565771

γ-Secretase Inhibitor X

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

• 别名: 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
• 经验公式（希尔记法）: C₃₉H₅₂N₄O₆
• 分子量: 672.85
• 分類程式碼代碼: 12352200
• NACRES: NA.54

属性

• product name: γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM
• 品質等級: 100
• 化驗: ≥90% (HPLC)
• 形狀: liquid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; desiccated; protect from light
• 運輸包裝: ambient
• 儲存溫度: −20°C

说明

一般說明

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.

生化／生理作用

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

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

外觀

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

重構

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

其他說明

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.

法律資訊

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

安全信息

• 儲存類別代碼: 10 - Combustible liquids
• 水污染物質分類（WGK）: WGK 1
• 閃點（°F）: 188.6 °F - closed cup - (Dimethylsulfoxide)
• 閃點（°C）: 87 °C - closed cup - (Dimethylsulfoxide)