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JIB-04 is a small molecule inhibitor of Jumonji histone demethylase with IC50 values of [1].

JIB-04 is a pyridine hydrazone. It is a pan -selective inhibitor of Jumonji histone demethylases. In a sensitive ELISA assay, JIB-04 inhibits JARID1A, JMJD2A, JMJD2B, JMJD2C, JMJD2E and JMJD3 with IC50 values of 230nM, 445nM, 435nM, 1100nM, 340nM and 855nM, respectively. Among the JMJD2 (KDM4) subfamily, JMJD2D has highest sensitivity. JIB-04 inhibits Jumonji demethylases in a unique manner. It is found not to be a competitive inhibitor of α-ketoglutarate in the competition assay [1].

JIB-04 shows consistently selective for cancer cells over normal cells. It has efficacy in cultured lung and prostate cancer lines with IC50 values as low as 10nM. JIB-04 is also effective in controlling lung cancer growth in animals. It significantly suppresses tumor growth of H358 and A549 lung cancer cell xenografts in mice with IC50 values of 100nM and 250nM, respectively. Furthermore, the anti-proliferation activity of JIB-04 results in a reduction in cancer-induced death rates in mice [1].

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