cell-permeable, selective inhibitor of SIRT2
CAS：304896-21-7
分子式：C23H13Cl2N3O2
分子量：434.3
纯度：98%
存储：Store at -20°C

Background:

AGK7 is an inactive control of AGK2, a cell-permeable and selective SIRT2 inhibitor [1][2].

The sirtuins are members of the histone deacetylase family of proteins that participate in many cellular functions and play an important role in aging. Silent information regulator 2 (Sir2) is a nicotinamide adenine dinucleotide-dependent histone deacetylase (HDAC) in yeast that participates in cell protection and cell cycle regulation. Human SIRT2 is involved in cell cycle regulation through the deacetylation ofα-tubulin [1].

AGK7 is an inactive control of AGK2 to be used in experiments with AGK2. AGK2 is a cell-permeable, potent and selective SIRT2 inhibitor with IC50 value of 3.5 μM. AGK2 slightly inhibited SIRT1 and 3 only at concentrations over 40 μM. Relative to an inactive control AGK7, AGK2 increased acetylated tubulin. In H4 cells transfected with α-Syn, AGK2 reduced α-Syn-mediated toxicity in a dose-dependent way. By contrast, the inactive AGK7 had no effect. In H4 cells cotransfected withα-Syn and synphilin-1, the inactive AGK7 failed to affect a-Syn aggregation, whereas AGK2 promoted the formation of enlarged inclusions [1].

参考文献:
[1].  Outeiro TF, Kontopoulos E, Altmann SM, et al. Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science. 2007 Jul 27;317(5837):516-9.
[2].  Cole PA. Chemical probes for histone-modifying enzymes. Nat Chem Biol. 2008 Oct;4(10):590-7.