WDR5 WIN site inhibitor 16 is a potent, selective inhibitor of WD repeat domain 5 (WDR5) WIN site with TR-FRET Kd of <0.02 nM, exhibits histone methyltransferase inhibition with IC50 of 2.2 nM.
WDR5 WIN site inhibitor 16 is a potent, selective inhibitor of WD repeat domain 5 (WDR5) WIN site with TR-FRET Kd of <0.02 nM, exhibits histone methyltransferase inhibition with IC50 of 2.2 nM.
WDR5 WIN site inhibitor 16 displaced WDR5 from chromatin and repressed mRNA expression of WDR5-bound genes.
WDR5 WIN site inhibitor 16 (0.01-3 uM) induced p53 and p21 protein levels and apoptosis in MV4:11 cells.
WDR5 WIN site inhibitor 16 displaced MYC from chromatin at WDR5-displaced genes.
WDR5 WIN site inhibitor 16 exhibited potent anti-proliferative activity against MYC-driven cancer cells, including CHP-134 (neuroblastoma, wt p53, GI50=0.26 uM) and Ramos (Burkitt's lymphoma, mutant p53, GI50=0.49 uM).
