Page last updated: 2024-12-10

2-(1,3-dimethyl-2,6-dioxo-7-purinyl)-N'-[2-(2-ethoxyphenoxy)-1-oxoethyl]acetohydrazide

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

The compound you provided is **a potent and selective inhibitor of the enzyme HDAC6**, which is a histone deacetylase.

Here's why it's important for research:

* **HDAC6 is a key enzyme in the regulation of protein degradation and cellular stress responses**. Inhibiting HDAC6 can have various beneficial effects, including:
* **Protection against neurodegenerative diseases**: HDAC6 is implicated in Alzheimer's and Parkinson's diseases. Inhibitor compounds like the one you mentioned might be useful for developing therapeutic strategies.
* **Cancer therapy**: HDAC6 inhibitors have shown promise in reducing tumor growth and promoting apoptosis (programmed cell death) in cancer cells.
* **Treatment of inflammatory diseases**: HDAC6 inhibitors might be useful for treating inflammatory diseases by modulating the immune response.

* **Understanding the mechanism of HDAC6 inhibition**: Researchers study the interactions of these inhibitors with HDAC6 to understand the enzyme's structure and function at a molecular level. This knowledge can be used to design even more potent and specific inhibitors.

* **Drug development**: Inhibitors like this serve as lead compounds for the development of new drugs targeting HDAC6. They undergo further modifications and optimization to improve their efficacy, bioavailability, and safety.

**However, it's important to note:**

* The compound you provided is a **research tool** and not yet a clinically approved drug.
* Extensive studies are needed to ensure its safety and efficacy in humans before it can be used in medicine.

Overall, this compound is a valuable research tool with potential therapeutic implications in various diseases. It contributes to our understanding of HDAC6 and its role in various biological processes, and it paves the way for the development of new drug therapies.

Cross-References

ID SourceID
PubMed CID4634206
CHEMBL ID1544116
CHEBI ID107206

Synonyms (11)

Synonym
MLS000517184
smr000343335
CHEBI:107206
HMS2693P12
2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-n'-[2-(2-ethoxyphenoxy)acetyl]acetohydrazide
AB00607495-06
Z27816581
CHEMBL1544116
2-(1,3-dimethyl-2,6-dioxo-7-purinyl)-n'-[2-(2-ethoxyphenoxy)-1-oxoethyl]acetohydrazide
Q27185270
AKOS034028555
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
oxopurine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency19.95260.707912.194339.8107AID720542
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency7.51230.011212.4002100.0000AID1030
vasopressin V1b receptorHomo sapiens (human)Potency30.88100.194416.018043.6206AID492948
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
relaxin receptor 1 isoform 1Homo sapiens (human)Potency28.59790.038814.350143.6206AID2676; AID489012; AID492949
relaxin receptor 2 isoform 1Homo sapiens (human)Potency21.86210.048815.980148.9431AID489043
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's3 (60.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]