EPZ015666 (GSK3235025)

EPZ015666 (GSK3235025)是一种有效的,选择性且口服生物有效的 PRMT5 抑制剂,Ki 为 5 nM,选择性比其它 PMTs 高 20,000多倍。

EPZ015666 (GSK3235025) Chemical Structure

EPZ015666 (GSK3235025) Chemical Structure

CAS: 1616391-65-1

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1875.51 现货
5mg RMB 1602.26 现货
25mg RMB 4906.16 现货
100mg RMB 7944.3 现货
1g RMB 16134.3 现货
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客户使用Selleck的EPZ015666 (GSK3235025)发表文献27

客户使用该产品的1个实验数据

产品质控

批次: 纯度: >97%
97

EPZ015666 (GSK3235025)相关产品

Histone Methyltransferase抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
MDA-MB-468 Function assay 48 h inhibits PRMT5 activity 30957988
MDA-MB-453 Cell viability assay IC50=1 μM 30957988
HCC1954 Cell viability assay IC50=0.8 μM 30957988
HCC38 Cell viability assay IC50=2.2 μM 30957988
MDA-MB-468 Cell viability assay IC50=2.2 μM 30957988
MCF7 Cell viability assay IC50=2.6 μM 30957988
SKBR3 Cell viability assay IC50=3.9 μM 30957988
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [3H]-SAM by Topcount method, IC50=0.022μM 29628326
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [4H]-SAM by Topcount method, IC50=0.022μM 29628326
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [5H]-SAM by Topcount method, IC50=0.022μM 30366617
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [6H]-SAM by Topcount method, IC50=0.022μM 30366617
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [7H]-SAM by Topcount method, IC50=0.047μM 30366617
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [8H]-SAM by Topcount method, IC50=0.047μM 30366617
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [9H]-SAM by Topcount method, IC50=0.047μM 30605830
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [10H]-SAM by Topcount method, IC50=0.047μM 30605830
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [11H]-SAM by Topcount method, IC50=0.047μM 30605830
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [12H]-SAM by Topcount method, IC50=0.047μM 30605830
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [13H]-SAM by Topcount method, IC50=0.096μM 29870258
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [14H]-SAM by Topcount method, GI50=0.106μM 30605830
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [15H]-SAM by Topcount method, GI50=0.106μM 30605830
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [16H]-SAM by Topcount method, GI50=0.212μM 30605830
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [17H]-SAM by Topcount method, GI50=0.212μM 30605830
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [18H]-SAM by Topcount method, IC50=0.45μM 29870258
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [19H]-SAM by Topcount method, IC50=0.96μM 30366617
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [20H]-SAM by Topcount method, IC50=1.1μM 30366617
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [21H]-SAM by Topcount method, IC50=1.8μM 30366617
Sf9 Function assay Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [22H]-SAM by Topcount method, IC50=2.6μM 30366617
点击查看更多细胞系数据

生物活性

产品描述 EPZ015666 (GSK3235025)是一种有效的,选择性且口服生物有效的 PRMT5 抑制剂,Ki 为 5 nM,选择性比其它 PMTs 高 20,000多倍。
靶点
PRMT5 [1]
(Cell-free assay)
5 nM(Ki)
体外研究(In Vitro)
体外研究活性

EPZ015666(GSK3235025)表现出有效的细胞活性,阻断SmD3的对称二甲基化,并抑制MCL细胞系(Z-138,Granta-519,Maver-1,Mino,和 Jeko-1)的增殖,IC50 为96-904 nM。[1]

细胞实验 细胞系 MCL细胞系(Z-138,Granta-519,Maver-1,Mino,和 Jeko-1)
浓度 5 μM
孵育时间 12天
方法

--

实验图片 检测方法 检测指标 实验图片 PMID
Western blot PRMT5 / H3R8me2s H4R3me2s 30957988
Immunofluorescence IKKβ 29158558
Growth inhibition assay Cell viability 30957988
体内研究(In Vivo)
体内研究活性

EPZ015666 (200 mg/kg, p.o.)在MCL异种移植动物模型中表现出强的抗肿瘤活性。[1]

动物实验 Animal Models MCL (Z-138,和 Maver-1) 异种移植模型
Dosages 200 mg/kg BID
Administration p.o.

化学信息&溶解度

分子量 383.44 分子式

C20H25N5O3

CAS号 1616391-65-1 SDF Download EPZ015666 (GSK3235025) SDF
Smiles C1CN(CC2=CC=CC=C21)CC(CNC(=O)C3=CC(=NC=N3)NC4COC4)O
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 77 mg/mL ( (200.81 mM); DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 26 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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