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].
MYCMI-6 细胞实验
Cell Line
Concentration
Treated Time
Description
References
SK-N-BE(2) cells
2.5 μM
16 hours
To validate the inhibitory effects of MYCMI-6 on endogenous MYCN:MAX interaction
Sci Rep. 2018 Jul 3;8(1):10064
MCF7 cells
10 μM
16 hours
To validate the inhibitory effects of MYCMI-6 on endogenous MYC:MAX interaction
Sci Rep. 2018 Jul 3;8(1):10064
HEK293 cells
25 μM
24 hours
To validate the inhibitory effects of MYCMI-6 on MYC:MAX interaction
Sci Rep. 2018 Jul 3;8(1):10064
MYCMI-6 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
SK-N-DZ neuroblastoma xenograft model
Intraperitoneal injection
20 mg/kg body weight
Daily for 1-2 weeks
To evaluate the inhibitory effects of MYCMI-6 on MYCN:MAX interaction in vivo and its impact on tumor growth
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