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Updated: Mar 8, 2026

Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays
Published on: June 13, 2019
The small molecule JIB-04 disrupts O2 binding in the Fe-dependent histone demethylase KDM4A/JMJD2A
Barbara Cascella1, Soon Goo Lee2, Sukrit Singh3
1Department of Chemistry, Washington University, St. Louis, Missouri 63130, USA. mirica@wustl.edu and Department of Biology, Washington University, St. Louis, Missouri 63130, USA. jjez@wustl.edu.
Abstract:
JIB-04, a specific inhibitor of the O2-activating, Fe-dependent histone lysine demethylases, is revealed to disrupt the binding of O2 in KDM4A/JMJD2A through a continuous O2-consumption assay, X-ray crystal structure data, and molecular docking.
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