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Overview
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Background
IOX 1 (5-carboxy-8HQ) is an inhibitor of histone demethylase JMJD with IC50 values of 0.2 μM for JMJD2E [1].
The Jumonji domain (JMJD) is a histone demethylase and acts as a transcriptional repressor.
IOX 1 is a histone demethylase JMJD inhibitor. In the FDH-coupled assay, IOX 1 inhibited JMJD2E with IC50 value of 0.2 μM. In MALDI-TOF MS assay, IOX 1 inhibited JMJD2E, JMJD2A, FIH and PHD2 with IC50 values of 2.4, 1.7, 20.5 and 14.3 μM, respectively. In HeLa cells, IOX 1 increased H3K9me3 fluorescence intensity, suggesting that IOX 1 inhibited H3K9me3 demethylation induced by JMJD2A with IC50 value of 86.5 μM. Also, IOX 1 exhibited cytotoxicity with IC50 value of 291.6 μM [1].
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