Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pevonedistat (MLN4924) 是有效的,选择性的NEDD8 活化酶(NAE) 抑制剂,其IC50=4.7 nM。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (281.83 mM), Sonification is recommended
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Pevonedistat 905579-51-3 Metabolism Ubiquitination E1/E2/E3 Enzyme NEDD8 NEDD8-activating Enzyme MLN-4924 MLN4924 Inhibitor MLN 4924 inhibit NAE inhibitor