| 货号 | 11138-1g |
| 描述 | 2,4-Pyridinedicarboxylic Acid (2,4-PDCA) is a compound that structurally mimics 2-oxoglutarate (2-OG, also known as α-ketoglutarate) and chelates zinc, thus affecting a range of enzymes.1,2 As a 2-OG mimic, it blocks the activity of 2-OG oxygenases, which include certain lysine demethylases and a variety of hydroxylases (e.g., prolyl, collagen, lysyl).2,3 2,4-PDCA inhibits several Jumonji domain-containing lysine demethylases when used at low micromolar concentrations.4,5,6 Through its effects on hydroxylases, including prolyl hydroxlase 1 (IC50 = 1.5 µM), 2,4-PDCA modulates hypoxia-inducible factor turnover, collagen synthesis, and plant cell wall formation.2,7 It can inhibit zinc-dependent enzymes, like metallo-β-lactamase.8 2,4-PDCA also affects and is translocated by organic anion transporters.9 |
| 别名 | 2,4-Dicarboxypyridine;Lutidinic Acid;NSC 403248;2,4-PDCA; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Kidani, Y. and Hirose, J. Coordination chemical studies on metalloenzymes II. Kinetic behavior of various types of chelating agents towards bovine carbonic anhydrase. Journal of Biochemistry 81(5), 1383-1391 (1977). 2.Koski, M.K.,Hieta, R.,Böllner, C., et al. The active site of an algal prolyl 4-hydroxylase has a large structural plasticity. The Journal of Biological Chemisty 282(51), 37112-37123 (2007). 3.Mackeen, M.M.,Kramer, H.B.,Chang, K.H., et al. Small-molecule-based inhibition of histone demethylation in cells assessed by quantitative mass spectrometry. Journal of Proteome Research 9(8), 4082-4092 (2010). 4.Leurs, U.,Clausen, R.P.,Kristensen, J.L., et al. Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C). Bioorganic & Medicinal Chemistry Letters 22(18), 5811-5813 (2012). 5.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). 6.Kristensen, L.H.,Nielsen, A.L.,Helgstrand, C., et al. Studies of H3K4me3 demethylation by KDM5B/Jarid1B/PLU1 reveals strong substrate recognition in vitro and identifies 2,4-pyridine-dicarboxylic acid as an in vitro and in cell inhibitor. FEBS Journal 279(11), 1905-1914 (2012). 7.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). 8.Horsfall, L.E.,Garau, G.,Liénard, B.M.R., et al. Competitive inhibitors of the CphA metallo-β-lactamase from Aeromonas hydrophila. Antimicrobial Agents and Chemotherapy 51(6), 2136-2142 (2007). 9.Hagos, Y.,Schley, G.,Schödel, J., et al. α-Ketoglutarate-related inhibitors of HIF prolyl hydroxylases are substrates of renal organic anion transporters 1 (OAT1) and 4 (OAT4). Pflugers.Arch. 464(4), 367-374 (2012). | |
| 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 | 167.1 |
| 分子式 | C7H5NO4 |
| CAS号 | 499-80-9 |
| 稳定性 | ≥ 2 years |
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