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- 技术资料
- CAS号：
2089293-61-6
- 规格：
1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥273.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥247.0 |
| 规格： | 10mg | 产品价格： | ￥397.0 |
| 规格： | 25mg | 产品价格： | ￥780.0 |
| 规格： | 50mg | 产品价格： | ￥1464.0 |
| 规格： | 100mg | 产品价格： | ￥2312.0 |
| 规格： | 500mg | 产品价格： | ￥5272.0 |
Product Introduction
Bioactivity
| 名称 | NAcM-OPT |
| 描述 | NAcM-OPT is a specific, reversible inhibitor targeting N-Acetyl-UBE2M interaction with DCN1 （IC50: 79 nM). |
| 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]. |
| 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]. |
| 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]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (23.02 mM), Solution. DMSO : 270 mg/mL (621.55 mM), Sonication is recommended. H2O : Insoluble 10% DMSO+90% Saline : < 10 mg/mL (23.02 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. |
| 关键字 | Ubiquitin ligase | Ubiquitin conjugating enzyme | Ubiquitin activating enzyme | NEDD8-activating Enzyme | NEDD8 | NAE | NAcM-OPT | NAcMOPT | NAcM OPT | Inhibitor | inhibit | E3Enzyme | E3 ligating enzyme | E3 Enzyme | E2Enzyme | E2 Enzyme | E2 conjugating enzyme | E1Enzyme | E1/E2/E3 Enzyme | E1 Enzyme | E1 activating enzyme | DCN1-UBE2M |
| 相关产品 | Auxinole | Nutlin-3 | T521 | Yucasin | NSC697923 | Indole-3-carbinol | TRIM25 ligand-1 | BC-1293 | EN219 | Idasanutlin | PYZD-4409 | NSC232003 |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Metabolism Compound Library | NO PAINS Compound Library | Ubiquitination Compound Library | Multi-Target Compound Library | Orally Active Compound Library | PPI Inhibitor Library | Post-Translational Modification Compound Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 NAcM-OPT【2089293-61-6】
￥247 - 5272
