IZCZ-3 is a potent c-MYC transcription inhibitor with antitumor activity[1].
IZCZ-3 (2.1 μM-15.9 μM; 24 hours) significantly inhibits SiHa, HeLa, Huh7, and A375 cancer cell proliferation (IC50s of 3.3, 2.1，4.1, and 4.2 μM, respectively). IZCZ-3 induces only weak growth inhibition in the BJ fibroblasts (IC50=15.9 μM) and mouse mesangial cells (IC50=15.6 μM), suggesting that IZCZ-3 is more effective against cancer cells than against c-MYC-independent normal cells[1]. IZCZ-3 (0-5 μM; 12 hours) induces an apparent accumulation of cells in the G0/G1 phase in SiHa cells in a dose-dependent manner[1].
IZCZ-3 (20, 10, and 5 mg/kg; intraperitoneally; every other day for 24 days) inhibits tumor growth in BALB/c nude mice with SiHa human cervical squamous cancer xenograft[1].
[1]. Hu MH, et al. Discovery of a New Four-Leaf Clover-Like Ligand as a Potent c-MYC Transcription Inhibitor Specifically Targeting the Promoter G-Quadruplex. J Med Chem. 2018 Mar 22;61(6):2447-2459.