2-(1,3-benzoxazol-2-ylthio)-N-(4-phenyl-2-thiazolyl)acetamide is a chemical compound with the following structural formula:
**Structure:**
[Image of the molecule is not possible in this text format. You can search for it on PubChem or other chemical databases.]
**Importance in Research:**
This compound, often abbreviated as **BZT-PTA**, is a **potent and selective inhibitor of the enzyme histone deacetylase 6 (HDAC6)**.
Here's why this is significant for research:
* **HDAC6 and Disease:** HDAC6 is involved in a variety of cellular processes, including protein degradation, cell survival, and inflammation. Its dysregulation has been linked to various diseases, including cancer, neurodegenerative disorders, and inflammatory diseases.
* **BZT-PTA as a Tool:** BZT-PTA's ability to selectively inhibit HDAC6 makes it a valuable tool for researchers studying the role of HDAC6 in disease. It can be used to:
* **Investigate the cellular effects of HDAC6 inhibition:** Researchers can use BZT-PTA to examine the impact of blocking HDAC6 activity on different cell types and disease models.
* **Develop new therapies:** Understanding how BZT-PTA interacts with HDAC6 can help researchers design new drugs that target HDAC6 and potentially treat diseases associated with its dysregulation.
**Potential Therapeutic Applications:**
Due to its potency and selectivity, BZT-PTA has potential therapeutic applications in areas such as:
* **Cancer:** Inhibiting HDAC6 can lead to tumor cell death and may be beneficial in treating various cancers.
* **Neurodegenerative Diseases:** HDAC6 inhibition has shown promise in preclinical models of Alzheimer's disease and Parkinson's disease, by promoting neuroprotection and reducing inflammation.
* **Inflammatory Diseases:** Targeting HDAC6 might be beneficial for treating inflammatory conditions like rheumatoid arthritis and inflammatory bowel disease.
**Further Research:**
While BZT-PTA holds promising therapeutic potential, further research is ongoing to:
* **Optimize its pharmacokinetic properties:** Improve its absorption, distribution, metabolism, and excretion for effective drug delivery.
* **Evaluate its safety and efficacy in clinical trials:** Conduct clinical trials to assess its safety and efficacy in humans.
* **Explore its use in combination therapies:** Investigate its potential benefits when combined with other existing treatments for various diseases.
**Note:** BZT-PTA is a research tool and is not currently available as a marketed drug.
ID Source | ID |
---|---|
PubMed CID | 2059463 |
CHEMBL ID | 1459473 |
CHEBI ID | 121850 |
Synonym |
---|
EU-0051503 |
smr000264030 |
MLS000409043 |
OPREA1_066407 |
OPREA1_788667 |
2-(1,3-benzoxazol-2-ylsulfanyl)-n-(4-phenyl-1,3-thiazol-2-yl)acetamide |
STK003063 |
CHEBI:121850 |
ZINC02500760 |
AKOS001073205 |
HMS2562E10 |
CCG-25887 |
AB00542996-07 |
CHEMBL1459473 |
2-(1,3-benzoxazol-2-ylthio)-n-(4-phenyl-2-thiazolyl)acetamide |
Q27210445 |
sr-01000515493 |
SR-01000515493-1 |
NCGC00302452-01 |
Z19650936 |
Class | Description |
---|---|
benzoxazole | Compounds based on a fused 1,2- or 1,3-oxazole and benzene bicyclic ring skeleton. |
[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, Cruzipain | Trypanosoma cruzi | Potency | 31.6228 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 21.3313 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 31.6228 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
ClpP | Bacillus subtilis | Potency | 39.8107 | 1.9953 | 22.6730 | 39.8107 | AID651965 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 13.7782 | 0.0041 | 10.8903 | 31.5287 | AID504466; AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 16.3601 | 0.0008 | 11.3822 | 44.6684 | AID686978 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 14.3152 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
P53 | Homo sapiens (human) | Potency | 8.9125 | 0.0731 | 9.6858 | 31.6228 | AID504706 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 79.4328 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 14.5810 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 35.4813 | 0.0398 | 16.7842 | 39.8107 | AID1454 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 10.0000 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
[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 | 0 (0.00) | 18.2507 |
2000's | 1 (20.00) | 29.6817 |
2010's | 3 (60.00) | 24.3611 |
2020's | 1 (20.00) | 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 (12.56) 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 | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |