半岛bd体育手机客户端 说明
生化/生理作用
I-BET469 is an orally active bromodomain (BrD) inhibitor with selectivity toward a subset of bromodomain-containng proteins (BCPs) and BrDs (Kdin nM: BRD4 BrD1/2 = 1.5/2.9, BRD3 BrD1/2 = 2/2.3, BRD2 BrD1/2 = 2.3/2.8, BRDT BrD1/2 = 12/100, CREBBP = 37, EP300 = 49; Kd≥4.8 μM toward 22 other BCPs). I-BET469 targets cellular BRD4 with high affinity (pKd= 8.3 or Kd= 5.0 nM by NanoBRET) and showsin vivoefficacy in a murine acute endotoxic shock model (1, 3, 10 mg/kg po. 30 min prior to LPS) and a chronic T cell-dependent immunization model (IgG suppression on day 14 = 24% and 65%, respectively, with 0.3 mg/kg or 3 mg/kg daily po.).
基本信息
| 经验(实验)分子式 | C23H30N4O4 |
| 分子量 | 426.51 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
