| Identification | Back Directory | [Name]
TP-064 | [CAS]
2080306-20-1 | [Synonyms]
TP-064
N-Methyl-N-((2-(1-(2-(methylamino)ethyl)piperidin-4-yl)pyridin-4-yl)methyl)-3-phenoxybenzamide
Benzamide, N-methyl-N-[[2-[1-[2-(methylamino)ethyl]-4-piperidinyl]-4-pyridinyl]methyl]-3-phenoxy-
TP-064,anticancer,inhibit,Histone Methyltransferase,Inhibitor,BAF155,TP064,MED12,CARM1,dimethylation,PRMT4 | [Molecular Formula]
C28H34N4O2 | [MDL Number]
MFCD30720896 | [MOL File]
2080306-20-1.mol | [Molecular Weight]
458.6 |
| Chemical Properties | Back Directory | [Boiling point ]
642.8±55.0 °C(Predicted) | [density ]
1.134±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml | [form ]
A crystalline solid | [pka]
10.48±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
TP-064 (10 mg/kg; i.p.; 3 times in 5 days) induces peritonitis-associated neutrophilia in C57BL/6 mice[2]. | [IC 50]
PRMT4: <10 nM (IC50); PRMT6: 1300 μM (IC50) | [storage]
Store at -20°C | [References]
[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 |
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