| 货号 | 11181-1mg |
| 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.1 I-BET151 is an isoxazole class pan-BET family inhibitor, blocking BRD2, BRD3, and BRD4 with IC50 values of 0.5, 0.25, and 0.79 µM, respectively.2,3,4,5 Through this action, it blocks the growth of leukemic cell lines driven by mixed lineage leukemia (MLL) fusions at nanomolar concentrations, whereas tyrosine kinase activated cells were much less sensitive.6 Specifically, I-BET151 induces apoptosis via reduced expression of BCL2 or triggers G0/G1 cell cycle arrest in MLL-fusion cell lines.6 I-BET151 is effective in vivo, suppressing MLL leukemia progression in two different mouse models.6 |
| 别名 | GSK1210151A; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Gallenkamp, D.,Gelato, K.A.,Haendler, B., et al. Bromodomains and their pharmacological inhibitors. ChemMedChem 9(3), 438-464 (2014). 2.Kline, T.B.,Benington, F.,Morin, R.D., et al. Structure-activity relationships for hallucinogenic N,N-dialkyltryptamines: Photoelectron spectra and serotonin receptor affinities of methylthio and methylenedioxy derivatives. Journal of Medicinal Chemistry 25(11), 1381-1383 (1982). 3.Vidler, L.R.,Brown, N.,Knapp, S., et al. Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites. Journal of Medicinal Chemistry 55(17), 7346-7359 (2012). 4.Hewings, D.S.,Fedorov, O.,Filippakopoulos, P., et al. Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. Journal of Medicinal Chemistry 56(8), 3217-3227 (2013). 5.Dawson, M.A.,Kouzarides, T. and Huntly, B.J. Targeting epigenetic readers in cancer. N. Engl. J. Med. 367(7), 647-657 (2012). 6.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 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 415.5 |
| 分子式 | C23H21N5O3 |
| CAS号 | 1300031-49-5 |
| 稳定性 | ≥ 2 years |
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