OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.

WDR5-IN-1 is a potent and selective inhibitor of WD repeat domain 5 (WDR5) (Kd <0.02 nM), and also inhibits MLL1 histone methyltransferase (HMT) activity (IC50: 2.2 nM).

MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM. MM-102 compound prevents the interaction between mixed lineage leukemia 1 (MLL1) and WD Trp-Asp repeat domain 5 (WDR5) and results in the inhibition of MLL1 H3K4 histone methyltransferase (HMT) activity. Down-Regulation of H3K4me3 by MM-102 Facilitates Epigenetic Reprogramming of Porcine Somatic Cell Nuclear Transfer Embry

WDR5-IN-5 is a selective, orally active inhibitor targeting the WD repeat domain 5 (WDR5) WIN site.WDR5-IN-5 exhibits high affinity for WDR5 (Ki<0.02 nM).WDR5-IN-5 exhibits anti-cancer cell proliferation and a good pharmacokinetic profile.

MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.

MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.