| 货号 | 17408-1mg |
| 描述 | The c-Myc oncoprotein is overexpressed in many tumors and is essential for maintaining the proliferation of transformed cells. To function as a transcription factor, c-Myc must dimerize with Max via the basic helix-loop-helix leucine zipper protein (bHLH-ZIP) domains in each protein. 10074-G5 is a c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM).1,2,3 10074-G5 is cytotoxic to c-Myc-overexpressing cells lines with IC50 values of 15.6 and 13.5 µM for Daudi Burkitt lymphoma cells and HL60 promyelocytic leukemia cells, respectively.4 10074-G5 can also interfere with N-Myc/Max interactions (Kd = 19.2 µM for binding the bHLH-Zip of N-Myc), inducing apoptosis in N-Myc amplified neuroblastoma Kelly cells (IC50 = 22.5 µM).5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Follis, A.V.,Hammoudeh, D.I.,Wang, J., et al. Structural rationale for the coupled binding and unfolding of the c-Myc oncoprotein by small molecules. Chemistry & Biology 15(11), 1149-1155 (2008). 2.Hammoudeh, D.I.,Follis, A.V.,Prochownik, E.V., et al. Multiple independent binding sites for small-molecule inhibitors on the oncoprotein c-Myc. Journal of the American Chemical Society 131(21), 7391-7401 (2009). 3.Yap, J.L.,Wang, H.,Hu, A., et al. Pharmacophore identification of c-Myc inhibitor 10074-G5. Bioorganic & Medicinal Chemistry Letters 23(1), 370-374 (2013). 4.Clausen, D.M.,Guo, J.,Parise, R.A., et al. In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization. Journal of Pharmacology and Experimental Therapeutics 335(3), 715-727 (2010). 5.Müller, I.,Larsson, K.,Frenzel, A., et al. Targeting of the MYCN protein with small molecule c-MYC inhibitors. PLoS One 9(5), (2014). | |
| 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 | 332.3 |
| 分子式 | C18H12N4O3 |
| CAS号 | 413611-93-5 |
| 稳定性 | ≥ 2 years |
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