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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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Givinostat

Category:HDACi
Cas Number:497833-27-9
Molecular Formula:C24H27N3O4
Molecular Weight:421.48888 g/mol
Smiles:CCN(CC)CC1=CC2=C(C=C1)C=C(C=C2)COC(=O)
NC3=CC=C(C=C3)C(=O)NO
Description:HDAC Inhibitor ITF2357 is an orally bioavailable hydroxymate inhibitor of histone deacetylase (HDAC) with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. Givinostat inhibits class I and class II HDACs, resulting in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression. At low, nonapoptotic concentrations, this agent inhibits the production of pro-inflammatory cytokines such as tumor necrosis factor- (TNF-), interleukin-1 (IL-1), IL-6 and interferon-gamma. Givinostat has also been shown to activate the intrinsic apoptotic pathway, inducing apoptosis in hepatoma cells and leukemic cells. This agent may also exhibit anti-angiogenic activity, inhibiting the production of angiogenic factors such as IL-6 and vascular endothelial cell growth factor (VEGF) by bone marrow stromal cells.
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (9.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex

Disease list

ConditionsDrug NameStatusNct NumberPhases
Hodgkin’s lymphomaGivinostatTerminatedNCT00496431Phase 1 2
Hodgkin’s lymphomaGivinostatCompletedNCT00792467Phase 1 2
Myeloproliferative diseasesGivinostatCompletedNCT00606307Phase 2
Chronic lymphocytic leukemiaGivinostatTerminatedNCT00792831Phase 2
Polycythemia veraGivinostatCompletedNCT00928707Phase 2
primary pediatric T-ALLGivinostat Preclinical study
healthySuberoylanilide hydroxamic acid
Romidepsin
Givinostat
abexinostat
Preclinical study
Hodgkin lymphomaGivinostatPreclinical study
healthyGivinostatPreclinical study
bladder cancerRomidepsin
Givinostat
Suberoylanilide hydroxamic acid
Preclinical study
Hodgkin lymphomaGivinostatPreclinical study
Hodgkin lymphomaGivinostatPreclinical study

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
Specific molecular signatures underlie response to decitabine in CMML [ERRBS] GivinostatHDACihuman primary pediatric T-ALL cells26764573
Inhibition of class I histone deacetylases 1 and 2 promotes urothelial carcinoma cell death by various mechanisms (HDAC inhibitor treatments) Suberoylanilide hydroxamic acid
Romidepsin
Givinostat
abexinostat
HDACihuman VM-CUB1 cells human UM-UC-3 cells26772204
Gene expression analysis of Hodgkin lymphoma cell lines treated with the AKT inhibitor perifosine and the multikinase inhibitor sorafenib GivinostatHDACihuman HDLM-2 Hodgkin lymphoma cell line24561519
23360848
The HDAC inhibitor Givinostat modulates key hematopoietic genes in JAK2V617F cells, affecting proliferation, differentiation and apoptosis GivinostatHDACihuman JAK2V617F cell lines (HEL, UKE1 and SET2) 22579713
Inhibition of class I histone deacetylases 1 and 2 promotes urothelial carcinoma cell death by various mechanisms (HDAC inhibitor treatments) Romidepsin
Givinostat
Suberoylanilide hydroxamic acid
HDACiVM-CUB1 and UM-UC-3 cells26772204
TGene expression profiling of HDLM-2 Hodgkin lymphoma cell line after in vitro and in vivo treatment with Givinostat in combination with Sorafenib GivinostatHDACiHDLM-2 Hodgkin lymphoma cell line24561519
Gene expression profiling of L-540 Hodgkin lymphoma cell line after in vitro and in vivo treatment with Givinostat in combination with Sorafenib GivinostatHDACiL-540 Hodgkin lymphoma cell line24561519

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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