| 货号 | 17055-25mg |
| 描述 | Rho-associated protein kinase II (ROCK-II) regulates the formation of actin stress fibers and focal adhesions, smooth muscle contraction, and gene expression. KD 025 is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively).1 Treatment of fibrosis-derived smooth muscle cells with KD 025 (40 µM) for 24 hours reduces the expression of connective tissue growth factor and remodels actin cytoskeleton.1 KD 025 decreases cell-spanning F-actin fibers and increases motility of microvascular endoethelial cells.2 In mice, KD 025 given by oral gavage dose-dependently reduces infarct volume after transient middle cerebral artery occlusion without causing significant hypotension.3 In humans, oral KD 025 diminishes STAT3 phosphorylation and pro-inflammatory cytokine production in CD4+ T cells while up-regulating phosphorylation of STAT5 in regulatory T cells, altering the immune response.4 |
| 别名 | SLx-2119; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Boerma, M.,Fu, Q.,Wang, J., et al. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin. Blood Coagul.Fibrinolysis 19(7), 709-718 (2008). 2.Breyer, J.,Samarin, J.,Rehm, M., et al. Inhibition of Rho kinases increases directional motility of microvascular endothelial cells. Biochemical Pharmacology 83(5), 616-626 (2012). 3.Lee, J.H.,Zheng, Y.,von Bornstadt, D., et al. Selective ROCK2 inhibition in focal cerebral ischemia. Ann.Clin.Transl.Neurol. 1(1), 2-14 (2014). 4.Zanin-Zhorov, A.,Weiss, J.M.,Nyuydzefe, M.S., et al. Selective oral ROCK2 inhibitor down-regulates IL-21 and IL-17 secretion in human T cell via STAT3-dependent mechanism. Proceedings of the National Academy of Sciences of the United States of America 1-6 (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 | 452.5 |
| 分子式 | C26H24N6O2 |
| CAS号 | 911417-87-3 |
| 稳定性 | ≥ 2 years |
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