Cat. No. 4283
Alternative Name: GSI-953
Chemical Name: 5-Chloro-N-[(1S)-3,3,3-trifluoro-1-
Biological Activityγ-secretase inhibitor; selectively inhibits cleavage of amyloid precursor protein (APP) over Notch. Lowers levels of Aβ42 and Aβ40 (EC50 values are 12.4 and 14.8 nM respectively in cells expressing human recombinant APP). Orally active.
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Martone et al (2009) Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein γ-secretase for the treatment of Alzheimer's disease. J.Pharmacol.Exp.Ther. 331 598. PMID: 19671883.
Mayer et al (2008) Discovery of begacestat, a Notch-1-sparing gamma secretase inhibitor for the treatment of Alzheimer's disease. J.Med.Chem. 51 7348. PMID: 19012391.
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Keywords: Begacestat, supplier, GSI953, Begacestat, pfizer, gamma, gamma-secretase, γ, g-secretase, inhibitors, inhibits, APP, amyloid, precursor, proteins, notch, AB40, Abeta40, Aβ40, AB42, Abeta42, Aβ42, amyloidbeta, amyloidb, amyloidβ, Tocris Bioscience, γ-Secretase Inhibitor products
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