,17H2,1-2H3,(H,18,20)(H,21,22)/t12-,13?,14+/m1/s1. InChi Key: VGGGPCQERPFHOB-YIOYIWSBSA-N. Origin: Synthetic.