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It is an in vitro and in cell inhibitor, as well as a known inhibitor of the histone lysine demethylases. 2,4-Pyridinedicarboxylic acid has been used in a study to determine that ruthenium(II) complexes exert antimetastatic effects on several tumor cell lines in vitro, achieved mostly by the effect on cell adhesion, migration and angiogenesis. 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. Through its effects on hydroxylases, including prolyl hydroxlase 1 (IC50 = 1.5 µM), It modulates hypoxia inducing factor turnover, collagen synthesis, and plant cell wall formation. It can inhibit zinc-dependent enzymes, like metallo-β-lactamase.8 2,4-PDCA also affects and is translocated by organic anion transporters.
Line H Kristensen, 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 J.,2012,279(11), 1905-1914.
Koski, M.K, et al.The active site of an algal prolyl 4-hydroxylase has a large structural plasticity. Biol Chem.,2007,282(51), 37112-37123.
Mackeen, et al. Small-molecule-based inhibition of histone demethylation in cells assessed by quantitative mass spectrometry. J Proteome Res.,2010,9(8), 4082-4092.