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Beschreibung

A cell-permeable, reversible dipeptide aldehyde that reduces amyloid-beta protein (Abeta) production by blocking gamma-secretase activity in vitro (Abeta40 IC50 = 7.9 µ,M, Abeta42 IC50 = 7.6 µ,M) and in cultured cells that stably over-express APP695 (Abeta40 IC50 = 11.5 µ,M, Abeta42 IC50 = 8.3 µ,M). Also shown to block the generation of gammaCTF (gamma-secretase-generated carboxy-terminal fragment)., A cell-permeable, reversible dipeptide aldehyde that reduces Abeta production by blocking gamma-secretase activity in vitro (Abeta40 IC50 = 7.9 µ,M, Abeta42 IC50 = 7.6 µ,M) and in cultured CHO 2b-7 cells that stably overexpress APP695 (Abeta40 IC50 = 11.5 µ,M, Abeta42 IC50 = 8.3 µ,M). Also blocks the generation of CTFgamma (gamma-secretase-generated carboxyl-terminal fragment). Does not affect the formation of amyloid-beta-precursor protein (APP).