Chemical Name:7-Amino-4-chloro-3-methoxy-1H-2-benzopyran
Biological Activity:
Inhibitor of γ-secretase
that selectively inhibits βAPP
cleavage without affecting other γ-secretase-mediated
pathways. Prevents recovery of Aβ40
and Aβ42 from HEK293 cell overexpressing wild-type or Swedish-mutated βAPP
(IC50 ~ 30 μM) but displays no
effect on Notch cleavage and Notch-mediated intracellular signalling. Displays
no activity on BACE1, BACE2, α-secretase,
the proteosome or GSK3β.
Petitet
al (2001) New protease inhibitors prevent γ-secretase-mediated
production of Aβ40/42 without affecting Notch cleavage. Nat.Cell.Biol. 3
507. Petitet al (2003) JLK isocoumarin inhibitors: selective γ-secretase
inhibitors that do not interfere with Notch pathway in vitro or in vivo.
J.Neurosci.Res. 74 370. Hellstromet al (2007) DII4
signalling through Notch1 regulates formation of tip cells during angiogenesis.
Nature 445 776.