Description: Selisistat (EX-527) is a potent and specific inhibitor of the deacetylase SIRT1 (IC50 = 38 nM) and can be utilized in the study of neurological disorders such as Huntington's chorea. Target: Sirtuin. Smiles: NC(=O)C1CCCC2=C1NC1=CC=C(Cl)C=C21. References: Kabra N, et al. SirT1 is an inhibitor of...

EX-527 is an inhibitor of sirtuin 1 (SIRT1, IC50 = 0.098 µM). It is selective for SIRT1 over SIRT2, and SIRT3 (IC50s = 19.6 and 48.7 µM, respectively) and the cytochrome P450 (CYP) isoforms CYP3A4, CYP2D6, CYP2C9, CYP2C19, and CYP1A2 at 1 µM. EX-527 (50 µM) induces cell cycle arrest at the G1 phase in MCF-7...

EX 527 is an inhibitor of sirtuin 1 (SIRT1), sirtuins are considered class III histone deacetylases (HDACs). EX 527 binds the NAD+ site of sirtuin 1, stabilizing a closed conformation. EX 527 exhibits immunostimulatory and anti-inflammatory activities. In animal models of autoimmune colitis and inflammatory bowel...