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CAS No.: 1616391-65-1

EPZ015666 Catalog No. CSN16273

Synonyms: GSK3235025

EPZ015666 is a selective inhibitor of PRMT5 with Ki of 5 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PRMT5

Ki:5nM
描述The mammalian protein arginine methyltransferases are a group of nine enzymes that perform NG-mono methylation-, asymmetric-, or symmetric dimethylation of arginine residues on a range of nuclear and cytoplasmic protein substrates. Protein arginine methyltransferase-5 (PRMT5) is one member of this group which catalyzes the transfer of up to two methyl groups to arginine residues, forming ω-NG-monomethyl arginine and symmetrical ω-NG-dimethyl arginine on protein substrates^[3]. EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity with IC₅₀ of 22 nM^[4]. SCID mice bearing subcutaneous mantle cell lymphoma cell lines Z-138 and Maver-1 xenografts were orally given EPZ015666 on four doses: 25, 50, 100 and 200 mg/kg twice daily. Dosing at 200 mg/kg induced tumor stasis in Z-138 cells, with >93% tumor-growth inhibition (TGI) after 21 d, whereas Maver-1 cells showed >70% TGI^[4]. EPZ0156660 (0 to 10 uM) dose-dependently inhibited the proliferation of multiple myeloma cell lines^[5]. EPZ015666 at 5 uM also inhibited growth in patient multiple myeloma (pMM) cells cultured on a BMSCs monolayer, and also induced apoptosis of pMM cells within bone marrow mononuclear cell cultures^[5]. 10 uM -EPZ treatment significantly suppressed the proliferation of several human glioblastoma cell lines: GI261, T98G, U-87 MG and A172, with loss of active S phase cells and accumulation of G2/M populations, but did not induce apoptosis^[6].
作用机制EPZ015666 binds in the peptide-binding site of PRMT5, including in the pocket occupied by the substrate arginine side chain.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6079 mL
- 13.0397 mL
- 26.0794 mL
- 5 mM
- 0.5216 mL
- 2.6079 mL
- 5.2159 mL
- 10 mM
- 0.2608 mL
- 1.3040 mL
- 2.6079 mL

技术信息

CAS号

1616391-65-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H25N5O3

运输

蓝冰

分子量

383.44

别名

GSK3235025

溶解度

DMSO	74.0 mg/mL (193.0 mM) warming
Water	Insoluble
Ethanol	39.0 mg/mL (101.7 mM) warming

动物实验配方

2% DMSO+30% PEG 300+water

5 mg/mL

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