ITC
OICR-9429 disrupts WDR5 interaction with a peptide from WDR5-interacting protein Kdisp = 64 nM.
PDB ID for probe-target interaction (3D structure):
4E5G
Potency assay (off target):
No activity detected against 9 WDR40 or epigenetic reader proteins.
Probe Selectivity in Vitro:
No binding or inhibition was detected against 22 protein methyltransferases.
Negligible activity was detected against >250 human kinases, GPCRs, ion channels (Cerep) at 1 uM.
In cell validation
Potency in cells:
IC50
223 nM
Potency assay (cells):
OICR-9429 disrupted WDR5-MLL interaction as well as C/EBPalpha p30-WDR5 interaction in cells.
Target engagement assay (cells):
A biotinylated version of OICR-9429 selectively pulled down WDR5 in cells.