While we were initially interested in HKMTI-1-005 as an EZH2 inhibitor, evidence of a role for G9A in AML pathogenesis (Lehnertz et al., 2014) and maintenance of a cancer stem cell phenotype (Haebe et al., 2021) suggested that the dual inhibitory activities of HKMTI-1-005 could be therapeutically advantageous in the context of AML. This evidence concerns the gene EZH2 and acute myeloid leukemia.