Merck, 565755-1MG, γ-Secretase Inhibitor II

General description
A cell-permeable, reversible and selective peptidomimetic inhibitor of γ-secretase with an IC₅₀ of 13 µM for the inhibition of amyloid β-protein (Aβ) production in β-amyloid precursor protein (APP)-transfected Chinese hamster ovary cells. Displays only weak inhibitory activity against calpain II (IC₅₀ = 100 µM in a purified enzyme assay).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
γ-secretase
Product does not compete with ATP.
Reversible: yes
Target IC₅₀: 13 µM against γ-secretase
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Wolfe, M.S., et al. 1999. Biochemistry38, 4720.
Wolfe, M.S., et al. 1998. J. Med. Chem. 41, 6.
Citron, M., et al. 1996. Proc. Natl. Acad. Sci. USA93, 13170.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)