Biological Activity:OICR9429 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist (Kd ~24-52 nM). It has >100-fold selectivity over other methyltransferases tested. It disrupts WDR5 interaction with peptide regions of MLL and Histone 3. OICR-9429 also disrupts the interaction of WDR5 with MLL1 and RbBP5 in cells with IC50 values below 1 μM.How to Use:In vitro: OICR9429 was used at 5-10 μM final concentration in various in vitro assays.In vivo: n/a Reference:
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