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I-BET469
产品别名
2003197-53-1
I-BET469
5-[1-[2-Methoxy-1-(methoxymethyl)ethyl]-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-1,3-dimethyl-2(1H)-pyridinone
5-(1-(1,3-Dimethoxypropan-2-yl)-5-morpholino-1H-benzo[d]imidazol-2-yl)-1,3-dimethylpyridin-2(1H)-one
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C23H30N4O4 |
| Molecular weight | 426.51 |
| Biochem/physiol Actions【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 (Kd in 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 shows in vivo efficacy 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.). |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
