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Begacestat
- GSI 953
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C9H8ClF6NO3S2
- MW: 391.74
Description
Begacestat (GSI-953) is a highly potent and selective gamma (γ)-secretase inhibitor (GSI) that reduces Aβ40 and Aβ42 production in cells expressing human amyloid precursor protein (APP). It exhibits potency (EC50 values) of 14.8 nM and 12.4 nM for Aβ40 and Aβ42, respectively. It functions as a "Notch-sparing" inhibitor, demonstrating a >16-fold in vitro selectivity for processing APP over the Notch signaling pathway.
γ-Secretase is a multi-subunit protease complex involved in APP cleavage and Notch signaling. Begacestat is used to study γ-secretase-dependent APP processing and amyloid-β generation. Begacestat is pharmacologically relevant for Alzheimer disease research and for evaluating selective modulation of amyloidogenic processing.
Key Features
- Potent γ-secretase inhibitor
- Reduces Aβ40 and Aβ42 production
- Targets APP processing pathways
- Useful tool for amyloid-β biology
Applications
- Alzheimer disease pathway research
- APP processing studies
- Amyloid-β production assays
- γ-Secretase pharmacology and selectivity profiling
More Information
| Parent CAS No. | 769169-27-9 |
|---|---|
| Chemical Name | (S)-5-chloro-N-(4,4,4-trifluoro-1-hydroxy-3-(trifluoromethyl)butan-2-yl)thiophene-2-sulfonamide |
| extra_info | . |
| SMILES | C1=C(S(=O)(=O)N[C@H](CO)C(C(F)(F)F)C(F)(F)F)SC(Cl)=C1 |&1:6,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C9H8ClF6NO3S2/c10-5-1-2-6(21-5)22(19,20)17-4(3-18)7(8(11,12)13)9(14,15)16/h1-2,4,7,17-18H,3H2/t4-/m1/s1 |
| InChiKey | PSXOKXJMVRSARX-SCSAIBSYSA-N |
| CID | 11269353 |
| Short Description | γ-Secretase inhibitor |
References
- RL Martone et al. Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. J. Pharmacol. Exp. Ther. 2009, 331(2), 598-608.
- SC Mayer et al. Discovery of Begacestat, a Notch-1-Sparing γ-Secretase Inhibitor for the Treatment of Alzheimer’s Disease. J. Med. Chem. 2008, 51(23), 7348-7351.
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