JIB-04

JIB-04 is a pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC₅₀s values = 230, 340, 435, 445, 855 and 1,100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively).¹ It does not inhibit histone deacetylases and has minimal effect on the iron-containing enzymes methylcytosine dioxygenase TET1 and hypoxia-inducible factor prolyl hydroxylase 2.¹ JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells.^1,2 It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.¹

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1. Wang, L., Chang, J., Varghese, D., et al. A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth. Nat. Commun. 4, 2035 (2013).

2. Easmon, J., Heinisch, G., Pürstinger, G., et al. Azinyl and diazinyl hydrazones derived from aryl N-heteroaryl ketones: Synthesis and antiproliferative activity. J. Med. Chem. 40(26), 4420-4425 (1997).