MS37452

MS37452 is a small molecule and a selective, competitive inhibitor of the chromodomain of Chromobox homolog 7 (CBX7), with a Kd of approximately 27.7 μM and Ki of 43 μM[1][2][3]. CBX7 is part of the Polycomb Repressive Complex 1 (PRC1) and plays an important role in gene transcription regulation by recognizing histone H3 trimethyl lysine 27 (H3K27me3). By binding to the methyl-lysine binding pocket on CBX7, MS37452 disrupts its interaction with H3K27me3, leading to derepression of target genes such as p16/CDKN2A at the INK4A/ARF locus. This mechanism has been shown to upregulate p16/CDKN2A expression in prostate cancer cells and reduce cell viability when combined with doxorubicin in glioblastoma models[2][5]. The compound has also demonstrated potential utility in reversing steroid resistance in asthma models by inhibiting CBX7 activity[6]. No clinical trials or approved therapeutic uses are reported; it is used for research purposes only.

Other names

1-(2,3-Dimethoxybenzoyl)-4-[(3-methylphenoxy)acetyl]-piperazine