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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.
Sold under license from Epizyme, Inc.
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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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.
|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|
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
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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
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