199596-05-9

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

JIB-04 has been used in sulforhodamine B cell growth assay. It has also been used as a control to determine the inhibitory action of ML324 on KDM4A (histone lysine demethylase 4A).

JIB-04 is a specific inhibitor of Jumonji demethylases.

JIB-04 is a selective inihibitor of Jumonji demethylases without inhibiting other α-ketoglutarate-dependent hydroxylases or histone-modifying enzymes including amine oxidase LSD1 (also known as KDM1A), which demethylates histone lysines. JIB-04 is a pan-inhibitor of Jumonji demethylases with JARID1A (KDM5A) being the most sensitive (IC50=230 nM) followed by JMJD2D (IC50=290 nM) and JMJD3 (KDM6B) and JMJD2C (KDM4C) more resistant (IC50 855 and 1100 nM, respectively). JIB-04 selectively inhibited viability of several human cancer cell lines with little toxicity towards normal cells, and also diminished tumor growth in two separate xenograft mouse models.

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1) Wang?et al.?(2013),?A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth; Nature Commun., 4?2035