Merck, 565784-10MG, γ-Secretase Inhibitor IX

General description
A cell-permeable dipeptide that inhibits γ-secretase activity and suppresses Aβ production (Aβ total IC₅₀ = 115 nM; Aβ₄₂ IC₅₀ = 200 nM). Reported to be functionally active in both HEK293 cells overexpressing human APP751 and neuronal cultures, however, it does not affect the secretion of amyloid-b precursor protein (APP). Effective in acutely lowering Ab in APPV717F-transgenic mice. Also effective in inhibiting the production of a ~6 kDa C-terminal cleavage product (CTFg) in HEK293 cells stably transfected with the Swedish mutant, βAPP₆₉₅. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice.
Biochem/physiol Actions
Primary Target
Aβtotal
Target IC₅₀: 115 nM, 200 nM against Aβtotal, Aβ42, respectively
Physical form
A 25 mM (5 mg/462 µl or 10 mg/924 µl) solution of γ-Secretase Inhibitor IX (Cat. No. 565770) in DMSO.
Preparation Note
Following initial use, aliquot and freeze (-20°C).
Other Notes
Oddo, S., et al. 2004. Neuron43, 321.
Dovey, H.F., et al. 2001. J. Neurochem.76, 173.
Vandermeeren, M., et al. 2001. Neurosci. Lett.315, 145.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)