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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-EPZ020411
EPZ020411

Chemical Structure : EPZ020411

CAS No.: 1700663-41-7

EPZ020411 (EPZ-020411)

货号: PC-43300Not For Human Use, Lab Use Only.

EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10 nM, displays 10-fold and 20-fold selectivity over PRMT1/8, and >100-fold over other histone methyltransferases (PRMT3/4/5/7).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10 nM, displays 10-fold and 20-fold selectivity over PRMT1/8, and >100-fold over other histone methyltransferases (PRMT3/4/5/7).
EPZ020411 dose-dependently decreases H3R2 methylation A375 cell line with IC50 of 0.637 uM, with no affect levels of PRMT6 expression.
EPZ020411 exhibits good bioavailability following subcutaneous dosing in rats making it a suitable tool for potential in vivo target validation studies.

物理化学性质&存储条件

分子量 442.5942
分子式 C25H38N4O3
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

10 mM in DMSO

Chemical Name/SMILES

1,2-Ethanediamine, N1,N2-dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-

参考文献

1. Mitchell LH, et al. ACS Med Chem Lett. 2015 Apr 6;6(6):655-9.

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