Biological Activity
Inhibitor of γ-secretase; causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Aβ and Aβ42 respectively) and in brain extract, cerebrospinal fluid and plasma in vivo. Does not affect APPα and APPβ levels. Blocks Notch signaling in hybrid human-mouse fetal thymus organ culture (FTOC). Activity causes ESCs to commit to neuronal differentiation.
Compound Libraries
DAPT is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 432.46 |
| Formula | C23H26F2N2O4 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 208255-80-5 |
| PubChem ID | 5311272 |
| InChI Key | DWJXYEABWRJFSP-XOBRGWDASA-N |
| Smiles | CC(C)(C)OC([C@H]([C@]2=CC=CC=C2)NC([C@H](C)NC(CC1=CC(F)=CC(F)=C1)=O)=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.24 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 432.46. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.31 mL | 11.56 mL | 23.12 mL |
| 5 mM | 0.46 mL | 2.31 mL | 4.62 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.31 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Dovey et al (2001) Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. J.Neurochem. 76 173 PMID: 11145990
De Smedt et al (2005) Different thresholds of notch signaling bias human precursor cells towards B-, NK-, monocytic/dendritic, or T-cell lineage in thymus microenvironment. Blood 106 3498 PMID: 16030192
Crawford and Roelink (2007) The notch response inhibitor DAPT enhances neuronal differentiation in embryonic stem cell-derived embryoid bodies independently of sonic hedgehog signaling. Dev.Dyn. 236 886 PMID: 17295317
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