565771

γ-Secretase Inhibitor X

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

• 別名: 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
• 実験式（ヒル表記法）: C₃₉H₅₂N₄O₆
• 分子量: 672.85
• UNSPSCコード: 12352200
• NACRES: NA.54

特性

• 製品名: γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM
• 品質水準: 100
• アッセイ: ≥90% (HPLC)
• フォーム: liquid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated; protect from light
• 輸送温度: ambient
• 保管温度: −20°C

詳細

詳細

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.

生物化学的／生理学的作用

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

物理的形状

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

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 10 - Combustible liquids
• WGK: WGK 1
• 引火点(°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• 引火点(℃): 87 °C - closed cup - (Dimethylsulfoxide)