Synonyms: EN-450
Compound class:
Synthetic organic
Comment: A chemoproteomic approach identified EN450 as a molecular glue type degrader of the (oncogenic) transcription factor NF-κB1 [1]. It binds covalently to an E2 ubiquitin-conjugating enzyme (most likely UBE2D1 and UBE2D4), and this initiates the formation of a ternary complex with NF-κB1 that ultimately promotes proteasome-dependent degradation of NF-κB1. This mechanism impairs viability of leukemia cells in vitro.
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References |
1. King EA, Cho Y, Hsu NS, Dovala D, McKenna JM, Tallarico JA, Schirle M, Nomura DK. (2023)
Chemoproteomics-enabled discovery of a covalent molecular glue degrader targeting NF-κB. Cell Chem Biol, 30 (4): 394-402.e9. [PMID:36898369] |