Jumonji Domain Containing 2A (JMJD2A) is a Jumonji C (JmjC) histone demethylase that catalyzes the demethylation of di- and trimethylated lysine 9 and lysine 36 of histone H3. The development of JmjC-specific inhibitors will be an important tool for studying the functions of the various JmjC enzymes. Cayman’s JMJD2A Inhibitor Screening Assay Kit provides a convenient fluorescence-based method for screening JMJD2A inhibitors. The assay is based on the multistep reaction in which JMJD2A first produces formaldehyde during the demethylation of the trimethylated peptide substrate, histone H3 trimethyl lys9, with the concomitant oxidation/decarboxylation of 2-oxoglutarate. The detection reaction involves the cyclization between formaldehyde and acetoacetanilide in the presence of ammonia. The resulting fluorescent product is analyzed using an excitation wavelength between 365-375 nm and an emission wavelength between 465-475 nm.

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