Stemcell, 73052, AGK2

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.

IMMUNOLOGY

· Activates the NLRP3 inflammasome in mouse bone marrow-derived macrophages (Youm et al.).

CANCER RESEARCH

· 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).

DISEASE MODELING

· Protects dopaminergic neurons from α-synuclein-mediated toxicity in in vitro and in vivo models of Parkinson's disease (Outeiro et al.).