Selisistat_product_DataBase

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.

PeptideDB

Selisistat

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