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EI1

产品编号 T6484Cas号 1418308-27-6
别名 KB-145943, Ezh2 inhibitor

EI1 (Ezh2 inhibitor) 是一种EZH2抑制剂,能够作用于 EZH2 (WT) 和 EZH2 (Y641F),IC50值分别为 15 nM 和 13 nM。

EI1

EI1

纯度: 99.98%
产品编号 T6484 别名 KB-145943, Ezh2 inhibitorCas号 1418308-27-6

EI1 (Ezh2 inhibitor) 是一种EZH2抑制剂,能够作用于 EZH2 (WT) 和 EZH2 (Y641F),IC50值分别为 15 nM 和 13 nM。

规格价格库存数量
1 mg¥ 296现货
5 mg¥ 662现货
10 mg¥ 1,060现货
25 mg¥ 1,980现货
50 mg¥ 3,390现货
100 mg¥ 4,830现货
200 mg¥ 6,720现货
1 mL x 10 mM (in DMSO)¥ 678现货
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纯度:99.98%
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产品介绍

生物活性
产品描述
EI1 (Ezh2 inhibitor) is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
靶点活性
EZH2 (Y641F):13 nM, EZH2 (WT):15 nM
体外活性
在DLBCL细胞中,EI1通过抑制细胞H3K27的甲基化作用,并激活Ezh2靶基因p16的表达。在小鼠胚胎成纤维细胞中,EI1同样抑制H3K27me3和细胞增殖。此外,EI1选择性地抑制带有Ezh2突变的DLBCL细胞的生长,并导致细胞周期停滞及凋亡。[1]
激酶实验
Biochemical Assay: For IC50 determination, EI1 is serial diluted threefold in DMSO for a total of 12 concentrations, with the starting concentration at 1 μM. The reaction is incubated at room temperature for 120 min, and stopped by adding quench solution (2.5% TFA with 320 nM d4-SAH). SAH production is quantitated using an API 4000 triple quadrupole mass spectrometry with Turbulon Spray coupled with Prominence UFLC. The percentage of inhibition is normalized using positive (no inhibitor) and negative (no enzyme) controls, and IC50 calculated using PRISM. Enzymology studies of S-Adenosyl methionine (SAM) competition are performed with slight modification of reaction condition: 10 μM EI1 is used as the starting dose for serial dilution. SAM is titrated over a range between 1 μM and 50 μM (corresponding to 1 × Km and 50 × Km), and substrate peptide is present in the final reaction mixture at its saturated condition (10 μM). For histone methyltransferase (HMT) profiling in Table 1, all HMTs are purified recombinant proteins from either Escherichia coli or Baculovirus system. The catalytic domain of G9a, SuV39H2, Set7/9, CARM1, SETD8, NSD3, SETD2, and Dot1L, and the full-length SmyD2 protein were used in the biochemical assays. HMT biochemical reactions are carefully characterized with enzymology studies and the SAM and substrate Km determined. The SAM and substrate concentrations are kept at their respective Km for most of the HMTs, except the ones (SmyD2 and Set7/9) with low SAM-Km value, for which 0.5 μM SAM is used. All HMT reactions are performed using the same assay format where the production of SAH from the biochemical reaction is quantitated by LC-MS.
细胞实验
Exponentially growing diffused large B-cell lymphoma (DLBCL) cells are seeded in 12-well plates at a density of 1 × 105 cells/mL with the indicated concentration of EI1. Viable cell number is determined every 3–4 d for up to 14 or 15 d by Vi-CELL. Mouse embryonic fibroblasts (MEFs) are seeded in a six-well plate at 2.5 × 104 cell/mL and treated with EI1 (3.3 μM) or 4-OH-tamoxifen (100 nM). Viable cell number is determined at days 3, 6 and 11. On days of cell counts, fresh growth medium and compound are replenished and cells split back to a density of 1 × 105 cells/mL. Total cell number is expressed as split-adjusted viable cells per milliliter. IC50 is calculated by PRISM and all proliferation experiments are repeated more than two times and representative data are presented.(Only for Reference)
别名KB-145943, Ezh2 inhibitor
化学信息
分子量390.48
分子式C23H26N4O2
CAS No.1418308-27-6
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: Insoluble
DMSO: 12.5 mg/mL (32.01 mM)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.5610 mL12.8048 mL25.6095 mL128.0475 mL
5 mM0.5122 mL2.5610 mL5.1219 mL25.6095 mL
10 mM0.2561 mL1.2805 mL2.5610 mL12.8048 mL
20 mM0.1280 mL0.6402 mL1.2805 mL6.4024 mL

计算器

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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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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μL
2 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

剂量转换

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