Pepstatin A Methyl Ester

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 (K_is = 150 nM, K_ii = 320 nM in solubilized human γ-secretase at 20°C; K_is is the inhibition constant for inhibitor binding to the free enzyme and K_ii is the inhibition constant for inhibitor binding to the Enzyme-Substrate complex). Sta = (3S,4S)-4-Amino-3-hydroxy-6-methyl-heptanoic acid.

A cell-permeable methyl ester derivative of Pepstatin A (Cat. No. 516482) that acts as a potent, non-competitive, transition-state analog inhibitor of γ-secretase (K_is = 15 nM and K_ii = 32 nM in solubilized human γ-secretase; K_is is the inhibition constant for inhibitor binding to the free enzyme and K_ii is the inhibition constant for inhibitor binding to the Enzyme-Substrate complex).

Cell permeable: yes

Primary Target
γ-secretase

Product does not compete with ATP.

Reversible: no

Packaged under inert gas

Toxicity: Standard Handling (A)

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.

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.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany