JIB-04

A pan Jumonji histone demethylase inhibitor

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

308.8

≥95%

JHDM Inhibitor VII|NSC 693627

ClC(C=C1)=CN=C1N/N=C(C2=CC=CC=C2)/C3=CC=CC=N3

C17H13ClN4

199596-05-9

≥ 4 years

DMF: 20 mg/ml DMSO: 5 mg/ml Ethanol: 1 mg/ml

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, 1-24 (2013).
2.Easmon, J.,Heinisch, G.,Pürstinger, G., et al. Azinyl and diazinyl hydrazones derived from aryl N-heteroaryl ketones: Synthesis and antiproliferative activity. Journal of Medicinal Chemistry 40(26), 4420-4425 (1997).