Highly potent DOT1L inhibitor (IC50
= 0.4 nM). Exhibits >1000-fold selectivity for DOT1L over a panel of other methyltransferases. Selectively inhibits proliferation and induces apoptosis of MLL
-rearranged cells in vitro
. Prolongs survival in a MLL xenograft mouse model.
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Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu et al.