565771

γ-Secretase Inhibitor X

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

• 동의어(들): 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
• 실험식(Hill 표기법): C₃₉H₅₂N₄O₆
• Molecular Weight: 672.85
• UNSPSC 코드: 12352200
• NACRES: NA.54

속성

• product name: γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM
• Quality Level: 100
• 분석: ≥90% (HPLC)
• 형태: liquid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; desiccated; protect from light
• 배송 상태: ambient
• 저장 온도: −20°C

설명

일반 설명

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.

생화학적/생리학적 작용

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

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

물리적 형태

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

재구성

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

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 1
• Flash Point (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Flash Point (°C): 87 °C - closed cup - (Dimethylsulfoxide)