| 应用 |
A selective inhibitor of SIRT1 over SIRT2 and SIRT3 |
| 产品介绍 |
EX 527 (Selisistat)是一种有效的，选择性的SIRT1抑制剂，IC50为38 nM，比作用于SIRT2和SIRT3选择性高200倍以上。 |
| 备注 |
EX 527 is a potent and selective SIRT1 inhibitor with IC50 of 38 nM, exhibits >200-fold selectivity against SIRT2 and SIRT3. |
| 生化机理 |
EX 527 is a potent and selective inhibitor of the SIRT1 class III histone deacetylase enzyme, thought to block the release of deacetylated peptide and O-acetyl-ADP-ribose from the enzyme following the deacetylation process. EX 527 has been used a powerful tool for studying the relationship between SIRT1 and cell regulation. The deacetylation of cortactin, a protein responsible for rearrangements of the actin cytoskeleton, is associated with cell motility and possibly tumorigenesis, and blocking of this deacetylation by EX 527 correlated to a decrease in cell motility. Blocking of SIRT1 by EX 527 also demonstrated that deacetylation of the important tumor suppressor protein p53 is mediated by SIRT1 as well. EX 527 inhibits other sirtuin family deacetylases only at much higher concentrations (IC50 = 19.6 and 48.7 μM for SIRT2 and SIRT3, respectively). |
| 别名 |
6-氯-2,3,4,9-四氢-1H-咔唑-1-甲酰胺;EX 527 (SEN0014196);SIRT1 Inhibitor III; 6-Chloro-2,3,4,9-tetrahydro-1H-Carbazole-1-carboxamide |
