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EPZ 004777

Catalog #: 5567
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5567/10
EPZ 004777 | CAS No. 1338466-77-5 | Lysine Methyltransferase Inhibitors
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Description: Highly potent DOT1L inhibitor

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

Purity: ≥98%

Product Details
Citations (1)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

EPZ 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 Information

Chemicalprobes.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.

Technical Data

M.Wt:
539.67
Formula:
C28H41N7O4
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1338466-77-5

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.

Additional Information

Licensing Caveats:
Sold under license from Epizyme, Inc.

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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

  1. Bromodomain inhibition of the coactivators CBP/EP300 facilitate cellular reprogramming.
    Authors: Ebrahimi Et al.
    Nat.Chem.Biol  2019;15:519

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