AS-8351

AS-8351 is a small molecule epigenetic modulator that acts as a potent and selective inhibitor of the histone lysine demethylase KDM5B (also known as JARID1B). KDM5B is a member of the JARID1 family of demethylases that specifically targets tri- and di-methylated lysine 4 on histone H3 (H3K4me3/2), a modification typically associated with active transcription. By inhibiting KDM5B, AS-8351 promotes the maintenance of H3K4 methylation levels, thereby influencing gene expression patterns involved in cell differentiation and proliferation. Research has demonstrated its potential in oncology, particularly in pediatric brain tumors like glioblastoma and medulloblastoma, where it has shown efficacy in suppressing tumor organoid growth both alone and in combination with radiation therapy. It is primarily utilized as a chemical probe in preclinical research.