| 货号 | 11187-25mg |
| 描述 | The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. JQ1 displaces BET proteins from chromatin by competitively binding to the acetyl-lysine recognition pocket of BET bromodomains.1,2 Enantiomerically pure (+)-JQ1 binds to BRD4 bromodomains 1 and 2 with Kd values of ~50 and 90 nM, respectively, whereas the (−)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains.1 JQ1 has been used as a chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis.1,2,3,4,5 See the Structural Genomics Consortium (SGC) website for more information. |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Filippakopoulos, P.,Qi, J.,Picaud, S., et al. Selective inhibition of BET bromodomains. Nature 468(7327), 1067-1073 (2010). 2.Dawson, M.A.,Kouzarides, T., and Huntly, B.J. Targeting epigenetic readers in cancer. N. Engl. J. Med. 367(7), 647-657 (2012). 3.Delmore, J.E.,Issa, G.C.,Lemieux, M.E., et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc. Cell 146(6), 904-917 (2011). 4.Mertz, J.A.,Conery, A.R.,Bryant, B.M., et al. Targeting MYC dependence in cancer by inhibiting BET bromodomains. Proc. Natl. Acad. Sci. USA 108(40), 16669-16674 (2011). 5.Dawson, M.A.,Prinjha, R.K.,Dittmann, A., et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 478, 529-533 (2011). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 457 |
| 分子式 | C23H25ClN4O2S |
| CAS号 | 1268524-70-4 |
| 稳定性 | ≥ 2 years |
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