DAPT is a γ-secretase inhibitor (with IC50s of 115 and 200 nM for total Aβ and Aβ42, respectively) that can reduce Aβ40 and Aβ42 levels in human primary neuronal cells and brain extracts, DAPT also inhibits γ-secretase complex and indirectly inhibits Notch, a γ-secretase substrate (Dovey, et al). Its activity causes neural cells to commit to neuronal differentiation (Crawford et al). and has been shown to reduce colony-forming efficiency in mouse neural stem cells (Androutsellis-Theotokis et al). DAPT has also been shown to promote differentiation of pancreatic cells from human pluripotent stem cells (D’Amour et al).
| Molecular Name | GSI-IX; GSI IX, γ-Secretase Inhibitor IX, LY-374973 |
|---|---|
| Form | Powder |
| Chemical Name | N-[(3,5-Difluorophenyl)acetyl]-L-alanyl-2-phenyl]glycine-1,1-dimethylethyl ester |
| Chemical Formula | C₂₃H₂₆F₂N₂O₄ |
| Molecular Weight | 432.46 |
| CAS Number | 208255-80-5 |
| PubChem ID | 5311272 |
| Purity | ≥95% by NMR |
| Physical Appearance | White to off-white (Solid) |
| Target | γ-secretase; Autophagy |
| Shelf-Life | ≥ 2 years (Solid) |
| Shipping | Room Temperature |
| Storage | Store at -20°C |
| Quality Statement | This product is for Research Use Only and is not intended for therapeutic or diagnostic use. |
References and Publications
- Feng, J., (2019) DAPT, a γ-Secretase Inhibitor, Suppresses Tumorigenesis, and Progression of Growth Hormone-Producing Adenomas by Targeting Notch Signaling. Front. Oncol.
- Crawford, T.Q., et al. (2007) The notch response inhibitor DAPT enhances neuronal differentiation in embryonic stem cell-derived embryoid bodies independently of sonic hedgehog signaling. Dev Dyn 236: 886-892.
- D’Amour, K.A., et al. (2006) Production of pancreatic hormone-expressing endocrine cells from human embryonic stem cells. Nat Biotechnol 24: 1392-1401.
- Androutsellis-Theotokis, A., et al. (2006) Notch signaling regulates stem cell numbers in vitro and in vivo. Nature 442: 823-826.
- Dovey, H.F., et al. (2001) Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. J Neurochem 76: 173-181.
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