EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism.
References:
[1]. King EA, et al. Chemoproteomics-enabled discovery of a covalent molecular glue degrader targeting NF-κB. Cell Chem Biol. 2023 Apr 20;30(4):394-402.e9.
















