OICR-9429 is a potent, selective, small-molecule antagonist of WDR5-MLL interaction that binds to WDR5 with Kd of 93±28 nM.
OICR-9429 competitively disrupts the interaction with a high-affinity Wdr5-INteracting (WIN) peptide of MLL (Kdisp=64 nM).
OICR-9429 shows no significant binding or inhibition for 22 human methyltransferases, 9 different WD40- and histone reader domains.
OICR-9429 selectively inhibits proliferation and induces differentiation in p30-expressing human AML cells.
