MYCMI-6

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 K_D 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 model².

溶解方案(细胞实验)

DMSO 中的溶解度 : 2.4 mg/mL (6.43 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：0.5% CMC-Na/saline waterSolubility: 5.56 mg/mL (14.89 mM); 悬浊液; 超声助溶"