| 货号 | 5173/50 |
| 别名 | (E)-4-[2-(2-Amino-4-hydroxy-5-methy |
| 供应商 | Tocris |
| 生物活性 | Potent and selective BRD4 bromodomain inhibitor (Ki = 30 - 50 nM for the first bromodomain (BRD4(1)). Exhibits 10-fold selectivity for BRD4(1) over BRD4(2). Blocks BRD4 transcriptional activity in lipopolysaccharide-induced production of both nitric oxide and IL-6 in mouse macrophages (IC50 values are 3.8 and 4.9 μM, respectively). Attenuates melanoma cell proliferation in vitro. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 383.42 |
| 分子式 | C18H17N5O3 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| 参考文献 | Seguraet al (2013) BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy. Cancer Res. 73 6264. PMID: 23950209. Zhanget al (2013) Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J.Med.Chem. 56 9251. PMID: 24144283. |