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Pevonedistat

Pevonedistat

产品编号 T6332   CAS 905579-51-3
别名: MLN4924

Pevonedistat (MLN4924) 是有效的,选择性的NEDD8 活化酶(NAE) 抑制剂,其IC50=4.7 nM。

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Pevonedistat Chemical Structure
Pevonedistat, CAS 905579-51-3
规格 价格/CNY 货期 数量
2 mg ¥ 651 现货
5 mg ¥ 995 现货
10 mg ¥ 1,718 现货
25 mg ¥ 2,996 现货
50 mg ¥ 4,110 现货
100 mg ¥ 5,850 现货
200 mg ¥ 10,600 现货
1 mL * 10 mM (in DMSO) ¥ 997 现货
其他形式的 Pevonedistat:
产品目录号及名称: Pevonedistat (T6332)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Pevonedistat (MLN4924) is an effective and specific small molecule NEDD8-activating enzyme (NAE) inhibitor (IC50: 4.7 nM).
靶点活性 NAE:4.7 nM
体外活性 MLN4924 is a potent inhibitor of NAE, and is selective relative to the closely related enzymes UAE, SAE, UBA6 and ATG7 (IC50=1.5, 8.2, 1.8 and >10 μM, respectively) when evaluated in purified enzyme assays that monitor the formation of E2-UBL thioester reaction products. MLN4924 selectively inhibits NAE activity compared to the closely related ubiquitin-activating enzyme (UAE, also known as UBA1) and SUMO-activating enzyme (SAE; a heterodimer of SAE1 and UBA2 subunits), in purified enzyme and cellular assays. MLN4924 exhibits potent cytotoxic activity against a variety of human tumour-derived cell lines[1].
体内活性 MLN4924 (sc, 10 mg/kg, 30 mg/kg, or 60 mg/kg) inhibits the NEDD8 pathway resulting in DNA damage in Mice bearing HCT-116 xenografts[1].Pevonedistat (sc, 120 mg/kg) and TNF-α (10 μg/kg) synergistically cause liver damage in SD rats[2].
激酶实验 Bcl-2 Binding affinity calculation: A predicted binding affinity for Obatoclax binding to BCL-2 is calculated using the SIE scoring function. [4] As a control in determining the reliability of the calculation, predicted binding affinities Ki) are calculated for a set of 12 small molecules with experimentally measured binding affinities to BCL-2.
细胞实验 MLN4924 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. HCT-116 cells grown in 6-well cell-culture dishes are treated with 0.1% DMSO (control) or 0.3 μM MLN4924 for 24 h. Whole cell extracts are prepared and analysed by immunoblotting. For analysis of the E2-UBL thioester levels, lysates are fractionated by non-reducing SDS-PAGE and immunoblotted with polyclonal antibodies to Ubc12, Ubc9 and Ubc10. For analysis of other proteins, lysates are fractionated by reducing SDS-PAGE and probed with primary antibodies as follows: mouse monoclonal antibodies to CDT1, p27, geminin, ubiquitin, securin/PTTG and p53 or rabbit polyclonal antibodies to NRF2, Cyclin B1 and GADD34[1].
别名 MLN4924
分子量 443.52
分子式 C21H25N5O4S
CAS No. 905579-51-3

存储

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

溶解度

DMSO: 125 mg/mL (281.83 mM), Sonification is recommended

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 2.2547 mL 11.2734 mL 22.5469 mL 56.3672 mL
5 mM 0.4509 mL 2.2547 mL 4.5094 mL 11.2734 mL
10 mM 0.2255 mL 1.1273 mL 2.2547 mL 5.6367 mL
20 mM 0.1127 mL 0.5637 mL 1.1273 mL 2.8184 mL
50 mM 0.0451 mL 0.2255 mL 0.4509 mL 1.1273 mL
100 mM 0.0225 mL 0.1127 mL 0.2255 mL 0.5637 mL

计算器

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稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Soucy TA, et al. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature. 2009 Apr 9;458(7239):732-6. 2. Wolenski, F., Fisher, C., Sano, T., Wyllie, S., Cicia, L., & Gallacher, M. et al. (2015). The NAE inhibitor pevonedistat (MLN4924) synergizes with TNF-α to activate apoptosis. Cell Death Discovery, 1(1). doi: 10.1038/cddiscovery.2015.34 3. Fu Z, Liao W, Ma H, et al. Inhibition of neddylation plays protective role in lipopolysaccharide-induced kidney damage through CRL-mediated NF-κB pathways[J]. Am J Transl Res. 2019, 11(5): 2830-2842. 4. Chen S M, Lin T K, Tseng Y Y, et al. Targeting inhibitors of apoptosis proteins suppresses medulloblastoma cell proliferation via G2/M phase arrest and attenuated neddylation of p21[J]. Cancer medicine. 2018 Aug;7(8):3988-4003. 5. Qin Z, Hu H, Sun W, et al. miR-224-5p Contained in Urinary Extracellular Vesicles Regulates PD-L1 Expression by Inhibiting Cyclin D1 in Renal Cell Carcinoma Cells. Cancers . 2021, 13, 618[J]. 2021.

文献引用

1. Qin Z, Hu H, Sun W, et al. miR-224-5p Contained in Urinary Extracellular Vesicles Regulates PD-L1 Expression by Inhibiting Cyclin D1 in Renal Cell Carcinoma Cells. Cancers. 2021 Feb 4;13(4):618. doi: 10.3390/cancers13040618. 2. Hussain M, Lu Y, Tariq M, et al. A small-molecule Skp1 inhibitor elicits cell death by p53-dependent mechanism. Iscience. 2022, 25(7): 104591. 3. Chen S M, Lin T K, Tseng Y Y, et al. Targeting inhibitors of apoptosis proteins suppresses medulloblastoma cell proliferation via G2/M phase arrest and attenuated neddylation of p21. Cancer Medicine. 2018 Aug;7(8):3988-4003 4. Fu Z, Liao W, Ma H, et al. Inhibition of neddylation plays protective role in lipopolysaccharide-induced kidney damage through CRL-mediated NF-κB pathways. Am J Transl Res. 2019, 11(5): 2830-2842 5. Sun Y, Baechler S A, Zhang X, et al.Targeting neddylation sensitizes colorectal cancer to topoisomerase I inhibitors by inactivating the DCAF13-CRL4 ubiquitin ligase complex.Nature Communications.2023, 14(1): 3762. 6. Zhong C, Zhu R, Jiang T, et al.Design and Characterization of a Novel eEF2K Degrader with Potent Therapeutic Efficacy Against Triple‐Negative Breast Cancer.Advanced Science.2023: 2305035.
SZL P1-41 TAS4464 Serdemetan Siremadlin Skp2 Inhibitor C1 BC-1382 RO8994 Subasumstat

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 抗癌药物库 血液病分子库 泛素化化合物库 抗肺癌化合物库 临床前化合物库 已知活性化合物库 NO PAINS 化合物库 人代谢物化合物库

剂量换算

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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
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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。
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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

Pevonedistat 905579-51-3 Metabolism Ubiquitination E1/E2/E3 Enzyme NEDD8 NEDD8-activating Enzyme MLN-4924 MLN4924 Inhibitor MLN 4924 inhibit NAE inhibitor

 

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