JIB-04 (199596-05-9) is a novel specific inhibitor of the Jumonji family of histone demethylases in vitro, in cancer cells and in tumors in vivo. IC50 = 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively. Reduces tumor burden and prolongs life in a mouse model.1 Suppresses translation initiation and enhances mTOR inhibitor sensitivity.2 Inhibits the growth of temozolomide-resistant glioblastoma cells and crosses the blood brain barrier.3
1) Wang et al. (2013), A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth; Nature Commun., 4 2035
2) Rechem et al. (2015), Lysine demethylase KDM4A associates with translocation machinery and regulates protein synthesis; Cancer Discov., 5 255
3) Banelli et al. (2017), Small molecules targeting histone demethylase genes (KDMs) inhibit growth of temozolomide-resistant glioblastoma cells; Oncotarget, 8 34896
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