DAPT (GSI-IX)

InformationDAPT (GSI-IX, LY-374973) is a novelγ-secretaseinhibitor, which inhibits Aβ production withIC50of 20 nM in HEK 293 cells. DAPT enhances theapoptosisof human tongue carcinoma cells and regulatesautophagy.In vitroIn 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.In vivoDAPT 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.Cell Datacell lines：Concentrations：2.5 μM to 160 μMIncubation Time：72 hoursPowder Purity:≥98%.

Specifications and Purity: 10mM in DMSO

Molecular Formula: C23H26F2N2O4

Molecular Weight: 432.46