GNE-987 represents a PROTAC that combines ligands for von Hippel-Lindau and BRD4. It demonstrates highly potent cell BRD4 degradation activity at the picomolar level, and it features a robust BET binder/inhibitor, a fragment that binds to VHL, and a spacer moiety with ten methylene units. Additionally, GNE-987 holds applicability in PROTAC-Antibody Conjugate (PAC) approaches.
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