TP-064

TP-064 is a potent and selective small molecule inhibitor of Protein Arginine Methyltransferase 4 (PRMT4), also known as Coactivator Associated Arginine Methyltransferase 1 (CARM1). Developed by Takeda Pharmaceutical Company Limited, it inhibits the methyltransferase activity of PRMT4 with high potency (IC50 < 10 nM) and selectivity over other PRMT family proteins. Preclinical studies demonstrated its anti-proliferative effects in a subset of multiple myeloma cell lines, arresting affected cells in the G1 phase of the cell cycle. It also reduced arginine dimethylation of PRMT4 substrates like BAF155 and MED12.

Other names

N-methyl-N-((2-(1-(2-(methylamino)ethyl)piperidin-4-yl)pyridin-4-yl)methyl)-3-phenoxybenzamide