| 货号 | 11572-50mg |
| 描述 | 2-oxoglutarate (2OG) and other Fe(II)-dependent oxygenases are an important family of enzymes with roles in collagen biosynthesis, lipid metabolism, nucleic acid repair and modification, histone demethylation, and hypoxic sensing.1,2,3 Impaired 2OG oxygenase activity is linked to the cellular hypoxic response and various diseases including cancer.4 Iron-chelators, Co(II) ions, and 2OG analogues such as pyridine-2,4-dicarboxylate and N-oxalylglycine have been used as non-selective inhibitors of 2OG oxygenases.3,4,5 However, they require administration as pro-drug diester derivatives. IOX1 is a broad-spectrum inhibitor of 2OG oxygenases that does not require application in a pro-drug formulation. IOX1 inhibits JMJD2A, JMJD2E and the 2OG oxygenases PHF8, PHD2, and FIH with IC50 values of 1.7, 2.4, 13.3, 14.3, and 20.5 μM, respectively.4 IOX1 inhibits H3K9me3 demethylation by JMJD2A in HeLa cells with an IC50 value of 87 μM.4 See the Structural Genomics Consortium (SGC) website for more information. |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kawamura, A.,Tumber, A.,Rose, N.R., et al. Development of homogeneous luminescence assays for histone demethylase catalysis and binding. Analytical Biochemistry 404, 86-93 (2010). 2.Hewitson, K.S.,Holmes, S.L.,Ehrismann, D., et al. Evidence that two enzyme-derived histidine ligands are sufficient for iron binding and catalysis by factor inhibiting HIF (FIH). The Journal of Biological Chemisty 283(38), 25971-25978 (2008). 3.Rose, N.R.,Ng, S.S.,Mecinovic, J., et al. Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. Journal of Medicinal Chemistry 51, 7053-7056 (2008). 4.King, O.N.F.,Li, X.S.,Sakurai, M., et al. Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors. PLoS One 5(11), 1-12 (2010). 5.Flashman, E.,Bagg, A.L.,Chowdhury, R., et al. Kinetic rationale for selectivity toward N- and C-terminal oxygen-dependent degradation domain substrates mediated by a loop region of hypoxia-inducible factor prolyl hydroxylases. The Journal of Biological Chemisty 283(7), 3808-3815 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥97% |
| 计算分子量 | 189.2 |
| 分子式 | C10H7NO3 |
| CAS号 | 5852-78-8 |
| 稳定性 | ≥ 2 years |
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