DAPT is a potent and specific inhibitor of γ-secretase. It has been shown to cause a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Aβ40 and Aβ42 respectively). There is evidence that DAPT does not effect APPα and APPβ levels. It mimics notch signaling deficiencies at morphological, molecular and biochemical levels and has been shown to block notch signaling in hybrid human-mouse foetal thymus organ culture (FTOC).
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2. Geling, Andrea., et al., 2002. A gamma-secretase inhibitor blocks Notch signaling in vivo and causes a severe neurogenic phenotype in zebrafish. EMBO reports. 3(7): 688-94. PMID: 12101103
3. Lanz, Thomas A., et al., 2003. The gamma-secretase inhibitor N-[N-(3,5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester reduces A beta levels in vivo in plasma and cerebrospinal fluid in young (plaque-free) and aged (plaque-bearing) Tg2576 mice. The Journal of pharmacology and experimental therapeutics. 305(3): 864-71. PMID: 12626636
4. Gowrishankar, Kavitha., et al., 2004. Release of a membrane-bound death domain by gamma-secretase processing of the p75NTR homolog NRADD. Journal of cell science. 117(Pt 18): 4099-111. PMID: 15280425
5. De Smedt, Magda., et al., 2005. Different thresholds of Notch signaling bias human precursor cells toward B-, NK-, monocytic/dendritic-, or T-cell lineage in thymus microenvironment. Blood. 106(10): 3498-506. PMID: 16030192
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See how others have used DAPT. Click on the entry to view the PubMed entry .
PMID: # 30839137 Niu, Y. et al. 2019. Cell Biol. Int.
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