2080306-20-1

TP-064 is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC50 <10 nM). TP-064 inhibits dimethylation of BAF155 (IC50 of 340 nM) and MED12 (IC50 of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC50 of 1.3 μM). TP-064 has anticancer activities[1].

PRMT4: <10 nM (IC₅₀); PRMT6: 1300 μM (IC₅₀)

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[1] Kazuhide Nakayama, et al. TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma. Oncotarget. 2018 Apr 6;9(26):18480-18493. DOI:10.18632/oncotarget.24883
[2] Yiheng Zhang, et al. PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo. Biochim Biophys Acta Mol Basis Dis. 2021 Jul 24;1867(11):166212. DOI:10.1016/j.bbadis.2021.166212