SRT2104 (GSK-2245840)

Description: SRT2104 (formerly GSK-2245840; SRT2104; GSK2245840; SRT-2104) is a novel, first-in-class, brain penetrant, and highly selective small molecule activator of SIRT1 (Sirtuin 1) with potential use for neurodegenerative diseases. SIRT1 (Sirtuin 1) is involved in the regulation of energy homeostasis. Sirtuin 1 is a nicotinamide adenine dinucleotide-dependent protein deacetylase which regulates longevity and improves metabolism. Activation of Sirtuin 1 confers beneficial effects in models of neurodegenerative diseases. SRT2104 can penetrate the blood-brain barrier, attenuate brain atrophy, improve motor function, and extend survival in a mouse model of Huntington's disease. These findings imply a novel therapeutic strategy for Huntington's disease by targeting Sirtuin 1.

References: Aging Cell. 2014 Oct; 13(5):787-96; Ann Clin Transl Neurol. 2014 Dec; 1(12):1047-52.

Publications Citing Use of InvivoChem SRT2104 (GSK-2245840): https://www.biorxiv.org/content/10.1101/2021.08.10.455847v1. doi.org/10.1101/2021.08.10.455847

GSK2245840; SRT2104; GSK-2245840; SRT 2104; GSK 2245840; SRT-2104.

Chemical Name: 4-methyl-N-(2-(3-(morpholinomethyl)imidazo[2, 1-b]thiazol-6-yl)phenyl)-2-(pyridin-3-yl)thiazole-5-carboxamide

SMILES Code: O=C(C1=C(C)N=C(C2=CC=CN=C2)S1)NC3=CC=CC=C3C4=CN5C(SC=C5CN6CCOCC6)=N4