GSK J4 HCl

Description: GSK J4 is a novel, cell permeable, and potent prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase (KDM) JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and is inactive against a panel of demethylases of the JMJ family. GSK-J4 is used to probe the consequences of demethylation of H3K27me3. GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF). GSK-J4 (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis.

References: Nature. 2012 Aug 16; 488(7411):404-8; J Autoimmun. 2016 Dec; 75:105-117.