化合物 EPZ015666|T6076|TargetMol

EPZ015666
1616391-65-1

￥587 2mg 起订

￥943 5mg 起订

￥1541 10mg 起订

上海更新日期：2024-09-29

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 EPZ015666

英文名称：: EPZ015666

CAS号：: 1616391-65-1

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：: 99.92%

产品类别：: 抑制剂

货号：: T6076

Product Introduction

Bioactivity

名称	EPZ015666
描述	EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.
细胞实验	EPZ015666 is dissolved in DMSO and stored, and then diluted with appropriate medium (final DMSO 0.2%) before use[1]. Cultured cells in linear/log-phase growth are split to a seeding density of 2×105 cells/mL in 2-20 mL of media, depending on the yield required at the end of the growth period. Compound is diluted in DMSO and added to each culture vessel with a final DMSO concentration of 0.2%. Cells are allowed to grow for 96 h undisturbed. At the conclusion of each treatment period, cells are harvested by centrifugation (5 min, 1,200 rpm), and cell pellets are rinsed once with PBS before being frozen on dry ice pending further processing. Long-term proliferation assays are performed on all MCL lines, with slight adjustments to initial seeding densities, depending on growth characteristics for each cell line. All assays are carried out for 12 d[1].
激酶实验	EPZ015666 is serially diluted threefold from 1,000 to 0.051 nM and spotted into a 384-well polypropylene V-bottom microplate. 3H-SAM is serially diluted twofold in assay buffer for a seven-point dilution series with a top concentration of 700 nM (final assay concentration). Reactions are initiated by the addition of 4 nM enzyme and 40 nM peptide (final assay concentrations for both). Reactions are incubated for 60 min and quenched by the addition of 10 μL per well of 600 μM unlabeled SAM in assay buffer (final assay concentration). For the peptide competition, EPZ015666 is serially diluted threefold from 1,000 to 0.051 nM and spotted into a 384-well polypropylene V-bottom microplate. Peptide is serially diluted twofold in assay buffer for a seven-point dilution series with a top concentration of 480 nM (final assay concentration). Reactions are initiated by the addition of 4 nM enzyme and 75 nM 3H-SAM (final assay concentrations for both). Reactions are incubated for 60 min, and the reactions are quenched by the addition of 10 μL per well of 600 μM unlabeled SAM in assay buffer (final assay concentration)[1].
体外活性	口服200 mg/kg EPZ015666对MCL异种移植动物模型具有强的抗肿瘤活性.
体内活性	EPZ015666显示有效的细胞活性,阻断SmD3的对称二甲基化,并抑制MCL细胞系的增殖,IC50为96-904 nM。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 45 mg/mL (117.36 mM) Ethanol : 45 mg/mL (117.4 mM)
关键字	inhibit \| Inhibitor \| GSK-3235025 \| EPZ015666 \| Histone Methyltransferase \| EPZ 015666 \| EPZ-015666 \| GSK 3235025
相关产品	Tazemetostat hydrobromide \| XY1 \| BML-278 \| OTS186935 FA \| MRTX-1719 \| MAK683 \| GSK126 \| Tazemetostat \| UNC 0631 \| AMI-1 free acid \| MS37452 \| Piribedil
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 高选择性抑制剂库 \| 抗衰老化合物库 \| 表观遗传库 \| 抗COVID-19化合物库 \| 共价抑制剂库 \| 细胞重编程化合物库

GSK3235025|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