516485

Pepstatin A Methyl Ester

A cell-permeable methyl ester derivative of Pepstatin A that acts as a potent, non-competitive, transition-state analog inhibitor of γ-secretase.

• Synonym(s): Pepstatin A Methyl Ester, Isovaleryl-V V-Sta-A-Sta-OCH₃, PME
• Empirical Formula (Hill Notation): C₃₅H₆₅N₅O₉
• Molecular Weight: 699.92
• UNSPSC Code: 12352108
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: lyophilized
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• solubility: DMSO: 5 mg/mL
• shipped in: wet ice
• storage temp.: −20°C

Description

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 (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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
γ-secretase

Product does not compete with ATP.

Reversible: no

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

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.

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable