MLN4924
货号：
15217-10mg 基本售价：
6370.0 元 规格：
10 mg
产品信息
概述| 货号 | 15217-10mg |
| 描述 | NEDD8 is an ubiquitin-like protein whose activity is required to activate cullin-RING ubiquitin E3 ligases (CRLs) responsible for the ubiquitination and proteasome-dependent turnover of certain substrates with roles relevant to cellular processes important for cancer cell survival. Neddylation of CRLs is initiated by NEDD8-activating enzyme (NAE), which has become a novel target in cancer therapeutic research.1 MLN4924 is an analog of adenosine 5’-monophosphate that selectively inhibits NAE (IC50 = 4.7 nM).2 At much higher concentrations, MLN4924 inhibits the related enzymes ubiquitin-activating enzyme (UAE) and SUMO-activating enzyme (SAE) with IC50 values of 1.5 and 8.2 μM, respectively.2 At 0.3 μM, MLN4924 has been shown to disrupt CRL-mediated protein turnover leading to apoptosis in HCT116 cells by deregulating S-phase DNA synthesis.2In vivo, 30-60 mg/kg MLN4924 dose-dependently suppresses the growth of human tumor xenografts in mice.2 |
| 别名 | Pevonedistat; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Soucy, T.A.,Smith, P.G. and Rolfe, M. Targeting NEDD8-activated cullin-RING ligases for the treatment of cancer. Clinical Cancer Research 15(12), 3912-3916 (2009).
2.Soucy, T.A.,Smith, P.G.,Milhollen, M.A., et al. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature 458(7239), 732-736 (2009).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 443.5 |
| 分子式 | C21H25N5O4S |
| CAS号 | 905579-51-3 |
| 稳定性 | ≥ 2 years |
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