InSolution γ-Secretase Inhibitor X-Calbiochem

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一般描述

A cell-permeable hydroxyethylene dipeptide isostere that acts as a potent and highly specific inhibitor of γ-secretase (Aβ total IC₅₀= 17 nM; Aβ₄₀IC₅₀= 48 nM; and Aβ₄₂IC₅₀= 67 nM in SH-SY5Y cells overexpressing spβA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Also reported to block the formation of εCTF, resulting in the accumulation of α- and βCTF. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease, however, it exhibits over 100-fold greater selectivity for γ-secretase than for cathepsin D.
A cell-permeable hydroxyethylene dipeptide isostere that acts as a highly specific and a potent inhibitor of γ-secretase (Aβ_totalIC₅₀= 17 nM, Aβ₄₀IC₅₀= 48 nM, and Aβ₄₂IC₅₀= 67 nM in SHSY5Y cells overexpressing spβA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease, however, it exhibits over 100-fold greater selectivity for γ-secretase than for cathepsin D.

包装

250, 500 μg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Product does not compete with ATP.
Cell permeable: yes
Target IC₅₀: Aβtotal 17 nM, Aβ40 48 nM, and Aβ42 67 nM in SHSY5Y cells overexpressing spβA4CTF
Reversible: no
Primary Target
Aβ_total

警告

Toxicity: Standard Handling (A)

外形

A 1 mM (250 ?g in 372 ?l or 500 ?g in 744 ?l) solution in DMSO.

重悬

Following initial thaw, aliquot and freeze (-20°C).

其他说明

Weidemann, A., et al. 2002.Biochemistry41,2825.
Doerfler, P., et al. 2001.Proc. Natl. Acad. Sci. USA98,9312.
Li, Y.M., et al. 2000.Proc. Natl. Acad. Sci. USA97,6138.
Shearman, M.S., et al. 2000.Biochemistry39,8698.

法律信息

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

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