MYC inhibitor EN4 is a covalent ligand and inhibitor of MYC, targets cysteine 171 of MYC and inhibits MYC transcriptional activity (EC50=2.8 uM).
EN4 inhibited MYC/MAX binding to the E-box response element DNA consensus sequence in a dose-responsive manner with EC50 of 6.7 uM.
EN4 directly and covalently modifies pure full-length c-MYC protein at C171 to inhibit MYC/MAX DNA binding in vitro.
EN4 engages MYC in cells, reduced MYC and MAX thermal stability in 231MFP breast cancer cells.
EN4 downregulates multiple MYC transcriptional targets, and impairs tumorigenesis.
