GSK J4

GSK J4 is a cell-permeable ethyl ester prodrug of GSK J1, a potent and selective inhibitor of the H3K27-specific histone demethylases JMJD3 (KDM6B) and UTX (KDM6A). Developed by GSK as a chemical probe, GSK J4 is rapidly hydrolyzed within cells to its active form, GSK J1, which competes with alpha-ketoglutarate to inhibit demethylase activity. This inhibition leads to increased levels of the repressive H3K27me3 histone mark, thereby modulating the transcription of genes involved in inflammation and oncogenesis. GSK J4 has been extensively studied in preclinical models for its anti-tumor effects, particularly in pediatric brain tumors such as diffuse intrinsic pontine glioma (DIPG), glioblastoma, and medulloblastoma, as well as for its ability to suppress pro-inflammatory cytokine production in macrophages.

Other names

GSK J4 HClGSK J4 hydrochlorideGSK-J4 HClGSK-J-4 HClGSK-J 4 HCl