EPZ 004777
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%
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 MEFsExternal 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
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
Background References
-
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu et al.
Nat.Commun., 2012;3:1288 -
Chromatin-modifying enzymes as modulators of reprogramming.
Onder et al.
Nature, 2012;483:598
Product Datasheets
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.
Nat.Chem.Biol 2019;15:519
FAQs
No product specific FAQs exist for this product, however you may
View all Small Molecule FAQsReviews for EPZ 004777
There are currently no reviews for this product. Be the first to review EPZ 004777 and earn rewards!
Have you used EPZ 004777?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
