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GSK126

GSK126

产品编号 T2079   CAS 1346574-57-9
别名: GSK2816126A, EZH2 inhibitor

GSK126 (GSK2816126A) 是一种选择性的EZH2甲基转移酶抑制剂,IC50为 9.9 nM。

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GSK126 Chemical Structure
GSK126, CAS 1346574-57-9
规格 价格/CNY 货期 数量
2 mg ¥ 365 现货
5 mg ¥ 658 现货
10 mg ¥ 971 现货
50 mg ¥ 2,431 现货
100 mg ¥ 3,355 现货
200 mg ¥ 4,990 现货
1 mL * 10 mM (in DMSO) ¥ 728 现货
其他形式的 GSK126:
产品目录号及名称: GSK126 (T2079)
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选择批次  
纯度: 99.67%
纯度: 99.59%
纯度: 99.43%
纯度: 99.31%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).
靶点活性 EZH2:9.9 nM
体外活性 在负荷人类B细胞淋巴瘤细胞和人弥漫性大细胞异种移植物的小鼠体内,用GSK126(150 mg/kg/d, i.p.)进行处理, 能够降低H3K27me3,从而抑制肿瘤细胞增殖.
体内活性 在EZH2野生型和突变型DLBCL细胞系中,GSK126能够有效地抑制H3K27me3和H3K27me2,抑制细胞增殖。在亲本H2087细胞中,GSK126通过下调VEGF-A和磷酸化Ser(473)-AKT的表达抑制细胞增殖,迁移和转移。在A687V EZH2突变细胞中,GSK126下调H3K27me3,抑制细胞增殖。
激酶实验 EZH2 assay: The five-member PRC2 complex (Flag–EZH2, EED, SUZ12, AEBP2, RbAp48) containing either wild-type or mutant EZH2 is prepared. GSK126 is dissolved in DMSO and tested at concentrations of 0.6?nM to 300?nM with a final DMSO concentration of 2.5%. In contrast to wild-type EZH2 which prefers H3K27me0 as a substrate in vitro, EZH2 Y641 mutants prefer H3K27me2 and have little activity with H3K27me0 or H3K27me1. The A677 g mutant is distinct from both the wild-type and Y641 mutant forms of EZH2 in that it efficiently methylates H3K27me0, H3K27me1, and H3K27me2; therefore, histone H3 peptides (residues 21–44; 10?μM final) with either K27me0 (wild type, A677 g EZH2), K27me1 (A677 g EZH2), or K27me2 (A677 g, Y641N, Y641C, Y641H, Y641S and Y641F EZH2) are used as methyltransferase substrates. GSK126 is added to plates followed by addition of 6?nM EZH2 complex and peptide. As the potency of GSK126 is at or near the tight binding limit of an assay run at [SAM] = Km, IC50 values are measured at a high concentration of the competitive substrate SAM relative to its Km (7.5 μM SAM where the SAM Km is 0.3?μM). Under these conditions, the contribution from the enzyme concentration becomes relatively small and accurate estimates of Ki can be calculated. Reactions are initiated with [3H]-SAM, incubated for 30 min, quenched with the addition of 500-fold excess unlabelled SAM, and the methylated product peptide is captured on phosphocellulose filters according to the vendor supplied protocol for MSPH Multiscreen plates. Plates are read on a TopCount after adding 20?μL of Microscint-20 cocktail. Apparent Ki values are calculated using the Cheng–Prusoff relationship for a competitive inhibitor. IC50=Ki (1+[S]/Km)+[E]/2, where E is the enzyme and S is the substrate.
细胞实验 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 two fold dilution series of GSK126 or 0.15% DMSO. Plates are incubated for 6?days at 37°C in 5% CO2. Cells are then lysed with CellTiter-Glo (CTG) 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)
别名 GSK2816126A, EZH2 inhibitor
化合物与蛋白结合的复合物

T2079_2

Chaetomium thermophilum Polycomb Repressive Complex 2 bound to GSK126

分子量 526.67
分子式 C31H38N6O2
CAS No. 1346574-57-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 5.27 mg/mL (10 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8987 mL 9.4936 mL 18.9872 mL 47.4681 mL
5 mM 0.3797 mL 1.8987 mL 3.7974 mL 9.4936 mL
10 mM 0.1899 mL 0.9494 mL 1.8987 mL 4.7468 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. McCabe MT, et al. Nature. 2012, 492(7427), 108-112. 2. Ott HM, et al. Mol Cancer Ther. 2014, 13(12), 3062-3073. 3. Takeshima H, et al. Carcinogenesis. 2015, 36(2), 192-201. 4. Huang H, Wu D, Yan Y, et al. A targetable epigenetic vulnerability in PI3K/AKT inhibitor resistant cancers[J]. bioRxiv. 2020 5. Wu D, Yan Y, Wei T, et al. An acetyl-histone vulnerability in PI3K/AKT inhibition-resistant cancers is targetable by both BET and HDAC inhibitors[J]. Cell Reports . 2021, 34(7): 108744.

文献引用

1. Wu D, Yan Y, Wei T, et al. An acetyl-histone vulnerability in PI3K/AKT inhibition-resistant cancers is targetable by both BET and HDAC inhibitors. Cell Reports. 2021, 34(7): 108744. 2. Zhang Q, Chen X, Cao J, et al.Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer.Journal of Medicinal Chemistry.2023
CARM1-IN-3 PRMT4-IN-1 UNC0638 EPZ011989 A-196 CARM1 degrader-1 Chaetocin PRMT6-IN-3

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 已知活性化合物库 抗衰老化合物库 表观遗传库 抑制剂库 经典已知活性库 NO PAINS 化合物库 甲基化化合物库 组蛋白修饰化合物库 染色质修饰分子库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

GSK126 1346574-57-9 Chromatin/Epigenetic Histone Methyltransferase inhibit Inhibitor GSK2816126A GSK-126 GSK 126 EZH2 inhibitor inhibitor

 

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