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NAcM-OPT

产品编号 T5374 CAS 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。

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NAcM-OPT, CAS 2089293-61-6

规格	价格/CNY	货期
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 * 10 mM (in DMSO)	￥ 322	现货

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其他形式的 NAcM-OPT:

NAcM-OPT HCl(2089293-61-6 free base)
现货

选择批次

纯度: 99.68%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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].

分子量	434.4
分子式	C23H29Cl2N3O
CAS No.	2089293-61-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (230.20 mM)

H2O: Insoluble

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.302 mL	11.5101 mL	23.0203 mL	57.5506 mL
	5 mM	0.4604 mL	2.302 mL	4.6041 mL	11.5101 mL
	10 mM	0.2302 mL	1.151 mL	2.302 mL	5.7551 mL
	20 mM	0.1151 mL	0.5755 mL	1.151 mL	2.8775 mL
	50 mM	0.046 mL	0.2302 mL	0.4604 mL	1.151 mL
	100 mM	0.023 mL	0.1151 mL	0.2302 mL	0.5755 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Scott DC, et al. Blocking an N-terminal acetylation-dependent protein interaction inhibits an E3 ligase. Nat Chem Biol. 2017 Aug;13(8):850-857. 2. Hammill JT, et al. Discovery of an Orally Bioavailable Inhibitor of Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation. J Med Chem. 2018 Apr 12;61(7):2694-2706.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

NAcM-OPT 2089293-61-6 Metabolism Ubiquitination E1/E2/E3 Enzyme NEDD8 E3 ligating enzyme Ubiquitin activating enzyme inhibit NAE Ubiquitin conjugating enzyme NAcMOPT Ubiquitin ligase NEDD8-activating Enzyme E1 activating enzyme E2 conjugating enzyme Inhibitor NAcM OPT inhibitor

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NAcM-OPT

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords