Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EPZ005687 是一种选择性EZH2抑制剂,Ki 值为 24 nM,对其选择性是对 EZH1 的 50 倍,对其他 15 种甲基转移酶的 500 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 191 | 现货 | ||
5 mg | ¥ 493 | 现货 | ||
10 mg | ¥ 756 | 现货 | ||
25 mg | ¥ 1,250 | 现货 | ||
50 mg | ¥ 1,950 | 现货 | ||
100 mg | ¥ 3,798 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 595 | 现货 |
产品描述 | EPZ005687 is a potent and selective inhibitor of EZH2. |
靶点活性 | EZH2:24 nM(Ki) |
体外活性 | 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。 |
激酶实验 | 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. |
细胞实验 | 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) |
分子量 | 539.67 |
分子式 | C32H37N5O3 |
CAS No. | 1396772-26-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.4 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.853 mL | 9.2649 mL | 18.5298 mL | 46.3246 mL |
5 mM | 0.3706 mL | 1.853 mL | 3.706 mL | 9.2649 mL | |
10 mM | 0.1853 mL | 0.9265 mL | 1.853 mL | 4.6325 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
EPZ005687 1396772-26-1 Chromatin/Epigenetic Histone Methyltransferase Inhibitor EPZ-005687 EPZ 005687 inhibit inhibitor