2,4-Pyridinedicarboxylic Acid CAS 499-80-9

2,4-Pyridinedicarboxylic Acid – Histone Lysine Demethylase Inhibitor for Epigenetic Research

Basic Information

• Product Name: 2,4-Pyridinedicarboxylic acid (2,4-PDCA)

• CAS Number: 499-80-9

• Molecular Formula: C₇H₅NO₄

• Molecular Weight: 167.12 g/mol

• EC Number: 207-892-2

• Appearance: White to off-white crystalline powder

• Solubility: Soluble in water, dimethyl sulfoxide (DMSO), and alkaline solutions

• Packaging: 20 kg or 25 kg per drum

Overview
2,4-Pyridinedicarboxylic acid (2,4-PDCA) is a small-molecule inhibitor of histone lysine demethylases (KDMs), specifically targeting members of the Jumonji domain-containing (JMJD) family. It acts as a competitive inhibitor of 2-oxoglutarate (2-OG)-dependent oxygenases, which play crucial roles in epigenetic regulation. This compound is widely used in biochemical and pharmacological research to study histone methylation dynamics and their role in gene expression, development, and disease.

Target Enzymes and Activity

• KDM4A (JMJD2A): IC₅₀ ~1.4 µM

• KDM4C (JMJD2C): IC₅₀ ~1.4 µM

• KDM4E (JMJD2E): IC₅₀ ~1.4 µM

• KDM5B (JARID1B): IC₅₀ ~3 µM

• KDM6A (UTX): Inhibits H3K27me3 demethylation

• Other 2-OG-dependent enzymes: Also inhibits related dioxygenases, making it a useful tool for studying oxidative demethylation pathways.

Mechanism of Action
JMJD2A (KDM4A) and KDM4C are trimethylation-specific histone demethylases that convert trimethylated histone lysine residues (e.g., H3K9me3, H3K36me3) to their dimethylated forms. KDM5B (JARID1B) is a demethylase specific for H3K4me3/me2. By inhibiting these enzymes, 2,4-PDCA modulates histone methylation states, influencing chromatin structure and transcriptional activity. This makes it a valuable tool for studying epigenetic regulation in cancer, stem cell biology, and neurobiology.

Applications

• Epigenetic research: Used as a chemical probe to study histone demethylase function in cellular models.

• Cancer research: Investigates the role of KDM4 and KDM5 family members in tumorigenesis and as potential therapeutic targets.

• Drug discovery: Serves as a lead compound or reference inhibitor in screening for novel epigenetic modulators.

• Biochemical assays: Employed in enzymatic activity assays to characterize demethylase activity and screen for new inhibitors.

Handling and Storage

• Store in a cool, dry, well-ventilated area, away from light and moisture.

• Keep containers tightly sealed to prevent contamination and degradation.

• Use appropriate personal protective equipment (gloves, safety goggles, lab coat) when handling.

• Avoid inhalation of dust and contact with skin and eyes.

Packaging
Available in 20 kg or 25 kg drums, or custom packaging upon request.

Quality Assurance
Each batch is tested for purity (by HPLC), identification (by NMR or MS), and water content to ensure consistent quality for research applications.