| 货号 | 13944-5mg |
| 描述 | The jumonji domain-containing protein 2 (JMJD2) subfamily of histone demethylases have been shown to catalyze demethylation of the methylated forms of histone 3 lysine 9 (H3K9) and H3K36 in vitro and in cells.1 Because histone demethylases are implicated in certain diseases, including cancer, selective inhibitors are candidate anticancer agents as well as potential tools for elucidating the biological functions of JMJDs.2 N-Oxalylglycine, the amide analog of α-ketoglutarate, is a cell permeable inhibitor of α-ketoglutarate-dependent enzymes, including JMJD2A, JMJD2C, and JMJD2E (IC50s = 250, 500, and 24 μM, respectively).3,4,5,6 It can also inhibit the prolyl hydroxylase domain-containing proteins PHD1 and PHD2 with IC50 values of 2.1 and 5.6 μM, respectively.4,5,7 |
| 别名 | NOG; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Krishnan, S.,Horowitz, S. and Trievel, R. Structure and function of histone H3 lysine 9 methyltransferases and demethylases. ChemBioChem 12, 254-263 (2011). 2.Tian, X. and Fang, J. Current perspectives on histone demethylases. Acta Biochimica et Biophysica Sinica 39(2), 81-88 (2007). 3.Hamada, S.,Kim, T.D.,Suzuki, T., et al. Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors. Bioorganic & Medicinal Chemistry Letters 19, 2852-2855 (2009). 4.Hamada, S.,Suzuki, T.,Mino, K., et al. Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of Jumonji domain-containing protein 2 histone demethylase inhibitors. Journal of Medicinal Chemistry 53, 5629-5638 (2010). 5.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). 6.Rose, N.R.,Woon, E.C.Y.,Kingham, G.L., et al. Selective inhibitors of the JMJD2 histone demethylases: Combined nondenaturing mass spectrometric screening and crystallographic approaches. Journal of Medicinal Chemistry 53, 1810-1818 (2010). | |
| 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 | 147.1 |
| 分子式 | C4H5NO5 |
| CAS号 | 5262-39-5 |
| 稳定性 | ≥ 2 years |
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