Amastatin hydrochloride hydrate 

Amastatin is a slow, tight-binding inhibitor of aminopeptidases. It inhibits cytosolic leucine aminopeptidase (EC.3.4.11.1), microsomal aminopeptidase M (EC.3.4.11.2) and bacterial leucine aminopeptidase (EC.3.4.11.10). It is less effective against aminopeptidase A (EC 3.4.11.7), the enzyme that converts Angiotensin II to Angiotensin III. Effective concentration: 1-10 μM.

≥97% (HPLC)

methanol: 1 mM Stock solution stable for 1 month at −20 °C. Working solution stable for 1 day.

−20°C

, Zollner, H. Handbook of Enzyme Inhibitors 2nd ed.,, (1993) 2nd Ed., 547

Ahmad, S., and Ward, P.E. , Role of aminopeptidase activity in the regulation of the pressor activity of circulating angiotensins. J. Pharmacol. Exp. Ther. 252, 643-650, (1990)

Wilkes, S.H., and Prescott, J.M., The slow, tight binding of bestatin and amastatin to aminopeptidases. J. Biol. Chem. 260, 13154-13162, (1985)

, Beynon, R.J. and Bond, J.S. Proteolytic Enzymes: A Practical Approach New York, NY , (1989), 247

Kim, H., and Lipscomb, W.N., X-ray crystallographic determination of the structure of bovine lens leucine aminopeptidase complexed with amastatin: formulation of a catalytic mechanism featuring a gem-diolate transition state. Biochemistry 32, 8465-8478, (1993)

3