JIB-04

Aliases: JIB-04, JHDM Inhibitor VII, (E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine
Catalog No: 14134 Format: 25 mg $225 Buy
Catalog No: 14135 Format: 5 mg $65 Buy
Application: Histone Methylation (HMT & HDM)

Chemical Properties

MW = 308.8
C17H13ClN4
CAS 199596-05-9
>98% (TLC); NMR (Conforms)

Description

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 (ref 1). Suppresses translation initiation and enhances mTOR inhibitor sensitivity (ref 2). Inhibits the growth of temozolomide-resistant glioblastoma cells and crosses the blood brain barrier (ref 3).

Contents

Yellow powder. May be dissolved in DMSO (30 mg/ml).

Storage Conditions

Store desiccated as supplied at -20°C for up to 2 years. Store solutions at -20°C for up to 2 months.

References

1. L Wang et al. Nature Commun. 2013, 4:2035
2. C Can Rechem et al. Cancer Discov. 2015, 5:255
3. B Banelli et al. Oncotarget 2017, 8:34896

 
Chemical structure of JIB-04.

Chemical structure of JIB-04.