565771

γ-Secretase Inhibitor X

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

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₃₉H₅₂N₄O₆
• Masa cząsteczkowa: 672.85
• Kod UNSPSC: 12352200
• NACRES: NA.54

Właściwości

• Nazwa produktu: γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM
• Poziom jakości: 100
• Próba: ≥90% (HPLC)
• Formularz: liquid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated; protect from light
• Warunki transportu: ambient
• temp. przechowywania: −20°C

Opis

Opis ogólny

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.

Działania biochem./fizjol.

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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Postać fizyczna

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

Rekonstytucja

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

Inne uwagi

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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 10 - Combustible liquids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Temperatura zapłonu (°C): 87 °C - closed cup - (Dimethylsulfoxide)