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 ActivityEPZ 004777 is a 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. Enhances efficiency of Yamanaka-factor factor reprogramming of fibroblasts by 3-4-fold.
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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu et al.
Chromatin-modifying enzymes as modulators of reprogramming.
Onder et al.
Citation for EPZ 004777
The citations listed below are publications that use Tocris products. Selected citations for EPZ 004777 include:
1 Citation: Showing 1 - 1
Bromodomain inhibition of the coactivators CBP/EP300 facilitate cellular reprogramming.
Authors: Ebrahimi Et al.
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