化合物 EPZ005687|T1905|TargetMol

EPZ005687
1396772-26-1

￥191 1mg 起订

￥493 5mg 起订

￥756 10mg 起订

上海更新日期：2024-09-30

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 EPZ005687

英文名称：: EPZ005687

CAS号：: 1396772-26-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.66%

产品类别：: 抑制剂

货号：: T1905

Product Introduction

Bioactivity

Name	EPZ005687
Description	EPZ005687 is a potent and selective inhibitor of EZH2.
Cell Research	Plating densities are determined for each cell line on the basis of linear log-phase growth. Cells are counted and split back to the original plating density in fresh medium with EPZ005687 on days 4 and 7.(Only for Reference)
Kinase Assay	Biochemical Enzyme Assays: Compound is incubated for 30 min with 40 μL per well of 5 nM PRC2 (final assay concentration in 50 μL is 4 nM ) in 1X assay buffer (20 mM Bicine [pH 7.6], 0.002% Tween-20, 0.005% Bovine Skin Gelatin and 0.5 mM DTT). 10 μL per well of substrate mix comprising assay buffer 3 H-SAM, unlabeled SAM, and peptide representing histone H3 residues 21-44 containing C-terminal biotin (appended to a C-terminal amide-capped lysine) are added to initiate the reaction (both substrates are present in the final reaction mixture at their respective Km values, an assay format referred to as ‘‘balanced conditions''. The final concentrations of substrates and methylation state of the substrate peptide are indicated for each enzyme Reactions are incubated for 90 min at room temperature and quenched with 10 μL per well of 600 μM unlabeled SAM, Then transferred to a 384-well flashplate and washed after 30 min.
In vitro	EPZ005687直接抑制PRC2酶活性,并且不会破坏PRC2亚基之间的蛋白质 - 蛋白质相互作用。EPZ005687显示对PRC2酶活性的浓度依赖性抑制,其IC 50值为54 nM。EPZ005687减少各种淋巴瘤细胞中的H3K27甲基化。它在杂合Tyr641或Ala677突变细胞中显示强烈的细胞杀伤作用,对野生型细胞的增殖影响最小。在Tyr641突变型淋巴瘤细胞系中,EPZ005687可导致已知EZH2靶基因的脱抑制,并影响由EZH2 Tyr641突变体特异性抑制的基因。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 5.4 mg/mL (10 mM)
Keywords	Inhibitor \| EPZ-005687 \| Histone Methyltransferase \| EPZ 005687 \| inhibit \| EPZ005687
Inhibitors Related	Tazemetostat hydrobromide \| XY1 \| BML-278 \| MRTX-1719 \| MAK683 \| GSK126 \| Tazemetostat \| EPZ015666 \| UNC 0631 \| AMI-1 free acid \| MS37452 \| Piribedil
Related Compound Libraries	Inhibitor Library \| Anti-Cancer Active Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Anti-Aging Compound Library \| Highly Selective Inhibitor Library \| Stem Cell Differentiation Compound Library \| NO PAINS Compound Library \| Hematonosis Compound Library \| Target-Focused Phenotypic Screening Library

EPZ005687|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务