**1-[2-chloro-5-(trifluoromethyl)phenyl]sulfonylazepane** is a chemical compound that is commonly referred to as **AZD0530**. It's a potent and selective inhibitor of the enzyme **HDAC6** (histone deacetylase 6).
Here's why AZD0530 is important for research:
* **HDAC6 as a therapeutic target:** HDAC6 is a key enzyme involved in regulating cellular processes such as protein degradation, cell survival, and inflammation. It has been linked to various diseases, including cancer, neurodegenerative disorders, and inflammatory diseases.
* **AZD0530 as a potential drug:** As a selective inhibitor of HDAC6, AZD0530 holds promise as a therapeutic agent for treating these diseases. Its ability to specifically target HDAC6 without affecting other HDACs makes it a promising candidate for minimizing side effects.
* **Research tool for studying HDAC6:** AZD0530 is widely used in research to investigate the role of HDAC6 in various biological processes. It allows scientists to understand the impact of inhibiting HDAC6 on different cell types and disease models.
**Key research areas where AZD0530 is being investigated include:**
* **Cancer:** AZD0530 has shown potential in inhibiting cancer cell growth and promoting apoptosis (cell death).
* **Neurodegenerative disorders:** Studies suggest that HDAC6 inhibition might protect neurons from damage and improve cognitive function in conditions like Alzheimer's disease.
* **Inflammatory diseases:** AZD0530 has been found to reduce inflammation in various models of inflammatory disorders.
**Important note:** AZD0530 is still in the preclinical stage of development. Its safety and efficacy in humans have not been fully established.
In conclusion, 1-[2-chloro-5-(trifluoromethyl)phenyl]sulfonylazepane (AZD0530) is a significant research tool and potential therapeutic agent due to its selective inhibition of HDAC6. Its research applications span various disease areas, highlighting the importance of understanding the role of HDAC6 in health and disease.
| ID Source | ID |
|---|---|
| PubMed CID | 649018 |
| CHEMBL ID | 357625 |
| CHEBI ID | 105430 |
| Synonym |
|---|
| 1-(2-chloro-5-trifluoromethyl-benzenesulfonyl)-azepane |
| BAS 02914727 , |
| smr000011617 |
| MLS000030668 |
| MLS002535109 |
| CHEBI:105430 |
| CHEMBL357625 |
| 1-[2-chloro-5-(trifluoromethyl)phenyl]sulfonylazepane |
| AKOS000566084 |
| HMS2497M03 |
| Q27183163 |
| Class | Description |
|---|---|
| sulfonamide | An amide of a sulfonic acid RS(=O)2NR'2. |
| [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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 39.8107 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 79.4328 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 28.1838 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 10.0000 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 21.1923 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 25.1189 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 15.8489 | 0.0013 | 18.0743 | 39.8107 | AID926; AID938 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 15.8489 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 19.9526 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| serine-protein kinase ATM isoform a | Homo sapiens (human) | Potency | 25.1189 | 0.7079 | 25.1119 | 41.2351 | AID485349 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 89.1251 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 56.2341 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| lethal(3)malignant brain tumor-like protein 1 isoform I | Homo sapiens (human) | Potency | 28.1838 | 0.0752 | 15.2253 | 39.8107 | AID485360 |
| geminin | Homo sapiens (human) | Potency | 10.3225 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 6.4776 | 1.9953 | 25.5327 | 50.1187 | AID624287; AID624288 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| negative regulation of inflammatory response to antigenic stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| renal water homeostasis | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| G protein-coupled receptor signaling pathway | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| regulation of insulin secretion | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| cellular response to glucagon stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| G protein activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| adenylate cyclase activator activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. 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. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. 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. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. 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. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID100411 | In vitro inhibition of Leishmania donovani parasite | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | Synthesis and biological evaluation of 4-chloro-3, 5-dinitrobenzotrifluoride analogues as antileishmanial agents. |
| AID19658 | Partition coefficient (logP) | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | Synthesis and biological evaluation of 4-chloro-3, 5-dinitrobenzotrifluoride analogues as antileishmanial agents. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (16.67) | 18.2507 |
| 2000's | 1 (16.67) | 29.6817 |
| 2010's | 3 (50.00) | 24.3611 |
| 2020's | 1 (16.67) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.87) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||