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Submit Review4283 has been discontinued.
Begacestat is a γ-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.
Sold for research purposes under agreement from Pfizer Inc.
M. Wt | 391.74 |
Formula | C9H8ClF6NO3S2 |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 769169-27-9 |
PubChem ID | 11269353 |
InChI Key | PSXOKXJMVRSARX-SCSAIBSYSA-N |
Smiles | ClC1=CC=C(S(N[C@H](CO)C(C(F)(F)F)C(F)(F)F)(=O)=O)S1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
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
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
Keywords: Begacestat, 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, GSI-953, Gamma-Secretase, Amyloid, Beta, Peptides, 4283, Tocris Bioscience
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