Proteolysis targeting chimeras (PROTACs) are therapeutic agents designed to induce selective intracellular degradation of pathogenic proteins. They consist of two covalently linked ligands: one binds to the target protein, while the other recruits an E3 ubiquitin ligase to tag the unwanted protein for degradation. Ciulli and coworkers developed several efficient small-molecule ligands that recruit the von Hippel-Lindau (VHL) E3 ubiquitin ligase for the degradation tagging, among them VH032, VH101, and VH298 with nanomolar binding affinity. Few PROTACs utilizing the VHL ligase – DT2216, PRT3789, ASP3082, and KT333 – have advanced to clinical trials. At Enamine, we provide building blocks related to VH101, including diverse attachment sites and structural modifications. Additionally, we offer support for the synthesis of custom PROTAC molecules that feature a range of linkers and protein binders.
We offer
Over 500 von Hippel-Lindau ligands from stock.
