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).

Packaged under inert gas

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

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

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

Toxicity: Standard Handling (A)