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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-TP-064
TP-064

Chemical Structure : TP-064

CAS No.: 2080306-20-1

TP-064 (TP064)

货号: PC-63546Not For Human Use, Lab Use Only.

TP-064 is a potent, selective, and cell-active inhibitor of PRMT4 with IC50 of <10 nM and Kd of 7.1 nM, shows high selectivity (>100-fold) for PRMT4 over other PRMTs.

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10 mg ¥1180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TP-064 is a potent, selective, and cell-active inhibitor of PRMT4 with IC50 of <10 nM and Kd of 7.1 nM.
TP-064  shows high selectivity (>100-fold) for PRMT4 over other PRMTs.
TP-064  reduces dimethylation of BAF155 (IC50=340±30 nM) and MED12 (IC50=43±10 nM) in a dose-dependent manner in cell-baed assays.
TP-064  inhibits the proliferation of a subset of multiple myeloma cell lines (NCI-H929, RPMI8226, Cell IC50 of 379 and 886 nM, respectively) with affected cells arrested in G1 phase of the cell cycle, but has no effect on acute myeloid leukemia, colon cancer, or lung cancer cell lines.

物理化学性质&存储条件

分子量 458.606
分子式 C28H34N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

250 mM in DMSO (114.65 mg/mL)

Chemical Name/SMILES

N-methyl-N-((2-(1-(2-(methylamino)ethyl)piperidin-4-yl)pyridin-4-yl)methyl)-3-phenoxybenzamide

参考文献

1. Nakayama K, et al. Oncotarget. 2018 Apr 6;9(26):18480-18493.

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