Chemical Name: 7-[5-Deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Biological ActivityHighly 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.
External Portal InformationChemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of EPZ004777 is reviewed on the chemical probes website.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu et al.
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