Selisistat (EX-527)是SIRT1选择性抑制剂,IC50为38 nM,作用于SIRT2和SIRT3时IC50分别为19.6 μM和48.7 μM,但对SIRT4-7和I/II类HDAC的活性影响不大。
参考文献
[1] Solomon JM, Pasupuleti R, Xu L, et al. Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Mol Cell Biol. 2006 Jan;26(1):28-38. doi: 10.1128/MCB.26.1.28-38.2006(IF:3.735).
[2] Velásquez DA, Martínez G, Romero A, et al. The central Sirtuin 1/p53 pathway is essential for the orexigenic action of ghrelin. Diabetes. 2011 Apr;60(4):1177-85. doi: 10.2337/db10-0802(IF:7.199).
[3] Smith MR, Syed A, Lukacsovich T, et al. A potent and selective Sirtuin 1 inhibitor alleviates pathology in multiple animal and cell models of Huntington's disease. Hum Mol Genet. 2014 Jun 1;23(11):2995-3007. doi: 10.1093/hmg/ddu010(IF:5.34).
-25~-15℃保存,有效期3年。