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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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BIX-01294

Category:HMTi
Cas Number:935693-62-2
Molecular Formula:C28H38N6O2
Molecular Weight:490.64032 g/mol
Smiles:CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC
Description:BIX-01294 induces accumulation of LC3 II and autophagy-related cell death, but not caspase-dependent apoptosis.We profiled the global gene expression pattern after treatment with BIX-01294, in comparison with rapamycin. BIX-01294 selectively activates the downstream genes of p53 signaling, such as p21 and DOR, but not PUMA, a typical p53 target gene inducing apoptosis.BIX-01294 also induces other autophagy-related genes, such as ATG4A and ATG9A. SMYD2 is a methyltransferase for p53 and regulates its transcription activity. Its deficiency enhances the BIX-01294-induced autophagy-related cell death through transcriptionally promoting the expression of p53 target genes. Taken together, our data suggest BIX-01294 induces autophagy-related cell death and selectively activates p53 target genes, which is repressed by SMYD2 methyltransferase.
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (10.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex
1195 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)19891491
1196 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)25406853
1197 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)19891491
1198 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)(G9a)19891491
1199 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)20614940
1200 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)18800048
1201 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)(G9a)18800048
1202 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)21316248
1203 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)
1204 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)(G9a)
1205 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)(G9a)20614940
1206 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)(G9a)20614940
1207 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)20614940
1208 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)20614940
1209 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)25406853
1210 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)(G9a)25406853
1211 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)(G9a)25406853
1212 BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (Homo sapiens)(G9a)19891491

Disease list

ConditionsDrug NameStatusNct NumberPhases
healthyBIX-01294Preclinical study

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
SMYD2 specificly regulate BIX-01294 induced TP53 target genes revealed by RNA-Seq BIX-01294HMTihuman LHCT116 cells25562686

Complex list

PDBIdDrug NameTargetmethodPubmedId
3FPD BIX-01294Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (Homo sapiens)X-RAY DIFFRACTION19219047

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.

Copyright

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

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