HDM201
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ¥1931.00 | 现货 | |
| 1mg | ¥404.00 | 现货 | |
| 5mg | ¥1560.00 | 现货 | |
| 10mg | ¥2330.00 | 现货 | |
| 50mg | ¥8388.00 | 现货 | |
| 100mg | ¥13420.00 | 现货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
HDM201, also known as Siremadlin or NVP-HDM201, inhibits the Mdm2-p53 protein-protein interaction, with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs. Mdm4. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction of the Mdm2 and p53 proteins as well as leading to the activation of the p53 pathway. Currently, interfering the interaction between the tumor suppressor p53 and its main negative regulator MDM2 has become a therapeutic concept explored to treat cancers.
References:
1. Stachyra-Valat T, Baysang F, D’Alessandro AC, et al. Abstract 1239: NVP-HDM201: Biochemical and biophysical profile of a novel highly potent and selective PPI inhibitor of p53-Mdm2. Cancer Research, 2016, 76(14 Suppl): Abstract nr 1239.
2. Jeay S, Ferretti S, Holzer P, et al. Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201. Cancer Research, 2018, 78(21): 6257-6267.
产品性质
| 物理外观 | Solid |
| CAS号 | 1448867-41-1 |
| 分子式 | C26H24Cl2N6O4 |
| 分子量 | 555.41 |
| 小分子别名 | Siremadlin |
| 化学名称 | (S)-5-(5-chloro-1-methyl-2-oxo-1,2-dihydropyridin-3-yl)-6-(4-chlorophenyl)-2-(2,4-dimethoxypyrimidin-5-yl)-1-isopropyl-5,6-dihydropyrrolo[3,4-d]imidazol-4(1H)-one |
| 溶解度 | insoluble in H2O; ≥49.1 mg/mL in DMSO; ≥51.8 mg/mL in EtOH |
| SMILES | ClC1=CC=C([C@@H]2N(C3=CC(Cl)=CN(C)C3=O)C(C4=C2N(C(C)C)C(C5=C(OC)N=C(OC)N=C5)=N4)=O)C=C1 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | Siremadlin(NVP-HDM201)是一种强效、口服生物利用度高且高度特异的 p53-MDM2 相互作用抑制剂。 |



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