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
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