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Description

A cell-permeable dipeptide that inhibits gamma-secretase activity and suppresses Abeta production (Abeta total IC50 = 115 nM, Abeta42 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 an ~6 kDa C-terminal cleavage product (CTFg) in HEK293 cells stably transfected with the Swedish mutant, betaAPP695. Reported to reduce extracellular Abeta plaques and intracellular Abeta accumulation in 3xTgAD transgenic mice., A cell-permeable dipeptide that suppresses Abeta production by blocking gamma-secretase (Abetatotal IC50 = 115 nM, Abeta42 IC50 = 200 nM). Prevents Abeta34 generation in murine N2a cells and hAPP/hBACE-1 transfected human HEK 293 cells. Reported to be functionally active in both HEK 293 cells and neuronal cultures without affecting the secretion of amyloid-beta precursor protein (APP). Also shown to lower Abeta levels acutely in APP-transgenic mice. Reported to reduce extracellular Abeta plaques and intracellular Abeta accumulation in 3xTgAD transgenic mice. A 25 mM (5 mg/462 µ,l) solution of gamma-Secretase Inhibitor IX (Cat. No. 565784) in DMSO is also available.