MS37452

MS37452 is a competitive inhibitor of CBX7 (Chromobox homolog 7) chromodomain binding to trimethylated lysine 27 of histone 3 (H3K27me3). It inhibits CBX7-H3K27me3 binding with a Ki of 43.0 μM. At 250 µM, it derepresses transcription of Polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in PC3 prostate cancer cells.