565771

γ-Secretase Inhibitor X

≥90% (HPLC), liquid, γ-secretase inhibitor, Calbiochem^®

• Sinônimo(s): InSolution γ-Secretase Inhibitor X, L-685,458, {1S-Benzyl-4R-[1-(1S-carbamoyl-2-phenethylcarbamoyl)-1S-3-methylbutylcarbamoyl]-2R-hydroxy-5-phenylpentyl}carbamic Acid tert-butyl Ester
• Fórmula empírica (Notação de Hill): C₃₉H₅₂N₄O₆
• Peso molecular: 672.85
• Código UNSPSC: 12352200
• NACRES: NA.54

Propriedades

• product name: γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM
• Nível de qualidade: 100
• Ensaio: ≥90% (HPLC)
• forma: liquid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated; protect from light
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

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.

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
Aβ_total

Product does not compete with ATP.

Reversible: no

Target IC₅₀: Aβtotal 17 nM, Aβ40 48 nM, and Aβ42 67 nM in SHSY5Y cells overexpressing spβA4CTF

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

forma física

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

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 10 - Combustible liquids
• Classe de risco de água (WGK): WGK 1
• Ponto de fulgor (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Ponto de fulgor (°C): 87 °C - closed cup - (Dimethylsulfoxide)