化合物 GSK2879552|T3677|TargetMol

GSK2879552
1401966-69-5

￥793 5mg 起订

￥389 2mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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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 GSK2879552

英文名称：: GSK2879552

CAS号：: 1401966-69-5

品牌：: TargetMol

产地：: 美国

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

纯度规格：: 99.22%

产品类别：: 抑制剂

货号：: T3677

Product Introduction

Bioactivity

Name	GSK2879552
Description	GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor, with potential antineoplastic activity.
Cell Research	The optimal cell seeding is determined empirically for all cell lines by examining the growth of a wide range of seeding densities in a 384-well format to identify conditions that permitted proliferation for 6?days. Cells are then plated at the optimal seeding density 24?h before treatment (in duplicate) with a 20-point twofold dilution series of GSK2879552 or 0.15% DMSO. Plates are incubated for 6?days at 37°C in 5% CO2. Cells are then lysed with CellTiter-Glo (CTG) (Promega) and chemiluminescent signal is detected with a TECAN Safire2 microplate reader. In addition, an untreated plate of cells is harvested at the time of compound addition (T0) to quantify the starting number of cells. CTG values obtained after the 6?day treatment are expressed as a percent of the T0 value and plotted against compound concentration. Data are fit with a four-parameter equation to generate a concentration response curve and the concentration of GSK126 required to inhibit 50% of growth (growth IC50) is determined.(Only for Reference)
Kinase Assay	LSD1 enzyme assay: LSD1 activity was measured using a horseradish peroxidase (HRP) coupled assay with amplex red as an electron donor. The formation of product over time is measured using fluorescence intensity, Ex 531 nm and Em 595 nm, in a PerkinElmer EnVision plate reader. Final assay conditions are: 5 nM LSD1, 2.5 μM H3K4me2 peptide, 50 mM HEPES pH 7, 1 U/ml of HRP, 1 mM CHAPS, 0.03% dBSA and 10 μM amplex red.
In vitro	在165个细胞系中，GSK2879552对9/28个小细胞肺癌(SCLC)系和20/29个AML系的生长抑制率在40%至100%之间。对于对GSK2879552产生生长抑制反应的SCLC细胞系和初级样本子集，显示出一组特征探针的DNA低甲基化。[1]
In vivo	在携带SCLC异种移植瘤的小鼠中，GSK2879552（1.5 mg/kg，p.o.）展现了17%-83%的肿瘤生长抑制效果。[1]
Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : <1 mg/mL DMSO : 27 mg/mL (74.1 mM)
Keywords	Inhibitor \| inhibit \| Histone Demethylase \| GSK-2879552 \| GSK2879552 \| GSK 2879552
Inhibitors Related	DDP-38003 dihydrochloride \| Zavondemstat \| FY-21 \| KDM4-IN-4 \| Procaine hydrochloride \| JIB-04 \| GSK-J4 \| LSD1-IN-24 \| Daminozide \| AS8351 \| GSK-LSD1 dihydrochloride \| Tranylcypromine hemisulfate

GSK 2879552 HCl|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
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