420202

JMJD Histone Demethylase Inhibitor III

The JMJD Histone Demethylase Inhibitor III controls the biological activity of JMJD Histone Demethylase. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonym(s): JMJD Histone Demethylase Inhibitor III, JHDM Inhibitor III, Histone Lysine Demethylase Inhibitor X, ( E)-4-(Hydroxy(4-(4-((naphthalen-1-ylcarbamoyloxy)methyl)benzylamino)butyl)amino)-4-oxobut-2-enoic acid
• Empirical Formula (Hill Notation): C₂₇H₂₉N₃O₆
• CAS Number: 1310809-17-6
• Molecular Weight: 491.54
• MDL number: MFCD32671872
• UNSPSC Code: 12352200
• NACRES: NA.32

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: O=C(NC1=CC=CC2=C1C=CC=C2)OCC3=CC=C(CNCCCCN(O)C(/C=C/C(O)=O)=O)C=C3

Description

General description

A substrate (methyl lysine) and cofactor (α-ketoglutarate) mimicking bivalent benzylamino-butylamino-N-hydroxybutenoic acid compound that acts as a selective in vitro inhibitor of Jumonji domain-containing histone demethylases (JHDMs; IC₅₀ = 4.3, 3.4, 5.9, 10 and 43 µM for JMJD2A, JMJD2C, JMJD2E, PHF8 and JMJD3, respectively) over LSD1, asparaginyl and prolyl hydroxylases, and histone deacetylases (IC₅₀ = 54, 83, 31, 22, 620, 680 and >800 µM for PHD1, PHD2, PHD3, FIH, LSD1 and HDACs, respectively). The cellular active JHDM Inhibitor, Methylstat is also available (Cat. No. 420203).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Luo, X., et al. 2011. J. Am. Chem. Soc.133, 9451.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable