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其它表观遗传学和基因调控试剂

EX 527 (Selisistat)

品牌 厂商性质 产地 货期
阿拉丁 生产商 上海 现货

在线咨询 询底价
产品参数
货号 CAS号 操作
E129892-10mg 49843-98-3 询底价
E129892-50mg 49843-98-3 询底价
E129892-5mg 49843-98-3 询底价
产品介绍

  • 分子式 C13H13ClN2O
  • 分子量248.71
  • Beilstein号
  • EC号
  • MDL号 MFCD03009471
  • PubChem编号

属性

沸点 531.72°C/760mmHg
熔点 178°C
折光率 1.69
溶解性 Soluble in DMSO (10 mg/ml), ethanol (5 mg/ml), DMF (~20 mg/ml), and DMSO:PBS (1:1 pH 7.2) (~0.5 mg/ml).
存贮条件 储存温度2-8℃
密度 1.3900

描述

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

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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途