PeptideDB

Selisistat

CAS: 49843-98-3 F: C13H13ClN2O W: 248.71

Selisistat (EX-527) is a potent and selective SirT1 (Sir2 in Drosophila melanogaster) inhibitor with an IC50 of 123 nM f
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Bioactivity Selisistat (EX-527) is a potent and selective SirT1 (Sir2 in Drosophila melanogaster) inhibitor with an IC50 of 123 nM for SirT1. Selisistat alleviates pathology in multiple animal and cell models of Huntington's disease[1][2].
Target IC50: 123 nM (SirT1)
Invitro Selisistat (1-10 μM) inhibits the deacetylation activity of both human SirT1 and Drosophila Sir2 in transfected cells[1].
In Vivo Selisistat (5 and 20 mg/kg, PO, daily; transgenic R6/2 mice beginning at 4.5 weeksof age to death) is protective in the R6/2 mouse model of Huntington’s disease (HD)[1].
Name Selisistat
CAS 49843-98-3
Formula C13H13ClN2O
Molar Mass 248.71
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [1]. Smith MR, et al. A potent and selective Sirtuin 1 inhibitor alleviates pathology in multiple animal and cell models of Huntington's disease. Hum Mol Genet. 2014;23(11):2995-3007. [2]. Napper AD, et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1 [published correction appears in J Med Chem. 2007 Mar 8;50(5):1086]. J Med Chem. 2005;48(25):8045-8054.