565771

γ-Secretase Inhibitor X

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

• Synonym(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
• Empirical Formula (Hill Notation): C₃₉H₅₂N₄O₆
• Molecular Weight: 672.85
• UNSPSC Code: 12352200
• NACRES: NA.54
• Assay: ≥90% (HPLC)
• Form: liquid
• Storage condition: OK to freeze, desiccated, protect from light

Properties

• Product Name: γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM
• Quality Segment: 100
• assay: ≥90% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, desiccated, protect from light
• shipped in: ambient
• storage temp.: −20°C

Description

General description

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Physical form

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

Preparation Note

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

Other Notes

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

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