GSK4J4

GSK4J4 is a cell-permeable small molecule inhibitor that targets the H3K27-specific histone demethylases JMJD3 (KDM6B) and UTX (KDM6A). It is the ethyl ester prodrug of GSK4J1, designed to improve cellular uptake. GSK4J4 acts as a competitive inhibitor with respect to alpha-ketoglutarate, effectively blocking the demethylation of trimethylated lysine 27 on histone H3 (H3K27me3). This inhibition maintains repressive chromatin states, thereby modulating the expression of genes involved in inflammation and cellular differentiation. Originally developed by GSK as a chemical probe, GSK4J4 is widely utilized in preclinical research to explore the therapeutic potential of targeting epigenetic regulators in diseases such as atherosclerosis, cancer, and inflammatory disorders.

Other names

GSK 4J4GSK4J4GSK-4J4GSK4J1 ethyl esterGSK-4J1 ethyl esterGSK 4J1 ethyl ester