Both compounds are potent inhibitors of DOT1L with IC50 values of 1.4 and 0.4 nM, respectively, inhibited the proliferation of MLL-rearranged leukemia cell line MV4-11 (IC50 = 85 and 128 nM, respectively), and were selective against a panel of 22 PMTs. Here, KMT2A is linked to leukemia.