EN219 is a fully synthetic covalent ligand that targets RNF114, recruites the E3 ubiquitin ligase RNF114 for targeted protein degradation.
EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM.
EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination.
EN219 can be used as an RNF114 recruiter in degrader applications (RNF114-based PROTACs).
