| 货号 | 16424-1mg |
| 描述 | The bromodomain and extra terminal (BET) proteins interact with acetylated lysine-containing sequences on target proteins via their bromodomains, commonly altering gene transcription.1 The human BET proteins contain two bromodomains, the first (BD1) being closer to the N-terminus than the second (BD2). RVX-208 is a selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC50 = 0.04-0.28 µM) over BD1 (IC50 = 1.8-3.1 µM).2,3 RVX-208 causes the selective release of BET proteins from chromatin in cells.2,3 It interferes with the BET protein BRD4, resulting in an increased expression of apolipoprotein (Apo) A1 in cells, mice, monkeys, and humans.4,5 RVX-208 also reduces atherosclerosis in hyperlipidemic ApoE-deficient mice.5 |
| 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.McLure, K.G.,Gesner, E.M.,Tsujikawa, L., et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One 8(12), 1-12 (2013). 3.Picaud, S.,Wells, A.,Felletar, I., et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proceedings of the National Academy of Sciences of the United States of America 110(49), 19754-19759 (2013). 4.Bailey, D.,Jahagirdar, R.,Gordon, A., et al. RVX-208: A small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo. Journal of the American College of Cardiology 55(23), 2580-2589 (2010). 5.Jahagirdar, R.,Zhang, H.,Azhar, S., et al. A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Atherosclerosis 236(1), 91-100 (2014). | |
| 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 | 370.4 |
| 分子式 | C20H22N2O5 |
| CAS号 | 1044870-39-4 |
| 稳定性 | ≥ 2 years |
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