TP-064 是一种有效的选择性蛋白精氨酸甲基转移酶 4 (PRMT4; CARM1) 抑制剂 (IC₅₀ <10 nM)。TP-064 抑制 BAF155 (IC₅₀ 为 340 nM) 和 MED12 (IC₅₀ 为 43 nM) 的二甲基化。TP-064 对除 PRMT6 (IC₅₀ 为 1.3 μM) 外的其他家族成员无活性。TP-064 具有抗癌活性。

TP-064 is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC 50 <10 nM). TP-064 inhibits dimethylation of BAF155 (IC 50 of 340 nM) and MED12 (IC 50 of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC 50 of 1.3 μM). TP-064 has anticancer activities.

Solid

PRMT4 <10 nM (IC50) PRMT6 1300 μM (IC

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. has not independently confirmed the accuracy of these methods. They are for reference only.

TP-064 (10 mg/kg; i.p.; 3 times in 5 days) induces peritonitis-associated neutrophilia in C57BL/6 mice. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.
[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.

In Vitro: DMSO : 125 mg/mL (272.57 mM; ultrasonic and warming and heat to 60°C)H₂O : ≥ 50 mg/mL (109.03 mM)