JIB-04 (NSC693627) --- Jumonji Histone Demethylase Inhibitor

Overview
Catalog #	bs-60132c-2mg-solid
Product Name	JIB-04 (NSC693627) --- Jumonji Histone Demethylase Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 308.76 Formula: C17 H13 Cl N4 CAS Number: 199596-05-9 InChi Key: YHHFKWKMXWRVTJ-OQKWZONESA-N InChi: 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+ Smiles: ClC1=CN=C(C=C1)N/N=C(/C1C=CC=CN=1)\C1C=CC=CC=1 Purity: 98.0 Solubility: DMSO up to 50 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	JIB-04 (NSC693627, E-isomer) is a potent, selective and cell permeable Jumonji histone demethylase inhibitor. Unlike the other known inhibitors, JIB-04 is not a competitive inhibitor of a-ketoglutarate. It inhibits the demethylase activity of Jumonji enzymes in vitro, with IC50 ~230 nM for JARID1A (KDM5A), ~440 nM for JMJD2A (KDM4A) and JMJD2B (KDM4B), ~340 nM for JMJD2E (KDM2E), and ~1 µM for JMJD3 (KDM6B) and JMJD2C (KDM4C). JIB-04 blocks Jumonji demethylase activity in cells and consequently inhibits cell growth, without affecting other a-ketoglutarate-dependent hydroxylases or histone-modifying enzymes, especially HDACs. JIB-04 alters transcriptional programs in cancer but not in normal cells, leading to cancer-specific cell death. Importantly, in vivo, JIB-04 lowers histone demethylase activity in tumors, reduces tumor burden and prolongs survival of mice in an aggressive breast cancer model.