InSolution γ-Secretase Inhibitor X-Calbiochem

C₃₉H₅₂N₄O₆

672.85

A cell-permeable hydroxyethylene dipeptide isostere that acts as a potent and highly specific inhibitor of γ-secretase (Aβ total IC₅₀ = 17 nM; Aβ₄₀ IC₅₀ = 48 nM; and Aβ₄₂ IC₅₀ = 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_total IC₅₀ = 17 nM, Aβ₄₀ IC₅₀ = 48 nM, and Aβ₄₂ IC₅₀ = 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.

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

Toxicity: Standard Handling (A)

A 1 mM (250 µg in 372 µl or 500 µg in 744 µl) solution in DMSO.

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

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.

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

100

≥90% (HPLC)

liquid

Calbiochem^®

OK to freeze
desiccated
protect from light

ambient

−20℃

250, 500 μg in Plastic ampoule
Packaged under inert gas

10 - Combustible liquids

WGK 1

188.6 °F - (Dimethylsulfoxide)

87 ℃ - (Dimethylsulfoxide)