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:

• 1. http://www.thesgc.org/chemical-probes/OICR-9429.