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Quantitative Analysis of Histone Demethylase Probes Using Fluorescence Polarization

Wenqing Xu, Jessica D Podoll, Xuan Dong, Anthony Tumber, Udo Oppermann, Xiang Wang

J Med Chem. 2013 Jun 27;56(12):5198-202.

PMID: 23725560

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1310877952 Methylstat Methylstat 1310877-95-2 Price
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