MS41 is a ENL PROTAC degrader with a DC 50 of 3.50 nM. MS41 recruits the VHL E3 ubiquitin ligase , triggers ENL degradation via the ubiquitin-proteasome system, and simultaneously induces AF9 degradation. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation complexes, suppresses oncogene expression, and activates differentiation gene expression. MS41 inhibits leukemia cell growth and induces cell cycle arrest and apoptosis . MS41 inhibits leukemia progression in xenograft mouse models. MS41 can be used for research on mixed lineage leukemia-rearranged leukemia and nephroblastoma. (Pink: ENL ligand ( HY-169094 ); Blue: VHL ligand ( HY-112078 ); Black: linker ( HY-W105744 )).
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