MDEG-541 is a small molecule MYC PROTAC degrader, induces cereblon-dependent degradation of MYC, GSPT1/2, and PLK1. MDEG-541 is based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide. MDEG-541 regulates MYC in a fashion dependent on CRBN, ubiquitination, and the proteasome, the compound acts pleiotropic and also decreased the expression of G1 To S Phase Transition 1 (GSPT1), GSPT2, and the Polo-like kinase 1 (PLK1). MDEG-541 shows cellular activity in conventional gastrointestinal cancer cell lines and primary cancer organoids.
