MI-538 is potent and selective menin-MLL interaction inhibitor (IC50=21 nM).
MI-538 shows the most potent binding affinity to menin (Kd = 6.5 nM) obtained for small molecule menin–MLL inhibitor reported to date.
MI-538 exhibits significantly increased activity, selectivity, polarity and pharmacokinetic profile over MI-136 and demonstrates a pronounced effect in a mouse model of MLL leukemia.
