EPZ 004777

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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% (HPLC)
Citations (1)
Protocols (1)

Biological Activity for EPZ 004777

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

Licensing Information

Sold under license from Epizyme, Inc.

External Portal Information for EPZ 004777

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.

Compound Libraries for EPZ 004777

EPZ 004777 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for EPZ 004777

M. Wt 539.67
Formula C28H41N7O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1338466-77-5
PubChem ID 56962336
Smiles NC1=C2C(N([C@H]3[C@H](O)[C@H](O)[C@@H](CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C)O3)C=C2)=NC=N1

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.

Solubility Data for EPZ 004777

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 53.97 100
ethanol 53.97 100

Preparing Stock Solutions for EPZ 004777

The following data is based on the product molecular weight 539.67. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.85 mL 9.26 mL 18.53 mL
5 mM 0.37 mL 1.85 mL 3.71 mL
10 mM 0.19 mL 0.93 mL 1.85 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

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Product Datasheets for EPZ 004777

Certificate of Analysis / Product Datasheet
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References for EPZ 004777

References are publications that support the biological activity of the product.

Yu et al (2012) Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat.Commun. 3 1288 PMID: 23250418

Onder et al (2012) Chromatin-modifying enzymes as modulators of reprogramming. Nature 483 598 PMID: 22388813

If you know of a relevant reference for EPZ 004777, please let us know.

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Keywords: EPZ 004777, EPZ 004777 supplier, EPZ004777, highly, potent, DOT1L, methyltransferases, histones, inhibitors, inhibits, HMTs, MLL, leukemia, mll-rearranged, H3K79me, Lysine, Methyltransferases, Other, Stem, Cell, Reprogramming, 5567, Tocris Bioscience

1 Citation for EPZ 004777

Citations are publications that use Tocris products. Selected citations for EPZ 004777 include:

Ebrahimi et al (2019) Bromodomain inhibition of the coactivators CBP/EP300 facilitate cellular reprogramming. Nat.Chem.Biol 15 519 PMID: 30962627

Do you know of a great paper that uses EPZ 004777 from Tocris? Please let us know.

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Protocols for EPZ 004777

The following protocol features additional information for the use of EPZ 004777 (Cat. No. 5567).