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WDR5-MYC probe 12 is an inhibitor of the protein-protein interaction between the master transcription factor Myc and WD repeat domain 5 (WDR5; IC50 = 0.39 µM).1 It reduces mRNA expression of the Myc and WDR5 co-binding target genes ribosomal protein L17 (RPL17), RPL23, RPL35, and RPL37A in HL-60 cells. WDR5-MYC probe 12 also inhibits the growth of HL-60, NB4, Ramos (RA 1), COR-L279, and NCI H520 cancer cells (GI50s = 4.2-9.4 µM).
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1. Discovery and structure-