Catalog No.: PC-49061Not For Human Use, Lab Use Only.
WDR5 PROTAC MS40 is a cereblon (CRBN)-recruiting proteolysis targeting chimera (PROTAC) of WDR5, selectively degrades WDR5 and the Ikaros zinc finger (IKZF) transcription factors IKZF1 and IKZF3.
WDR5 PROTAC MS40 is a cereblon (CRBN)-recruiting proteolysis targeting chimera (PROTAC) of WDR5, selectively degrades WDR5 and the Ikaros zinc finger (IKZF) transcription factors IKZF1 and IKZF3.
MS40-induced WDR5 degradation caused disassociation of the MLL/KMT2A complex off chromatin, resulting in decreased H3K4me2.
MS40 repressed transcriptomic profiling revealed that targets of both WDR5 and the well-established neo-substrates of immunomodulatory drugs (IMiDs):CRBN.
MS40 suppressed the growth of primary leukemia patient cells in vitro and patient-derived xenografts in vivo.
MS40 is superior in suppressing oncogenesis to the WDR5 PPI inhibitor and to VHL-based WDR5 PROTAC (MS169, which degrades WDR5 but not Ikaros).
