γ₄₀-Secretase Inhibitor I

A potent, cell-permeable, reversible γ-secretase inhibitor that preferentially appears to inhibit the secretion of Aβ_1-40 (>90%) over Aβ_1-42 (~15%). Aβ_total IC₅₀ ~ 15 M; Aβ_1-40 IC₅₀ ~ 22 M; Aβ_1-42 IC₅₀ >50 M in CHO cells stable transfected with the cDNA encoding βAPP695.

A potent, cell-permeable, reversible inhibitor of γ-secretase that is reported to preferentially inhibit the secretion of Aβ_1-40 (>90%) vs. Aβ_1-42. IC₅₀ = ~15 µM for Aβ_total; ~22 µM for Aβ_1-40; and >50 µM for Aβ_1-42 in CHO cells stably transfected with the cDNA encoding βAPP695. Reported to be about 10-fold more potent than Z-Val-Phe-CHO [MDL 28170 (Cat. No. 208722)].

Cell permeable: yes

Primary Target
secretion of Aβ₁₋₄₀

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: ~ 15 µM for Aβtotal; ~ 22 µM for Aβ1-40; <50 µM for Aβ1-42 in CHO cells stable transfected with the cDNA encoding βAPP695

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Higaki, J.N., et al. 1999. J. Med. Chem. 42, 3889.

trans-3,5-DMC-Ile-Leu-CHO (DMC = Dimethoxycinnamoyl)

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

Toxicity: Standard Handling (A)