MM-401 TFA is a potent inhibitor of MLL1/WDR5 protein-protein interaction with IC50 of 0.9 nM. MM-401 represents over 3 and 700 folds more potency relative to MM-101 (IC50=2.9 nM) and the WDR5-interacting motif in MLL1 (WIN, IC50=750 nM). MM-401 specifically blocks proliferation of MLL cells and induces changes in gene expression similar to those of MLL1 deletion. MM-401 reprograms mouse epiblast stem cells (EpiSCs) to naive pluripotency.
