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NAcM-OPT

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产品编号 T5374Cas号 2089293-61-6

NAcM-OPT 是口服活性、有效的 cullin neddylation 1 抑制剂,可以抑制 DCN1-UBE2M 相互作用。

NAcM-OPT

NAcM-OPT

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纯度: 99.68%
产品编号 T5374Cas号 2089293-61-6

NAcM-OPT 是口服活性、有效的 cullin neddylation 1 抑制剂,可以抑制 DCN1-UBE2M 相互作用。

规格价格库存数量
5 mg¥ 289现货
10 mg¥ 497现货
25 mg¥ 976现货
50 mg¥ 1,830现货
100 mg¥ 2,890现货
500 mg¥ 6,590现货
1 mL x 10 mM (in DMSO)¥ 322现货
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产品介绍

生物活性
产品描述
NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 (IC50: 79 nM).
靶点活性
DCN1-UBE2M:79 nM (cell free)
体外活性
NAcM-OPT inhibits neddylation in and prevents anchorage-independent growth of a DCN1 amplified cell line without causing changes in protein homeostasis [1].
体内活性
NAcM-OPT has an oral bioavailability of 88% (calculated using IV dose at 1.5 mg/kg and PO dose at 50 mg/kg) [2].
激酶实验
TR-FRET assays were carried out in black 384-well microtiter plates at a final volume of 20 μL per well. To screen library compounds, the assay cocktail was prepared as a mixture of 50 nM Biotin-DCN1, 20 nM Ac-UBE2M12-AlexaFluor488, 2.5 nM Tb-Streptavidin in assay buffer (25 mM HEPES, 100 mM NaCl, 0.1% Triton X-100, 0.5 mM DTT, pH 7.5). The assay cocktail was incubated for 1 hour at room temperature and distributed using a WellMate instrument. Compounds to be screened were added to assay plates from DMSO stock solutions by pin transfer using 50SS pins. The assay mixture was incubated for 1 hour at room temperature prior to measuring the TR-FRET signal with a PHERAstar FS plate reader equipped with modules for excitation at 337 nm and emissions at 490 and 520 nm. The integration start was set to 100 μs and the integration time to 200 μs. The number of flashes was fixed at 100. The ratio of 520/490 was used as TR-FRET signal in calculations. Assay endpoints were normalized from 0% (DMSO only) to 100% inhibition (unlabeled competitor peptide) for hit selection and for curve fitting [1].
细胞实验
Exponentially growing cells were plated in 6-well plates at 0.4 × 10^6 cells/well in 2 ml of media and incubated overnight at 37 °C in a humidified 5% CO2 incubator. 24 and 48 hrs after plating, the media was aspirated and replenished with 2 ml fresh media containing either 4 μL of DMSO or a 500× compound DMSO stock solution. The cells were harvested after 72 hrs via trypsinization, thoroughly washed with PBS, pelleted, flash frozen in liquid N2, and stored at ?80 °C. Cell pellets were thawed on ice and lysed by harvested resuspension in 30–40 μL of lysis buffer [50 mM Tris, 150 mM NaCl, 0.5% NP-40, 0.1% SDS, 6.5 M Urea, 2 mM 1,10-orthophenanthroline, 1× Halt Protease and Phosphatase inhibitor cocktail, 0.25 kU Universal Nuclease, pH 7.5]. Cell suspensions were incubated on ice for 25 minutes with occasional mixing by pipetting up and down. Lysates were cleared by centrifugation at 13,000 rpm for 20 minutes and the supernatant collected. The protein concentration of total cell lysate was determined by BCA assay using BSA as a control. Cell lysates were diluted into 2× SDS-PAGE sample buffer such that 25 μg of total protein was loaded per well. Samples were heated at 95 °C for 2 minutes, briefly cleared by pulse centrifugation, separated on 4–12% NuPAGE gels, and transferred to PVDF membranes at 100 V for 90 minutes at 4 °C. Membranes were blocked for 1 hour in blocking buffer consisting of 1× TBS, 0.1% Tween-20, and 5% Blotting grade non-fat dry milk. Primary antibodies were prepared in blocking buffer and incubated with membranes overnight at 4 °C with rocking, followed by extensive washing in 1× TBS, 0.1% Tween-20. Secondary antibodies were prepared in blocking buffer according to the manufactures recommendations and incubated with membranes for 1 hour at room temperature. After extensive washing, membranes were developed with SuperSignal West Pico Chemiluminescent substrate and developed by film exposure [1].
化学信息
分子量434.4
分子式C23H29Cl2N3O
CAS No.2089293-61-6
SmilesCCCCN1CCC(CC1)N(Cc1ccccc1)C(=O)Nc1ccc(Cl)c(Cl)c1
密度1.23 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: 45 mg/mL (103.59 mM)
H2O: Insoluble
溶液配制表
1mg5mg10mg50mg
1 mM2.3020 mL11.5101 mL23.0203 mL115.1013 mL
5 mM0.4604 mL2.3020 mL4.6041 mL23.0203 mL
10 mM0.2302 mL1.1510 mL2.3020 mL11.5101 mL
20 mM0.1151 mL0.5755 mL1.1510 mL5.7551 mL
50 mM0.0460 mL0.2302 mL0.4604 mL2.3020 mL
100 mM0.0230 mL0.1151 mL0.2302 mL1.1510 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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