Signal Transduction
Stem Cells
Signaling Pathways
Product Type
All Products
New Products
Small Molecules
Peptides
Controlled Substances
Toxins
Caged Compounds
Fluorescent Probes
Screening Libraries
Ligand Sets
Other Product Types
Research Area
Cancer
Cardiovascular System
Endocrinology
Immunology
Neuroscience
Pain & Inflammation
Respiratory System
BegacestatCat. No. 4283 |
Price and AvailabilityBy 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.Certificate of Analysis / 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 Target
Keywords: Begacestat, supplier, GSI953, Begacestat, pfizer, gamma, γ, g-secretase, inhibitors, APP, amyloid, precursor, proteins, notch, AB40, Abeta40, Aβ40, AB42, Abeta42, Aβ42
Quick Order
Find multiple products by catalog number
Cancer Research Guide
Request your free copy
Highlights over 350 products for cancer research. Request a copy or view PDF today.
VEGF Pathway & Anti-Angiogenic Therapy
Written by N. Ferrara & Y. Crawford
A summary of antiangiogenic therapies targeting the VEGF pathway and the mechanisms of therapy resistance.
The Neurobiology of Alzheimer's Disease
Written by Alan Palmer
'The Neurobiology of Alzheimer's Disease' summarizes structural and functional changes observed in the progression of AD.
New Products in this Area
γ-secretease inhibitor; inhibits Notch pathway
CA 074Selective cathepsin B inhibitor
P005091USP7 inhibitor
Hexa-D-arginineFurin inhibitor
Twitter Updates
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.