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DAPT

(CAS No:208255-80-5)
DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.
CAS No:208255-80-5
Molecular Weight(MW):432.46
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 208255-80-5
Molecular formula(MF) C23H26F2N2O4
Molecular Weight(MW): 432.46
Alias
Solubility
In vitro DMSO 86 mg/mL (198.86 mM)
Ethanol 50 mg/mL (115.61 mM)
Water <1 mg/mL
In vivo 4% DMSO+corn oil 10mg/mL
Biological Activity
Description DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.
Targets
γ secretase(Aβ) [1]
(HEK 293 cells)
20 nM
In vitro

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. [1] 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. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 CD133− Growth Inhibition Assay 2 μM 48 h enhances cell growth inhibition induced by CDDP 24502949
A549 CD133+ Growth Inhibition Assay 2 μM 48 h enhances cell growth inhibition induced by CDDP 24502949
HT29  Growth Inhibition Assay 0.5-75 μM 12/24/48 h DMSO inhibits the cell growth in a concentration manner 25257945
SHG-44 Growth Inhibition Assay 0.5-10 μM 1-5 d inhibits the cell viability at the optimal concentration of 1 μM 25063285
MG63 Function Assay 100 μM 24 h DMSO desensitizes the cell line to cisplatin treatment 24894297
Saos-2 Function Assay 100 μM 24 h DMSO desensitizes the cell line to cisplatin treatment 24894297
U251 Growth Inhibition Assay 2 μM 48 h DMSO strengthens t-AUCB-induced cell growth suppression 24793313
U87  Growth Inhibition Assay 2 μM 48 h DMSO strengthens t-AUCB-induced cell growth suppression 24793313
U251 Function Assay 2 μM 48 h DMSO blocks t-AUCB-induced activation of the p38 MAPK/MAPKAPK2/Hsp27 pathway and inhibits expression of NICD1 24793313
U87  Function Assay 2 μM 48 h DMSO blocks t-AUCB-induced activation of the p38 MAPK/MAPKAPK2/Hsp27 pathway and inhibits expression of NICD1 24793313
A549  Growth Inhibition Assay 10 μM 24h decreases the cell viability combined with PTE 23671619
GC-B  Growth Inhibition Assay 6.25-100 μM 24 h DMSO inhibits the cell growth in a dose-dependent manner 19542446

... Click to View More Cell Line Experimental Data

In vivo 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. [1] 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. [3]