Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a K i of 2 pM and an IC 50 of <0.1 nM. Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC 50 =3 nM), as well as the activity of the HoxA9 promoter (IC 50 =17 nM) in HeLa and Molm-13 cells, respectively.
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