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We previously reported methylstat as a selective inhibitor of jumonji C domain-containing histone demethylases (JHDMs). Herein, we describe the synthesis of a fluorescent analogue of methylstat and its application as a tracer in fluorescence polarization assays. Using this format, we have evaluated the binding affinities of several known JHDM probes, as well as the native cofactor and substrate of JHDM1A. This fluorophore allowed a highly robust and miniaturized competition assay sufficient for high-throughput screening.

Original publication

DOI

10.1021/jm3018628

Type

Journal article

Journal

J Med Chem

Publication Date

27/06/2013

Volume

56

Pages

5198 - 5202

Keywords

Enzyme Inhibitors, Fluorescence Polarization, Fluorescent Dyes, Histone Demethylases, Reproducibility of Results