MS37452 is a small-molecule modulator of methyl-lysine binding for CBX7 chromodomain, disrupts CBX7-H3K27me3 and H3K9me3 binding with Ki of 43.0 and 55.3 uM, respectively
MS37452 derepresses transcription of Polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells.
MS37452 disrupts CBX7 binding to the INK4A/ARF locus, subsequently resulting in transcriptional de-repression of its target genes p14/ARF and p16/INK4a in PC3 cells.
