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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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C646

Category:HATi
Cas Number:328968-36-1
Molecular Formula:C24H19N3O6
Molecular Weight:445.42416 g/mol
Smiles:CC1=C(C=C(C(=C1)C2=CC=C(O2)C=C3C(=NN(C3=O)C4=CC=C(C=C4)C
(=O)O)C)[N+](=O)[O-])C
Description:C646 is a kind of histone acetyltransferase inhibitors, inhibition of p300, Ki is 400 nM, selective effects on other acetyl transferase.10 microns C646 p300 in vitro inhibition of 86%.C646 is traditional, reversible p300 inhibitors.C646 (25 microns) effects on cells, reduce the histone H3 and H4 acetylation level, and the abolition of the acetylation induced by the TSA.C646 (20 microns) applies to castration of androgen sensitive department of prostate cancer cells, by interfering with AR and NF - kB pathways, and induce cell apoptosis.C646 effects on cells in mice, inhibit all H3K4me3 dynamic acetylation, and local starting sites across the promoter and induced genes, thus interference RNA polymerase II interactions and the activation of these genes.
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (8.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex

Disease list

ConditionsDrug NameStatusNct NumberPhases
colon cancer
pancreatic cancer
C646Preclinical study
healthyC646 Preclinical study
healthyC646Preclinical study
healthyC646
GSK126
KDM5-C70
Preclinical study

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
Combinatorial pharmacological approaches target EZH2-mediated gene repression in breast cancer cells C646HATihuman HCT116 colon cancer cells ; PANC1 pancreatic cancer cells
C646, a Novel p300/CREB-Binding Protein-Specific Inhibitor of Histone Acetyltransferase, Attenuates Influenza A Virus Infection C646HATihuman A549 cells26711748
Expression profile of melanoma cells following p300 HAT inhibition C646HATihuman WM35 cells23698071
A multiplexed system for quantitative comparisons of chromatin landscapes C646
GSK126
KDM5-C70
HATi
HMTi
KDMi
K562 cells SKM-1 and Toledo cells Human HSCs 26687680

Complex list

PDBIdDrug NameTargetmethodPubmedId

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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