生物活性 | |||
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描述 | The MYC family of oncogenes, which encodes basic helix-loop-helix leucine zipper (bHLHZip) transcription factors, is considered as one of the most important drivers of tumor development and has been highlighted as a key therapeutic target for cancer therapy for a number of tumor types. MYCMI-6 is a potent and selective inhibitor of MYC:MAX interaction with an IC50 less than 1.5 μM and binds to the MYC bHLHZip domain with a KD of 1.6 ± 0.5 μM. MYCMI-6 significantly reduced growth of the MYCN-amplified cell lines and the MYCN-non-amplified cell lines with average growth inhibition of 50% (GI50) values of 2.5-6 μM and 20 μM, respectively. Further, MYCMI-6 efficiently inhibited anchorage-independent growth of MYCN-amplified neuroblastoma cells with a GI50 value less than 0.4 μM. In vivo, MYCMI-6 (20 mg/kg; i.p.; daily for 1-2 weeks) induced massive apoptosis and reduces tumor cell proliferation, tumor microvasculature density and MYC:MAX interaction in a MYC-dependent xenograft tumor model[2]. | ||
作用机制 | MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.68mL 0.54mL 0.27mL |
13.39mL 2.68mL 1.34mL |
26.78mL 5.36mL 2.68mL |
参考文献 |
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