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.
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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.
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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