The proto-oncogene c-myc encodes a transcription factor c-Myc, which is of great importance in controlling cell growth and vitality[1]. The heterodimerization of c-Myc with Myc-associated factor X (MAX) plays a critical role in the proliferation, transformation, and apoptosis. Mycro3 is a small-molecule inhibitor of Myc-Max dimerization and also inhibit c-Myc/Max/DNA binding[2]. c-Myc has become an interesting and feasible target for novel therapies of a variety of human malignancies related to c-Myc, Mycro3 may be a novel and effective therapeutic agents to treat cancer.
Mechanism: Mycro-3 is shown to bind one of the three discrete binding sites on the c-Myc bHLH-Zip domain[3].
Mycro 3 细胞实验
Cell Line
Concentration
Treated Time
Description
References
CD8 T cells
above 100 μM
2 days
Mycro3 had almost no effect on CD8 T cells at those concentrations. When the Mycro3 concentration was increased by 10-fold to above 100 μM, the metabolic activities of all T cell subsets were inhibited
Cell Mol Immunol. 2022 Sep;19(9):1030-1041
AsPC-1 cells
5000 nM
4 hours
To evaluate the effect of Mycro3 on the migration and invasion capabilities of pancreatic cancer cells. Results showed that Mycro3 significantly reduced the migratory and invasive abilities of AsPC-1 cells.
Cancer Cell Int. 2021 Dec 14;21(1):670
Mycro 3 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
B16F10 mouse melanoma model
Intraperitoneal injection
100 mg/kg body weight
Once every 3 days for a total of four cycles
Mycro3 significantly reduced tumor volume, increased immune cell infiltration in tumors, and sensitized tumors to anti-PD-1 treatment by modulating the tumor microenvironment, including decreasing Treg cells and increasing CD8 T cells
Cell Mol Immunol. 2022 Sep;19(9):1030-1041
SCID mice
Metastatic mouse model
Intragastric administration
100 mg/kg/d
Once daily
To evaluate the inhibitory effect of Mycro3 on pancreatic cancer cell metastasis in vivo. Results showed that Mycro3 alone did not show significant anti-metastatic effects in vivo.
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