| 货号 | 15943-500ug |
| 描述 | MAP kinase-activated protein kinase 2 (MAPKAP2, MK2) is a stress-activated serine/threonine protein kinase that is phosphorylated by p38 MAP kinase and is involved in diverse cellular functions with a central role in inflammation.1,2,3 MK2 inhibitor III is a potent, cell-permeable inhibitor of MK2 (IC50 = 8.5 nM).4 It less potently blocks MK3 and MK5 (IC50s = 210 and 81 nM, respectively) and is weak or inactive against several other kinases, including other p38 MAP kinase targets.4 MK2 inhibitor III prevents LPS-induced synthesis of TNF-α in human monocyte-like U937 cells (IC50 = 4.4 µM).4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Huang, X.,Shipps, G.W., Jr.,Cheng, C.C., et al. Discovery and hit-to-lead optimization of non-ATP competitive MK2 (MAPKAPK2) inhibitors. ACS Med.Chem.Lett. 2, 632-637 (2011). 2.Wang, X.,Khaleque, M.A.,Zhao, M.J., et al. Phosphorylation of HSF1 by MAPK-activated protein kinase 2 on serine 121, inhibits transcriptional activity and promotes HSP90 binding. The Journal of Biological Chemisty 281(2), 782-791 (2006). 3.Werz, O.,Szellas, D.,Steinhilber, D., et al. Arachidonic acid promotes phosphorylation of 5-lipoxygenase at Ser-271 by MAPK-activated protein kinase 2 (MK2). J.Biol.Chem 277(17), 14793-14800 (2002). 4.Anderson, D.R.,Meyers, M.J.,Vernier, W.F., et al. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). Journal of Medicinal Chemistry 50(11), 2647-2654 (2007). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 358.4 |
| 分子式 | C21H16N4O • H2O |
| CAS号 | 1186648-22-5 |
| 稳定性 | ≥ 2 years |
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