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UNC 0631

产品编号 T2354Cas号 1320288-19-4
别名 UNC0631

UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂,IC50值为 4 nM。它有效降低 MDA-MB-231 细胞中 H3K9me2的水平,IC50为 25 nM。

UNC 0631
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UNC 0631

纯度: 98.76%
产品编号 T2354 别名 UNC0631Cas号 1320288-19-4

UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂,IC50值为 4 nM。它有效降低 MDA-MB-231 细胞中 H3K9me2的水平,IC50为 25 nM。

规格价格库存数量
1 mg¥ 247现货
5 mg¥ 619现货
10 mg¥ 1,160现货
25 mg¥ 2,320现货
50 mg¥ 3,730现货
100 mg¥ 5,320现货
1 mL x 10 mM (in DMSO)¥ 869现货
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产品介绍

生物活性
产品描述
UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
靶点活性
G9a:4 nM
体内活性
在MCF7,22RV1和IMR90细胞中,UNC0631显著降低H3K9me2水平。
激酶实验
SAHH-coupled assays: This assay utilizes SAHH to hydrolyze the methyltransfer product SAH to homocysteine and adenosine in the presence of adenosine deaminase which converts adenosine to inosine. The homocysteine concentration is then determined through conjugation of its free sulfhydryl moiety to a thiol-sensitive fluorophore, ThioGlo. For IC50 determinations, assay mixtures are prepared in 25 mM potassium phosphate buffer pH 7.5, 1 mM EDTA, 2 mM MgCl2, 0.01% Triton X-100 with 5 μM SAHH, 0.3 U/mL of adenosine deaminase, 25 μM SAM, and 15 μM ThioGlo. G9a, GLP, SETD7, SETD8, PRMT3 and SUV39H2 are assayed at 25 nM, 100 nM, 200 nM, 250 nM, 500 nM and 100 nM, respectively. Inhibitors are added at concentrations ranging from 4 nM to 16 μM. After 2 min incubation, reactions are initiated by addition of the histone peptides: 10 μM H3(1–25) for G9a, 20 μM H3(1–25) for GLP, 100 μM H3(1–25) for SETD7, 500 μM H4(1–24) for SETD8, 10 μM H4(1–24) for PRMT3 and 200 μM H3K9Me1 (1–15) for SUV39H2. The methylation reaction is followed by monitoring the increase in fluorescence using Biotek Synergy2 plate reader with 360/40 nm excitation filter and 528/20 nm emission filter for 20 min in 384 well-plate format. Activity values are corrected by subtracting background caused by the peptide or the protein. IC50 values are calculated using Sigmaplot. Standard deviations are calculated from two independent experiments.
细胞实验
MDA-MB-231, PC3, HCT116 cells are cultured in RPMI with 10% FBS, 22RV1 cells in alphaMEM and 10% FBS, MCF7 and IMR90 cells in DMEM with 10% FBS. Cells are treated with inhibitors for 48 h. The media is removed and replaced with DMEM 10% FBS without phenol red supplemented with 1 mg/mL of MTT and incubated for 1–2 h. Live cells reduce yellow MTT to purple formazan. The resulting formazanis solubilized in acidified isopropanol and 1% Triton. Formazan signal absorbance is measured at 570 nm and corrected for the 650 nm background. IC50s are calculated using GraphPad Prizm statistical package with sigmoidal variable slope dose response curve fit.(Only for Reference)
别名UNC0631
化学信息
分子量635.93
分子式C37H61N7O2
CAS No.1320288-19-4
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
Ethanol: 5 mg/mL (7.86 mM), Heating is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 100 mg/mL (157.25 mM), Heating is recommended.
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.5725 mL7.8625 mL15.7250 mL78.6250 mL
5 mM0.3145 mL1.5725 mL3.1450 mL15.7250 mL
DMSO
1mg5mg10mg50mg
10 mM0.1573 mL0.7863 mL1.5725 mL7.8625 mL
20 mM0.0786 mL0.3931 mL0.7863 mL3.9313 mL
50 mM0.0315 mL0.1573 mL0.3145 mL1.5725 mL
100 mM0.0157 mL0.0786 mL0.1573 mL0.7863 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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