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). 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. JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells. It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.Formal Name: phenyl-2-pyridinyl-methanone, (E,E)-2-(5-chloro-2-pyridinyl)hydrazone. CAS Number: 199596-05-9. Synonyms: JHDM Inhibitor VII, NSC 693627. Molecular Formula: C17H13ClN4. Formula Weight: 308.8. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 240, 334 nm. SMILES: ClC(C=C1)=CN=C1N/N=C(C2=CC=CC=C2)/C3=CC=CC=N3. InChi Code: InChI=1S/C17H13ClN4/c18-14-9-10-16(20-12-14)21-22-17(13-6-2-1-3-7-13)15-8-4-5-11-19-15/h1-12H,(H,20,21)/b22-17+. InChi Key: YHHFKWKMXWRVTJ-OQKWZONESA-N.