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.
Certificate of Analysis / Safety Data Sheet
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.
If you know of a relevant citation for this product please let us know.
View Related Products by Target
Keywords: Begacestat, supplier, GSI953, Begacestat, pfizer, gamma, gamma-secretase, γ, g-secretase, inhibitors, APP, amyloid, precursor, proteins, notch, AB40, Abeta40, Aβ40, AB42, Abeta42, Aβ42
Find multiple products by catalog number
New Products in this Area
Non-peptide, competitive angiotensin converting enzyme (ACE) inhibitorAprotinin
Competitive serine protease inhibitorTCID
Selective ubiquitin C-terminal hydrolase-L3 (UCH-L3) inhibitor2-MPPA
Selective glutamate carboxypeptidase II (GCP II) inhibitor; orally bioavailableE 64
Potent and irreversible cysteine protease inhibitorAEBSF
Broad spectrum, irreversible inhibitor of serine proteasesTC-E 5006
γ-secretase modulator; reduces Aβ42 levelsPTIQ
Potent MMP-3 expression inhibitor; neuroprotective
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.