VHL Spy Molecules for Ligand Discovery

Targeted protein degradation utilizes E3 ubiquitin ligases to mediate the disposal of target proteins from the cell. One of the most validated E3 ligases is von Hippel-Lindau (VHL), which is recruited by the VH032 ligand1. Using VH032 as a template, fluorinated reporter molecules were designed by Alessio Ciulli′s lab to indicate (or "spy" on) binding of other molecules to VHL through ligand-observed 19F NMR screening,2 facilitating the identification of novel VHL ligands and VHL-based degraders (such as PROTAC molecules).

Learn more about targeted protein degradation and PROTAC research from Professor Alessio Ciulli in our recent webinar with the Royal Society of Chemistry: Targeted protein degradation using small molecules.

To simplify the synthesis and library generation of protein degraders, visit our portal page that brings together our growing collection of Partial Degraders, ligands, crosslinkers, and other tools for protein degradation research.

1. Galdeano, C.; Gadd, M. S.; Soares, P.; Scaffidi, S.; van Molle, I.; Birced, I.; Hewitt, S.; Dias, D. M.; Ciulli, A. J. Med. Chem. 2014, 57, 8657
2. de Castro, G. V.; Ciulli, A. Chem. Commun. 2019, 55, 1482.

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

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Molecular Formula

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909416 Fluorinated VHL spy molecule 1 C23H28F3N3O3S
909432 Fluorinated VHL Spy Molecule 2 ≥98% C14H14BrF3N2O3
909440 Fluorinated VHL spy molecule 3 ≥95% C18H18F3N3O3S
909459 Fluorinated VHL Spy Molecule 4 ≥98% C15H16BrF3N2O3