A substrate (methyl lysine) and cofactor (a-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 43uM 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 >800uM for PHD1, PHD2, PHD3, FIH, LSD1 and HDACs, respectively). The cellular active JHDM Inhibitor, Methylstat is also available.
Formula:C₂₇H₂₉N₃O₆
Solubility:DMSO
Molecular Weight:491.5
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
