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 |
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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. |