| 货号 | 4499/10 |
| 别名 | (6S)-4-(4-Chlorophenyl)-2,3,9-trime |
| 供应商 | Tocris |
| 生物活性 | Potent, high affinity, selective BET bromodomain inhibitor (IC50 values are 17.7, 32.6, 76.9 and 12942 nM for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively; Kd values are 49, 59.5, 82, 90.1, 128 and 190 nM for BRD4 (N), BRD3 (N), BRD3 (C), BRD4 (C), BRD2 (N) and BRDT (N) respectively). Induces squamous differentiation in NUT midline carcinoma (NMC) cell lines; inhibits tumor growth in NMC xenograft models in vivo. Exhibits reversible contraceptive effects in germ cells from male mice. Inactive analog (-)-JQ1 available. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 456.99 |
| 分子式 | C23H25ClN4O2 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
| 参考文献 | Herrmannet al (2012) Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML. Oncotarget. [Epub ahead of print] 3 1588. PMID: 23249862. Matzuket al (2012) Small-molecule inhibition of BRDT for male contraception. Cell 150 673. PMID: 22901802. Filippakopouloset al (2010) Selective inhibition of BET bromodomains. Nature 468 1067. PMID: 20871596. |