| 货号 | 16259-1mg |
| 描述 | The E3 ubiquitin ligase known as murine double minute 2 (MDM2; HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53.1,2 JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM).3 It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells.3 JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models.2 As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.2,4,5 |
| 别名 | Serdemetan; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Fulda, S.,Rajalingam, K. and Dikic, I. Ubiquitylation in immune disorders and cancer: From molecular mechanisms to therapeutic implications. EMBO Mol.Med. 4(7), 545-556 (2012). 2.Yuan, Y.,Liao, Y.M.,Hsueh, C.T., et al. Novel targeted therapeutics: Inhibitors of MDM2, ALK and PARP. J. Hematol. Oncol. 4(16), 1-14 (2011). 3.Kojima, K.,Burks, J.K.,Arts, J., et al. The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias. Molecular Cancer Therapeutics 9(9), 2545-2557 (2010). 4.Lehman, J.A.,Hauck, P.M.,Gendron, J.M., et al. Serdemetan antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes. PLoS One 8(9), 1-5 (2013). 5.Jones, R.J.,Gu, D.,Bjorklund, C.C., et al. The novel anticancer agent JNJ-26854165 induces cell death through inhibition of cholesterol transport and degradation of ABCA1. Journal of Pharmacology and Experimental Therapeutics 346(3), 381-392 (2013). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 328.4 |
| 分子式 | C21H20N4 |
| CAS号 | 881202-45-5 |
| 稳定性 | ≥ 2 years |
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