A chemical probe of CARM1 alters epigenetic plasticity against breast cancer cell invasion

CARM1 is a cancer-relevant protein arginine methyltransferase that regulates many aspects of transcription. Its pharmacological inhibition is a promising anti-cancer strategy. Here SKI-73 ( 6a in this work) is presented as a CARM1 chemical probe with pro-drug properties. SKI-73 ( 6a ) can rapidly penetrate cell membranes and then be processed into active inhibitors, which are retained intracellularly with 10-fold enrichment for several days....