GSK1324726A (I-BET726)
规格
| Cas Number | 1300031-52-0 |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 简短描述 | 表观遗传阅读器域抑制剂 |
| 英文简短描述 | Epigenetic Reader Domain Inhibitors |
| 过滤标签 | Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | GSK1324726A （I-BET726）是一种高选择性的 BET 家族蛋白抑制剂，对 BRD2、BRD3 和 BRD4 的 IC50 分别为 41 nM、31 nM 和 22 nM。 |
| 英文描述 |
Information GSK1324726A (I-BET726) GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively. Targets BRD4 (Cell-free assay); BRD3 (Cell-free assay); BRD2 (Cell-free assay) 22 nM; 31 nM; 41 nM In vitro In neuroblastoma cell lines, GSK1324726A inhibits cell growth and induces cytotoxicity. GSK1324726A also modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways, including the direct suppression of BCL2 and MYCN. In vivo In the mouse SK–N-AS and CHP-212 models, GSK1324726A (15 mg/kg p.o.) results in tumor growth inhibition and down-regulation MYCN and BCL2 expression. In a mouse septic shock model, GSK1324726A (10 mg/kg i.v.) shows potent anti-inflammatory effects, and prevents death of diseased animals. Cell Research(from reference) Cell lines：LA-N-1, Kelly, LA1-55n, BE(2)-M17, BE(2)-C, KanTS, IMR32, LA-N-2, SK-N-SH, SK-N-BE(2), CHP-134, SK-N-AS, SH-SY5Y, SK-N-FI, CHP-212, LA1-5s, SK-N-DZ cells Concentrations：~10 μM Incubation Time：6 days |