Welcome to HEDD

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.

read more

KDM5-C70

Category:HDMi
Cas Number:N.A.
Molecular Formula:C17H28N4O3
Molecular Weight:336.42922 g/mol
Smiles:CCN(CCN(C)C)C(=O)CNCC1=NC=CC(=C1)C(=O)OCC
Description:KDM5-C70 is an ethyl ester derivative of KDM5-C49, which is a potent and selective inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases. The highly polar carboxylate group of KDM5-C49 restricts its cellular permeability; therefore KDM5-C70 was developed as a pro-drug, masking the polarity of the acid group of the KDM5-C49, for cellular assays and in vivo use. It has IC50 <1 µM for KDM5B (or PLU1) and UTX in histone lysine demethylase AlphaLISA assays, very good selectivity over JMJD1B, JMJD2A, JMJD2B and JMJD3. It has IC50 <1 µM for inhibiting demthylation of H3K4 in U2OS human osteosarcoma cell line. KDM5-C70 also suppresses human breast adenocarcinoma MCF7 tumor cell proliferation with IC50 < 1 µM.
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (7.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex

Disease list

ConditionsDrug NameStatusNct NumberPhases
healthyC646
GSK126
KDM5-C70
Preclinical study
multiple myeloma MM1SKDM5-C70Preclinical study

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
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
H3K4me3 ChIP in multiple myeloma MM1S cells in the presence and absence of KDM5-C70 KDM5-C70HDMimultiple myeloma MM1S cells27214403

Complex list

PDBIdDrug NameTargetmethodPubmedId

About

pix

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.

Copyright

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

吉ICP备16005872号