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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Molecular structure representations generated using Open Babel