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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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GSK343

Category:HMTi
Cas Number:1346704-33-3
Molecular Formula:C31H39N7O2
Molecular Weight:541.68706 g/mol
Smiles:CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=
CC(=NC=C4)N5CCN(CC5)C)C(C)C
Description:GSK343 inhibit H3K27 three methylation of the H3K27me3) in HCC1806 lung cancer cells, the IC50 of 174 nM.GSK343 effectively inhibit breast cancer cells and prostate cancer cell proliferation, prostate cancer cells is LNCaP's most sensitive to GSK343, IC50 of 2.9 microns.GSK343 significantly inhibit the growth of EOC cell, EOC cell in the simulation of the tumor microenvironment in vivo 3 d human basement membrane in the extracellular matrix (ECM) were sent to culture.GSK343 will induce the EOC cell apoptosis in 3 d, and significantly inhibit the infection of EOC cell.
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (10.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex
1176 GSK343EZH2/SUZ12/EED/RBBP7/RBBP4 (Homo sapiens (Human))
1177 GSK343Histone-lysine N-methyltransferase 2A (Homo sapiens)
1178 GSK343Histone-lysine N-methyltransferase SUV39H1 (Homo sapiens)
1179 GSK343Histone-lysine N-methyltransferase SETMAR (Homo sapiens)
1180 GSK343Histone-lysine N-methyltransferase SETD7 (Homo sapiens)
1181 GSK343PRMT5/MEP50 complex (Homo sapiens)
1182 GSK343Protein arginine methyltransferase 4 (PRMT4) (Homo sapiens (Human))
1183 GSK343Protein arginine methyltransferase 3 (PRMT3) (Homo sapiens (Human))
1184 GSK343Protein arginine methyltransferase 1 (PRMT1) (Homo sapiens (Human))
1185 GSK343Histone-lysine N-methyltransferase MLL4 (Homo sapiens)
1186 GSK343Histone-lysine N-methyltransferase MLL3 (Homo sapiens)
1187 GSK343Histone-lysine N-methyltransferase MLL2 (Homo sapiens)
1188 GSK343Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)
1189 GSK343Histone H3-K79 methyltransferase (DOT1L) (Homo sapiens (Human))
1190 GSK343DNA (cytosine-5)-methyltransferase 3B (Mus musculus)
1191 GSK343DNMT3A2/3L complex (Homo sapiens)
1192 GSK343DNA (cytosine-5)-methyltransferase 1 (Homo sapiens)
1193 GSK343EZH2/SUZ12/EED/RBBP7/RBBP4 (Homo sapiens (Human))
1194 GSK343Histone-lysine N-methyltransferase SUV39H2 (Homo sapiens)

Disease list

ConditionsDrug NameStatusNct NumberPhases
multiple myelomaGSK343Preclinical study
healthyGSK343
GSK126
Preclinical study

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
Treatment of multiple myeloma cells with EZH2 small molecule inhibitor GSK343HMTihuman multiple myeloma cell lines ( KMS11, TKO)25188243
PRC2 inhibition counteracts the culture-associated loss of engraftment potential of human cord blood-derived hematopoietic stem and progenitor cells GSK343
GSK126
HMTiCord blood hematopoietic stem cells (CB-HSCs)26198814

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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