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TP-064
- Development stage
- Discontinued
- Lead developer
- Takeda
- Modality
- Small Molecules
01
Overview
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
02
Targets
PRMT4 (Protein arginine N-methyltransferase 4)PRMT6
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