Inhibitor of γ -secretase that selectively inhibits β APP cleavage without affecting other γ -secretase-mediated pathways. Prevents recovery of A β 40 and A β 42 from HEK293 cell overexpressing wild-type or Swedish-mutated β APP (IC 50 ~ 30 μ M) but displays no effect on Notch cleavage and Notch-mediated intracellular signaling. Displays no activity on BACE1, BACE2, α -secretase, the proteosome or GSK3 β .
[1]. petit a, pasini a, alves da costa c, et al. jlk isocoumarin inhibitors: selective γ-secretase inhibitors that do not interfere with notch pathway in vitro or in vivo. journal of neuroscience research, 2003, 74(3): 370-377.
[2]. petit a, bihel f, da costa ca, et al. new protease inhibitors prevent γ-secretase-mediated production of aβ40/42 without affecting notch cleavage. nature cell biology, 2001, 3(5): 507-511.
