PF-543
货号：
17034-1mg 基本售价：
350.0 元 规格：
1 mg
产品信息
概述| 货号 | 17034-1mg |
| 描述 | PF-543 is a potent inhibitor of sphingosine kinase 1 (SK1; IC50 = 2-3.6 nM) that less effectively inhibits SK2 (IC50 = 356 nM).1 It does not significantly block the activity of other protein and lipid kinases, or bind sphingosine-1-phosphate receptors, when tested at a concentration of 10 µM.1 PF-543 prevents the phosphorylation of sphingosine in cancer cells and in whole blood (EC50s = 8.4 and 27 nM, respectively).1 Through its effects on SK1, PF-543 prevents sickling, hemolysis, and inflammation in sickling cell disease transgenic mice.2 Unlike inhibitors that are selective for SK2, PF-543 does not impair DNA synthesis in human pulmonary arterial smooth muscle cells.3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Schnute, M.E.,McReynolds, M.D.,Kasten, T., et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochemistry Journal 444(1), 79-88 (2012).
2.Zhang, Y.,Berka, V.,Song, A., et al. Elevated sphingosine-1-phosphate promotes sickling and sickle cell disease progression. Journal of Clinical Investigation 124(6), 2750-2761 (2014).
3.Byun, H.S.,Pyne, S.,Macritchie, N., et al. Novel sphingosine-containing analogues selectively inhibit sphingosine kinase (SK) isozymes, induce SK1 proteasomal degradation and reduce DNA synthesis in human pulmonary arterial smooth muscle cells. Medchemcomm. 4(10), 1-15 (2013).
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| 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 | 465.6 |
| 分子式 | C27H31NO4S |
| CAS号 | 1415562-82-1 |
| 稳定性 | ≥ 2 years |
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