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BRD4770

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产品编号 T1923Cas号 1374601-40-7

BRD4770 是组蛋白甲基转移酶G9a 抑制剂,可激活共济失调毛细血管扩张突变途径并诱导细胞衰老。它可抑制H3K9的二甲基和三甲基化,EC50为 5 µM。

BRD4770
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BRD4770

Rating icon 很棒
纯度: 99.82%
产品编号 T1923Cas号 1374601-40-7

BRD4770 是组蛋白甲基转移酶G9a 抑制剂,可激活共济失调毛细血管扩张突变途径并诱导细胞衰老。它可抑制H3K9的二甲基和三甲基化,EC50为 5 µM。

规格价格库存数量
1 mg¥ 247现货
5 mg¥ 538现货
10 mg¥ 868现货
25 mg¥ 1,680现货
50 mg¥ 2,860现货
100 mg¥ 4,270现货
1 mL x 10 mM (in DMSO)¥ 589现货
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产品介绍

生物活性
产品描述
BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.
靶点活性
G9a/EHMT2:5 μM
体内活性
BRD4770和棉酚联用可以增加LC3-II水平和自噬体数量,从而协同作用诱导PANC-1细胞死亡。BRD4770在胰腺癌细胞系PANC-1中,通过通过抑制G9a降低二 - 和三甲基化H3K9的细胞水平,诱导衰老,并抑制贴壁依赖性和非依赖性增殖。
激酶实验
Biochemical activity of G9a: Dissociation Enhanced Lanthanide Fluoro-ImmunoAssays (DELFIA) are performed in white, opaque 384-well plates coated with Neutravidin. Test compounds are diluted to 12 μg/mL in 50 mM Tris-HCl pH 8.5 containing 4% DMSO and 10 μL is dispensed into the wells. Blank and control wells received only compound buffer. GST-G9a at 10 μg/mL and SAM at 40 μM are diluted in 50 mM Tris HCl pH 8.5/10 mM DTT and added in a volume of 20 μL. Blank wells receives Tris/DTT buffer only. The reactions are initiated by the addition of 800 nM H3(1-20)-cysbiotin substrate in 50 mM Tris pH 8.5 in a volume of 10 μl, and incubated at room temperature for 60 minutes. The plates are washed 3 times with 100 μl of Wash Buffer (50 mM Tris pH 7.4, 150 mM NaCl, 0.05% Tween 20, 0.2% BSA). Next, 50 μl of Fluoroimmunoassay (FI) Buffer (50 mM Tris HCl pH 7.8, 150 mM NaCl, 0.05% Tween 40, 25 μM DTPA, 0.2% BSA, 0.05% BGG) containing 5ng α-2X-di-meth H3-K9 and 5ng goat anti-rabbit Eu chelate is added to all wells of the plate, and the plate is incubated for an additional hour at room temperature. The plates are washed 3 times with 100 μL of Wash Buffer, and 50 μL of Enhancement Solution is added to each well. Time resolved fluorescence is measured after 45 minutes on a Viewlux Microplate Imager imaging for 15 seconds with a 354 μs window, 400 μs delay, excitation at 360 nm, and emission at 618 nm.
细胞实验
PANC-1 cells are seeded and treated with BRD4770 in 6-well plates for 72 h. Cells are trypsinized and tested for soft agar colony formation using CytoSelect 96-Well Cell Transformation Assay, using the CyQuant GR dye to measure total cellular nucleic acid levels. Fluorescence is detected with an Analyst HT plate reader using a 485/520 nm filter set.(Only for Reference)
化学信息
分子量413.47
分子式C25H23N3O3
CAS No.1374601-40-7
SmilesCOC(=O)c1ccc2n(CCCc3ccccc3)c(NC(=O)c3ccccc3)nc2c1
密度1.21 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: 8.3 mg/mL (20 mM)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.4186 mL12.0928 mL24.1856 mL120.9278 mL
5 mM0.4837 mL2.4186 mL4.8371 mL24.1856 mL
10 mM0.2419 mL1.2093 mL2.4186 mL12.0928 mL
20 mM0.1209 mL0.6046 mL1.2093 mL6.0464 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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