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The Human Epigenetic Drug Database (HEDD) is a comprehensive web-based database for epigenetic drugs, which focuses on the storage and integration of epigenetic drug datasets that were obtained from laboratory experiments that is essential for understanding the mechanism of action of these epigenetic drugs at a systematic level.

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EPZ004777

Category:HMTi
Cas Number:1338466-77-5
Molecular Formula:C28H41N7O4
Molecular Weight:539.66964 g/mol
Smiles:CC(C)N(CCCNC(=O)NC1=CC=C(C=C1)C(C)(C)C)CC2C(C(C(O2)N3C
=CC4=C3N=CN=C4N)O)O
Description:EPZ004777 selective inhibition of cell H3K79 methylation and restrain key MLL fusion expression of target genes.DOT1L inhibition, selective inhibition of MLL gene rearrangement EPZ004777 cell lines and MLL - AF9 transformation of hematopoietic cell proliferation in mice.In addition, EPZ004777 ACTS on the MLL gene rearrangement of cell lines, differentiation and apoptosis.EPZ004777 selective inhibition of MLL - AF10 and reflux - AF10 transformation of hematopoietic cell proliferation in mice.After DOT1L EPZ004777 suppression, significantly reduce proliferation, reduce MLL - AF6 target gene expression, and MLL - AF6 transformation of hematopoietic cells in mice in the stagnation of the cell cycle.
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (11.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex
1226 EPZ004777Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))238794634ER3(100%)
4EKI(100%)
4ER5(100%)
1227 EPZ004777Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))254068534ER3(100%)
4EKI(100%)
4ER5(100%)
1228 EPZ004777Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))4ER3(100%)
4EKI(100%)
4ER5(100%)
1229 EPZ004777Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))4ER3(100%)
4EKI(100%)
4ER5(100%)
1230 EPZ004777Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))254068534ER3(100%)
4EKI(100%)
4ER5(100%)
1231 EPZ004777Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))254068534ER3(100%)
4EKI(100%)
4ER5(100%)
1232 EPZ004777Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))254068534ER3(100%)
4EKI(100%)
4ER5(100%)
1233 EPZ004777Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))234336704ER3(100%)
4EKI(100%)
4ER5(100%)
1234 EPZ004777Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))4ER3(100%)
4EKI(100%)
4ER5(100%)
1235 EPZ004777Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))238794634ER3(100%)
4EKI(100%)
4ER5(100%)

Disease list

ConditionsDrug NameStatusNct NumberPhases
MLLEPZ004777Preclinical study
healthyEPZ004777Preclinical study
leukemiaEPZ004777Preclinical study
breast cancerEPZ004777 Preclinical study

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
Expression Profiling of Mixed Lineage Leukemia Cells Treated with a Potent Small-Molecule DOT1L Inhibitor EPZ004777HMTihuman Cell lines bearing MLL translocations (MV4-11 and MOLM-13)21741596
Gene expression changes upon Dot1L knockdown and Dot1L inhibitor treatment during reprogramming EPZ004777HMTiEmbryonic stem cell-derived fibroblasts (dH1fs)22388813
The Histone Methyltransferases MLL1 and DOT1L Cooperate with Meningioma-1 to Induce AML EPZ004777HMTihuman leukemia cell lines26927674
Expression profiling of MDA-MB-231 breast cancer cells treated with DOT1L inhibitors and siDOT1L EPZ004777HMTiMDA-MB-231 breast cancer cells?25359765

Complex list

PDBIdDrug NameTargetmethodPubmedId
4EKI EPZ004777Histone-lysine N-methyltransferase, H3 lysine-79 specific (Homo sapiens)X-RAY DIFFRACTION22978415
4ER3 EPZ004777Histone-lysine N-methyltransferase, H3 lysine-79 specific (Homo sapiens)X-RAY DIFFRACTION
4ER5 EPZ004777Histone-lysine N-methyltransferase, H3 lysine-79 specific (Homo sapiens)X-RAY DIFFRACTION

About

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The Human Epigenetic Drug Database (HEDD) is a comprehensive web-based database for epigenetic drugs, which focuses on integrating epigenetic drug studies based Omics data from high through experiments that is essential for understanding the mechanism of action of these epigenetic drugs at a systematic level.

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©2016 Group of Computational Epigenomics and Bioinformatics, College of Life Science, Jilin Normal University, China

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