JIB-04
pan-JUMONJI histone demethylase inhibitor / 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
Biochemicals & reagents
199596-05-9
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 translation 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
-20°C
TARGET: Protein demethylase -- PATHWAY: Chromatin; mTOR; Posttranslational modification -- RESEARCH AREA: Epigenetics -- DISEASE AREA: Cancer