Mammalian sirtuin 2 (SIRT2) is a nicotinamide adenine dinucleotide-dependent histone deacetylase (HDAC) with roles in cell cycle progression and tumorigenesis. AGK2 is a cell-permeable, selective inhibitor of SIRT2 (IC50 = 3.5 μM) that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.1 It rescues dopamine neurons from α-synuclein toxicity in both in vitro and in vivo Parkinson’s disease models, mimicking the effect of siRNA-mediated blockade of SIRT2 expression.1 AGK2 may be a useful tool for studying the roles of SIRT2 in neurodegeneration and aging, as well as cell cycle progression and tumorigenesis.
1
Outeiro, T.F., Kontopoulos, E., Altmann, S.M., et al. Sirtuin 2 inhibitors rescue a-synuclein-mediated toxicity in models of Parkinson’s Disease. Science317516-519(2007).
Lee, M.J.C., Shoeman, D.W., Goon, D.J.W., et al. N-hydroxybenzenecarboximidic acid derivatives: A new class of nitroxyl-generating prodrugs. Nitric Oxide5(3)278-287(2001).
AGK2 is available in the following screening
libraries: