| 货号 | 9000487-1mg |
| 描述 | Mutations in the p53 tumor suppressor are found in many different neoplastic cells. PRIMA-1 (Item No. 63520) is a unique anti-oncogenic substance that re-activates the apoptotic function of mutant p53 via conformational modulation of function-specific epitopes.1,2PRIMA-1MET is a methylated derivative of PRIMA-1 that restores tumor-suppressor function to mutant p53 and induces cell death in various cancer cell lines.3PRIMA-1MET can synergize with chemotherapeutic drugs to induce tumor cell apoptosis.4 At 25-50 µM, it can also dose-dependently inhibit thioredoxin reductase, a key regulator of cellular redox balance.5 |
| 别名 | APR 246; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Bykov, V.J.N.,Issaeva, N.,Shilov, A., et al. Restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound. Nature Medicine 8(3), 282-288 (2002). 2.Lane, D.P., and Hupp, T.R. Drug discovery and p53. Drug Discovery Today 8(8), 347-355 (2003). 3.Aryee, D.N.,Niedan, S.,Ban, J., et al. Variability in functional p53 reactivation by PRIMA-1Met/APR-246 in Ewing sarcoma. British Journal of Cancer 109(10), 2696-2704 (2013). 4.Bykov, V.J.,Zache, N.,Stridh, H., et al. PRIMA-1MET synergizes with cisplatin to induce tumor cell apoptosis. Oncogene 24(21), 3484-3491 (2005). 5.Peng, X.,Zhang, M.Q.,Conserva, F., et al. APR-246/PRIMA-1MET inhibits thioredoxin reductase 1 and converts the enzyme to a dedicated NADPH oxidase. Cell Death Dis. 4, e881 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 199.3 |
| 分子式 | C10H17NO3 |
| CAS号 | 5291-32-7 |
| 稳定性 | ≥ 2 years |
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