| 货号 | 11049-5mg |
| 描述 | Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that controls genes involved in glycolysis, angiogenesis, migration, and invasion. Echinomycin is a cell-permeable inhibitor of HIF-1-mediated gene transcription.1,2 It acts by intercalating into DNA in a sequence-specific manner, blocking the binding of either HIF-1α or HIF-1β to the hypoxia-responsive element.1,2,3 Echinomycin reversibly inhibits hypoxia-induced HIF-1 transcription activity in U215 cells with an EC50 value of 1.2 nM.1 It inhibits hypoxia-induced expression of vascular endothelial growth factor, blocking angiogenesis and altering excitatory synaptic transmission in hippocampal neurons.2,4 Echinomycin also impairs expression of survivin, enhancing the sensitivity of multiple myeloma cells to melphalan.5 |
| 别名 | Antibiotic A 654I;NSC 13502;NSC 526417;Quinomycin A;SK 302B; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kong, D.,Park, E.J.,Stephen, A.G., et al. Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity. Cancer Research 65(19), 9047-9055 (2005). 2.Nickols, N.G.,Jacobs, C.S.,Farkas, M.E., et al. Modulating hypoxia-inducible transcription by disrupting the HIF-1-DNA interface. ACS Chemical Biology 2(8), 561-571 (2007). 3.Ward, D.C.,Reich, E. and Goldberg, I.H. Base specificity in the interaction of polynucleotides with antibiotic drugs. Science 149(3689), 1259-1263 (1965). 4.Huang, Y.F.,Yang, C.H.,Huang, C.C., et al. Pharmacological and genetic accumulation of hypoxia-inducible factor-1α enhances excitatory synaptic transmission in hippocampal neurons through the production of vascular endothelial growth factor. Journal of Neuroscience 30(17), 6080-6093 (2010). 5.Hu, Y.,Kirito, K.,Yoshida, K., et al. Inhibition of hypoxia-inducible factor-1 function enhances the sensitivity of multiple myeloma cells to melphalan. Molecular Cancer Therapeutics 8(8), 2329-2338 (2009). | |
| 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 | 1101.3 |
| 分子式 | C51H64N12O12S2 |
| CAS号 | 512-64-1 |
| 稳定性 | ≥ 1 year |
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