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MS436

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产品编号 T1854Cas号 1395084-25-9

MS436 是溴结构域抑制剂,作用于 BRD4 BrD1的Ki 为 30 到 50 nM 之间,比作用于 BrD2 选择性高 10 倍。

MS436
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MS436

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纯度: 98.92%
产品编号 T1854Cas号 1395084-25-9

MS436 是溴结构域抑制剂,作用于 BRD4 BrD1的Ki 为 30 到 50 nM 之间,比作用于 BrD2 选择性高 10 倍。

规格价格库存数量
1 mg¥ 266现货
2 mg¥ 378现货
5 mg¥ 622现货
10 mg¥ 1,080现货
25 mg¥ 2,320现货
50 mg¥ 3,660现货
100 mg¥ 5,330现货
500 mg¥ 10,900现货
1 mL x 10 mM (in DMSO)¥ 683现货
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产品介绍

生物活性
产品描述
MS436 is a selective, small-molecule inhibitor for the BRD4 bromodomains.
靶点活性
BRD4(1):<0.085 μM(Ki), BRD4(2):0.34 μM(Ki)
体内活性
对于第一溴结构域蛋白,MS436表现出低纳摩尔亲和力(Ki=30-50 nM)。在NF-κB定向产生的小鼠巨噬细胞中,MS436能够抑制NO和IL-6的BRD4活性。
激酶实验
Fluorescence Anisotropy Binding Assay: Binding affinity of the newly synthesized diazobenzene compounds for various bromodoamins is assessed in a fluorescence anisotropy competition assay using a fluorescein isothiocyanate (FITC)-labeled MS417 as an assay probe. Competition experiments are performed with a BrD protein (0.25–1 μM) and the fluorescent probe (80 nM), and increasing concentration of unlabeled competing ligand in a PBS buffer (pH 7.4) in total volume of 80 μL Measurements are obtained after a 1 hour incubation of the fluorescent ligand and the protein at 25°C with Safire 2 microplate reader. In a competition-binding assay, fluorescent ligand concentration is ≤ 2Kd, and protein concentration was set at which 50-80% of fluorescent ligand is bound. Dissociation constant of a competing ligand is calculated with the correction to Cheng-Prussoff equation introduced by Nicolovska-Coleska and colleagues. Assuming one-site competitive binding model, the equation used to calculate Ki's from IC50 values recovered from fitting data using Prism.
细胞实验
Murine macrophage RAW264.7 cells are plated at a density of 10000 cells per well in a 96-well plate and incubated at 37 °C for 18 h. The cells are then treated with the diazobenzene bromodomain inhibitors up to 100 μL for 24 hours. At the end of the 24 hr incubation, 10 μL of the MTT solution (4 mg/ml) is added to each well and incubated at 37°C for 4 h. The supernatants are then removed and the cells were solubilized in 100 μL of 100% DMSO. The diazobenzene compounds are first dissolved in DMSO then diluted with culture medium to concentrations that ranged from 0.28 to 50000 nM. The final concentration of DMSO is adjusted to 0.05% (v/v). The extent of the reduction is measured by the absorbance at 570/630 nm using EnVison 2104 Multilabel Reader.(Only for Reference)
化学信息
分子量383.42
分子式C18H17N5O3S
CAS No.1395084-25-9
SmilesCc1cc(\N=N\c2ccc(cc2)S(=O)(=O)Nc2ccccn2)c(N)cc1O
密度1.42 g/cm3 (Predicted)
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
DMSO: 40 mg/mL (104.32 mM)
溶液配制表
1mg5mg10mg50mg
1 mM2.6081 mL13.0405 mL26.0811 mL130.4053 mL
5 mM0.5216 mL2.6081 mL5.2162 mL26.0811 mL
10 mM0.2608 mL1.3041 mL2.6081 mL13.0405 mL
20 mM0.1304 mL0.6520 mL1.3041 mL6.5203 mL
50 mM0.0522 mL0.2608 mL0.5216 mL2.6081 mL
100 mM0.0261 mL0.1304 mL0.2608 mL1.3041 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

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
mg/kg
g
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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