DAPT (GSI-IX) 208255-80-5

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Molecular Weight:

432.46 DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.






Biological Activity


In human primary neuronal cultures, DAPT also shows inhibitory effects
on Aβ production with IC50 of 115 nM and 200 nM respectively for Aβ
total and Aβ42, which is 5-10-fold lower than is observed in HEK 293
cells.


A recent study shows that DAPT inhibits the
proliferation of SK-MES-1 cells in a concentration-dependent manner with
IC50 of 11.3 μM. In addition, DAPT also induces caspase-dependent and
caspase-independent Apoptosis in lung squamous cell carcinoma cells by
inhibiting Notch receptor signaling pathway.


DAPT administration (100mg/kg) leads to a robust and sustained
pharmacodynamic effect in PDAPP mice that DAPT levels in the brain
exceeds 100 ng/g within 1 hour and persists up to 18 hours after
administration, with peak levels of 490 ng/g observed after 3 hour.


And
during the period, DAPT (100 mg/kg) also reduces the cortical total Aβ
and Aβ42 in a dose-dependent manner with a 50% reduction. In rat cerebral cortexes, DAPT (40 mg/kg) suppresses the LPS-induced
activity of γ-secretase and increases the cell apoptosis with the
prolonged neuroinflammation.

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Product Categories : Proteases > Gamma-secretase Inhibitor