货号 | 13168-1mg |
描述 | Sir2p, the product of the SIR2 gene, is a conserved NAD+-dependent histone deacetylase (HDAC) involved in the regulation of the lifespan in yeast. It plays roles in silencing gene expression and negatively regulates the initiation of DNA replication. Splitomicin is a small molecule inhibitor of Sir2p histone deacetylase activity, displaying higher activity in vivo (minimal inhibitory concentration = 0.49 µM) than in vitro(IC50 = 60 µM).1,2,3 It less effectively inhibits yeast Hst1, a paralog of Sir2p.2 Splitomicin has diverse effects on mammalian cells.4,5,6 |
别名 | 1-Naphthalenepropanoic Acid; |
供应商 | Cayman |
应用文献 | |
1.Bedalov, A.,Gatbonton, T.,Irvine, W.P., et al. Identification of a small molecule inhibitor of Sir2p. Proceedings of the National Academy of Sciences of the United States of America 98(26), 15113-15118 (2001). 2.Hirao, M.,Posakony, J.,Nelson, M., et al. Identification of selective inhibitors of NAD+-dependent deacetylases using phenotypic screens in yeast. The Journal of Biological Chemisty 278(52), 52773-52782 (2003). 3.Posakony, J.,Hirao, M.,Stevens, S., et al. Inhibitors of Sir2: Evaluation of splitomicin analogues. Journal of Medicinal Chemistry 47, 2635-2644 (2004). 4.Biacsi, R.,Kumari, D., and Usdin, K. SIRT1 inhibition alleviates gene silencing in Fragile X mental retardation syndrome. PLoS Genetics 4(3), (2008). 5.Liu, F.C.,Liao, C.H.,Chang, Y.W., et al. Splitomicin suppresses human platelet aggregation via inhibition of cyclic AMP phosphodiesterase and intracellular Ca++ release. Thrombosis Research 124, 199-207 (2009). 6.Kang, M.R.,Lee, S.W.,Um, E., et al. Reciprocal roles of SIRT1 and SKIP in the regulation of RAR activity: Implication in the retinoic acid-induced neuronal differentiation of P19 cells. Nucleic Acids Research 38(3), 822-831 (2010). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 198.2 |
分子式 | C13H10O2 |
CAS号 | 1384339 |
稳定性 | ≥ 2 years |
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