AGK2 is a cell-permeable, reversible inhibitor of mammalian sirtuin 2 (SIRT2) activity (IC50 = 3.5 μM)
It displays minimal activity against SIRT1 or SIRT3 (IC50 > 50 μM; Outeiro et al.) Its target, SIRT2, is a nicotinamide adenine dinucleotide (NAD)-dependent histone deacetylase (HDAC) with roles in neurodegeneration, aging, cell cycle progression, and tumorigenesis
Activates the NLRP3 inflammasome in mouse bone marrow-derived macrophages (Youm et al.)
Decreases aldehyde dehydrogenase (ALDH1)+ cancer stem cells in primary breast cancer populations (Zhao et al.) 2014)
Decreases SIRT2-induced autophagy in human cancer cell lines (Zhao et al. 2010)
Protects dopaminergic neurons from α-synuclein-mediated toxicity in in vitro and in vivo models of Parkinson's disease (Outeiro et al.)
