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.
For more information about how EPZ 004777 may be used, see our protocol:Highly Efficient Generation of CiPSCs from MEFs
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.
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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