Chemical Properties
white to almost white crystalline powder
Uses
2,4-Pyridinedicarboxylic Acid is a jumonji C (JmjC) histone demethylase inhibitor.
Uses
2,4-Pyridinedicarboxylic acid 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. 2,4-Pyridinedicarboxylic acid has been used in a study to develop an assay that represents the first report of a RapidFire mass spectrometery assay for an epigenetics target.
Definition
ChEBI: A pyridinedicarboxylic acid carrying carboxy groups at positions 2 and 4.
Flammability and Explosibility
Not classified
Biological Activity
2,4-pyridinedicarboxylic acid (2,4-pdca) is an inhibitor of histone lysine-specific demethylases that targets on jmjd2a (kdm4a), kdm4c, kdm4e (ic50, 1.4 μm), kdm5b (ic50, 3 μm), kdm6a and other 2-oxogynases [1][2].histone lysine-specific demethylases jmjd2a (kdm4a) and kdm4c are both members of the jumonji domain 2 (jmjd2) family and function as trimethylation-specific demethylases, converting specific trimethylated histone residues to the dimethylated form. kdm5b is an h3k4me3⁄ me2-specific lysine demethylase [1][2].2,4-pyridinedicarboxylic acid (2,4-pdca) is an inhibitor of jmjd2a (kdm4a), kdm4c and kdm5b. in the fdh-coupled assay, 2,4-pdca inhibited cckdm5b with ic50 value of 3 ± 1 μm. in maldi-tof analysis of h3(1-21)k4me3, 2,4-pdca reduced the level of h3(1-15) induced by cckdm5b. in u2-os cells transfected with kdm5b, 2,4-pdca inhibited the decrease of h3k4me3 [1]. in hg-treated vsmcs, 2,4-pdca (1.0 mm) inhibited jmjd2a and hg-induced proliferation in a concentration-dependent way, and inhibited hg-induced migration. 2,4-pdca also reduced the mrna and protein levels of mcp-1 and il-6 [2].in diabetic rats, 2,4-pdca (7.5 mg/kg/d) reduced neointimal area and i/m ratio in the injured arteries 28 days after injury. 2,4-pdca also inhibited the percentage of pcna-positive cells in the neointima [2].
References
[1]. kristensen lh, nielsen al, 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 j, 2012, 279(11): 1905-1914.
[2]. qi h, jing z, xiaolin w, et al. histone demethylase jmjd2a inhibition attenuates neointimal hyperplasia in the carotid arteries of balloon-injured diabetic rats via transcriptional silencing: inflammatory gene expression in vascular smooth muscle cells. cell physiol biochem, 2015, 37(2): 719-734.
