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EN4 is a covalent inhibitor of c-Myc.1 It inhibits c-Myc-induced increases in transcriptional activity in a reporter assay using HEK293T cells (EC50 = 12.5 µM). EN4 (1, 10, or 50 µM) reduces the proliferation of 231MFP breast cancer cells. In vivo, EN4 (50 mg/kg per day) decreases tumor volume in a 231MFP mouse xenograft model.
WARNING This product is not for human or veterinary use.
1. Discovery of a functional covalent ligand targeting an intrinsically disordered cysteine within MYC. Cell Chem. Biol. 28(1), 4-13 (2021).