Begacestat

Cat. No. 4283

Begacestat C9H8ClF6NO3S2 [769169-27-9]

Price and Availability

For Begacestat pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Alternative Name: GSI-953

Chemical Name: 5-Chloro-N-[(1S)-3,3,3-trifluoro-1-(hydroxymethyl)-2-(trifluoromethyl)propyl]-2-thiophenesulfonamide

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
391.74
Formula:
C9H8ClF6NO3S2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
769169-27-9

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 / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

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 Product Action

Keywords: Begacestat, supplier, GSI953, Begacestat, pfizer, gamma, gamma-secretase, γ, g-secretase, inhibitors, APP, amyloid, precursor, proteins, notch, AB40, Abeta40, Aβ40, AB42, Abeta42, Aβ42, amyloidbeta, amyloidb, amyloidβ, Tocris Bioscience, γ-Secretase Inhibitors

Quick Order

Find multiple products by catalog number

divider line

Cancer Research Product Guide

Cancer Research Product Guide

Highlights over 750 products for cancer research. Request copy or view PDF today.

divider line

Neurodegeneration Research Product Guide

Neurodegeneration Product Guide

Updated in 2015, this guide highlights over 275 products for neurodegeneration research. Request copy or view PDF today.

divider line

VEGF Pathway & Anti-Angiogenic Therapy

Written by N. Ferrara & Y. Crawford

Angiogenesis Life Science Poster

A summary of antiangiogenic therapies targeting the VEGF pathway and the mechanisms of therapy resistance. Request copy today.

divider line

Alzheimer's Disease: Neurobiology and Drug Targets

Written by Alan Palmer

Alzheimer's Life Science Poster

Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets. Request copy or view PDF today.

divider line

New Products in this Area

VTP 27999 trifluoroacetate

Highly potent and selective renin inhibitor

Tiplaxtinin

Plasminogen activator inhibitor-1 (PAI-1) inhibitor

Balicatib

Potent and selective cathepsin K inhibitor

HFI 142

Insulin-regulated aminopeptidase (IRAP) inhibitor

Sign-up for new product e-alerts
divider line

Twitter Updates

Follow @Tocris on Twitter

Follow us on Twitter!

Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.