Dot1l-in-2 is an effective, selective and oral bioutilization inhibitor of histone methyltransferase Dot1L, with IC50 and Ki of 0.4 nM and 0.08 nM, respectively.

DOT1L:(ki)0.08 nM , DOT1L:0.4 nM

Dot1l-in-2 is an effective and selective Dot1L inhibitor with IC50 and Ki of 0.4 nM and 0.08 nM, respectively.Dot1l-in-2 effectively inhibits H3K79 dimethylation (IC50, 16 nM) and blocks the activity of the HoxA9 promoter (IC50, 340 nM) IN the cellular system.Dot1l-in-2 also significantly inhibited the proliferation of human mll-recombinant leukemia cell line mv4-11 carrying carcinogenic mll-af4 fusion (IC50, 128nm).