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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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JIB-04

Category:HDMi
Cas Number:199596-05-9
Molecular Formula:C17H13ClN4
Molecular Weight:308.76492g/mol
Smiles:C1=CC=C(C=C1)C(=NNC2=NC=C(C=C2)Cl)C3=CC=CC=N3
Description:JIB-04, which specifically inhibits the activity of the Jumonji family of histone demethylases in vitro, in cancer cells, and in tumors in vivo. Unlike known inhibitors, JIB-04 is not a competitive inhibitor of α-ketoglutarate. In cancer but not in patient-matched normal cells, JIB-04 alters a subset of transcriptional pathways and blocks viability. In mice, JIB-04 reduces tumor burden and prolongs survival. Importantly, we find that patients with breast tumors that overexpress Jumonji demethylases have significantly lower survival. Thus JIB-04, a novel inhibitor of Jumonji demethylases in vitro and in vivo, constitutes a unique potential therapeutic and research tool against cancer, and validates the use of unbiased cellular screens to discover chemical modulators with disease relevance.
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (6.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex

Disease list

ConditionsDrug NameStatusNct NumberPhases
lung cancerJIB-04Preclinical study

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
Identification of genes modulated by JIB-04 in lung cancer cells JIB-04HDMihuman H358 lung cancer cells the patient matched HCC4017 (cancer) human HBEC30KT (immortalized normal) lung cell23792809

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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