Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Primary Targetγ-secretase

Cell permeable: yes

General description

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).

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.

Legal Information

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

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.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

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.

Warning

Toxicity: Standard Handling (A)