产品
编 号:F594618
分子式:C28H34N4O2
分子量:458.6
产品类型
结构图
CAS No: 2080306-20-1
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产品详情
生物活性:
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.
体内研究:
TP-064 (10 mg/kg; i.p.; 3 times in 5 days) induces peritonitis-associated neutrophilia in C57BL/6 mice.
体外研究:
TP-064 (1 μM; 72 hours) treatment reduces the proportion of NCI-H929 cells in S and G2/M phases while increasing the G1 phase fraction.TP-064 (0.03-3 μM; 72 hours) treatment reduces dimethyl-BAF155 level in a dose-dependent manner in both TP-064-sensitive and -insensitive cells.TP-064 (10 nM-10 μM; 6 days) treatment inhibits the growth of NCI-H929, RPMI8226, and MM.1R cells in a dose-dependent manner, but had no effect on acute myeloid leukemia, colon cancer, or lung cancer cell lines.