Merck, 516485-1MG, Pepstatin A Methyl Ester

General description
A cell-permeable methyl ester derivative of Pepstatin A (Cat. No. 516481) that acts as a potent, non-competitive, transition-state analog inhibitor of γ-secretase (Kis = 150 nM, Kii = 320 nM in solubilized human γ-secretase at 20°C; Kis is the inhibition constant for inhibitor binding to the free enzyme and Kii is the inhibition constant for inhibitor binding to the Enzyme-Substrate complex). Sta = (3S,4S)-4-Amino-3-hydroxy-6-methyl-heptanoic acid.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
γ-secretase
Product does not compete with ATP.
Reversible: no
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Avoid freeze/thaw cycles of solutions.
Other Notes
Tian, G., et al. 2002. J. Biol. Chem.277, 31499.
Zhang, L., et al. 2001. Biochemistry40, 5049.
Murphy, M.P., et al. 1999. J. Biol. Chem.274, 11914.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)