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AGK2
Epigenetic modifier; Inhibits SIRT2 histone deacetylase
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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.).