MS41 is a highly potent and selective PROTAC degrader of eleven-nineteen leukemia (ENL) that recruits the von Hippel–Lindau (VHL) E3 ubiquitin ligase, with DC50 values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). It effectively inhibits the growth of ENL-dependent leukemia cells by inducing G1 cell cycle arrest and increasing apoptosis, reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression in both cellular and xenograft mouse models.
Structure of 2768610-97-3
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