| 货号 | 14568-1mg |
| 描述 | The hypoxia-inducible factor (HIF) transcription factors are members of the basic-helix-loop-helix (bHLH) family of transcription factors and play important roles in maintaining cellular oxygen homeostasis.1,2 HIF-1α has emerged as an important drug target in breast and prostate cancer, cardiovascular disease, and ischemia.3,4 ML-228 is an activator of the HIF signaling pathway, as demonstrated by HIF response element (HRE) reporter assay (EC50 = 1.2 µM), HIF-1α nuclear translocation assay (EC50 = 1.3 µM), and increased VEGF expression (EC50 = 1.6 µM).5 Its activity in the HRE assay is blocked by excess iron, suggesting that ML-228 can chelate iron.5 Molecular modeling indicates that ML-228 does not modulate HIF signaling by binding to prolyl hydroxyases.5 ML-228 also significantly inhibits ligand binding to several channels, receptors, and transporters, including ERG potassium channel, 5-HT2B and A3 adenosine receptors, and dopamine transporter.5 |
| 别名 | CID-46742353; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Wang, G.L.,Jiang, B.H.,Rue, E.A., et al. Hypoxia-inducible factor 1 is a basic-helix-loop-helix-PAS heterodimer regulated by cellular O2 tension. Proceedings of the National Academy of Sciences of the United States of America 92, 5510-5514 (1995). 2.Safran, M. and Kaelin, W.G., Jr. HIF hydroxylation and the mammalian oxygen-sensing pathway. Journal of Clinical Investigation 111, 779-783 (2003). 3.William, C.,Masson, N.,Tian, Y.M., et al. Peptide blockade of HIFα degradation modulates cellular metabolism and angiogenesis. Proceedings of the National Academy of Sciences of the United States of America 99(16), 10423-10428 (2002). 4.Welsh, S.,Williams, R.,Kirkpatrick, L., et al. Antitumor activity and pharmacodynamic properties of PX-478, an inhibitor of hypoxia-inducible factor-1α. Molecular Cancer Therapeutics 3(3), 233-244 (2004). 5.Theriault, J.R.,Felts, A.S.,Bates, B.S., et al. Discovery of a new molecular probe ML228: An activator of the hypoxia inducible factor (HIF) pathway. Bioorganic & Medicinal Chemistry Letters 22(1), 76-81 (2012). | |
| 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 | 415.5 |
| 分子式 | C27H21N5 |
| CAS号 | 1357171-62-0 |
| 稳定性 | ≥ 2 years |
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