Drug intelligence / Profile preview

AGK2

Development stage
Preclinical
Modality
Small Molecules
Administration
In Vitro (laboratory Use), Not Clinically Approved For Human Administration; No Established Clinical Route
01

Overview

AGK2 is a potent and selective small molecule inhibitor of sirtuin 2 (SIRT2), a member of the class III histone deacetylase family. It has an IC50 of 3.5 µM for SIRT2 and shows much weaker inhibition against SIRT1 and SIRT3 (IC50s of 30 µM and 91 µM respectively)[1][4][8]. By inhibiting SIRT2 activity, AGK2 modulates cellular processes such as stress resistance, metabolism, differentiation, aging[3][7], apoptosis[1], autophagy[4], cell cycle regulation[1], inflammation[4], and neuronal signaling pathways. Preclinical studies have shown that AGK2 can reduce α-synuclein-mediated toxicity in models of Parkinson’s disease[8] and inhibit hepatitis B virus replication both in vitro and in vivo with minimal hepatotoxicity[6]. It is primarily used as a research tool compound to study the biological roles of sirtuins.

Other names
SIRT2 Inhibitor ISIRT-2 Inhibitor ISIRT 2 Inhibitor ISIRT1 Inhibitor IVSIRT-1 Inhibitor IVSIRT 1 Inhibitor IV2-Cyano-3-(5-(2,5-dichlorophenyl)-2-furanyl)-N-5-quinolinyl-2-propenamide
02

Targets

SIRT2 (NAD-dependent protein deacetylase sirtuin-2)

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