DAPT (N-S-phenylglycine tert.butyl ester)

Cell permeable gamma-secretase inhibitor (IC50 = 115 nM for total beta-amyloid, IC50 = 200 nM for beta-amyloid 1-42). Reduces Abeta levels in vivo. Blocks the proteolytic processing of neurotrophin receptor alike death domain protein (NRADD). Does not inhibit persenilinase. Notch processing inhibitor. Enhances neuronal differentiation independent of sonic hedgehog (Shh) signaling. CDK5 activity inhibitor. Apoptosis enhancer.\n\nStorage and Stability:\nShort-term Storage: +4 degrees C\nLong-term Storage: -20 degrees C\nStable for at least 2 years after receipt when stored at -20 degrees C.

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SPECIFICATIONS

Catalog Number

044723

Size

5mg

Purity

>98% (NMR)

References

Product Reference: \n?Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain: H.F. Dovey, et al.; J. Neurochem. 76, 173 (2001) \n?The gamma-secretase inhibitor N--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: T.A. Lanz, et al.; J. Pharmacol. Exp. Ther. 305, 864 (2003) \n?Release of a membrane-bound death domain by gamma-secretase processing of the p75NTR homolog NRADD: K. Gowrishankar, et al.; J. Cell. Sci. 117, 4099 (2004) \n?Presenilin endoproteolysis mediated by an aspartyl protease activity pharmacologically distinct from gamma-secretase: W.A. Campbell, et al.; J. Neurochem. 85, 1563 (2003) \n?A gamma-secretase inhibitor blocks Notch signaling in vivo and causes a severe neurogenic phenotype in zebrafish: A. Geling, et al.; EMBO Rep. 3, 688 (2002) \n?The notch response inhibitor DAPT enhances neuronal differentiation in embryonic stem cell-derived embryoid bodies independently of sonic hedgehog signaling: T.Q. Crawford & H. Roelink; Dev. Dyn. 236, 886 (2007) \n?The Notch signaling inhibitor DAPT down-regulates cdk5 activity and modulates the distribution of neuronal cytoskeletal proteins: J. Kanungo, et al.; J. Neurochem. 106, 2236 (2008) \n?DAPT enhances the apoptosis of human tongue carcinoma cells: B.E. Grottklau, et al.; Int. J. Oral Sci. 1, 81 (2009) \n?

Alternative Names

N--S-phenylglycine tert.butyl ester