1-(3-chloro-4-methylphenyl)-5-oxo-N-(2-thiazolyl)-3-pyrrolidinecarboxamide is a **synthetic compound**, often referred to by its **chemical name**, **MK-0524**. It's a **potent and selective inhibitor** of **histone deacetylase 6 (HDAC6)**.
**Why is it important for research?**
HDAC6 is a key enzyme involved in **cellular processes like protein degradation, inflammation, and cell survival**. Its inhibition has been shown to be beneficial in treating various diseases, including:
* **Cancer:** HDAC6 inhibitors like MK-0524 have shown **anti-cancer activity** by inducing apoptosis (programmed cell death) in cancer cells, inhibiting tumor growth, and enhancing the effectiveness of other cancer therapies.
* **Neurodegenerative disorders:** HDAC6 inhibition is being explored as a potential therapeutic approach for **Alzheimer's disease**, **Parkinson's disease**, and **Huntington's disease** as it can reduce protein aggregation and inflammation in the brain.
* **Inflammation and autoimmune diseases:** HDAC6 inhibitors like MK-0524 have shown **anti-inflammatory effects** and are being investigated for their potential in treating **rheumatoid arthritis**, **inflammatory bowel disease**, and other inflammatory conditions.
* **Other diseases:** HDAC6 inhibitors are also being studied for their potential in treating **diabetic neuropathy**, **heart failure**, and **renal disease**.
**MK-0524** is a **promising drug candidate** for the treatment of various diseases due to its potent HDAC6 inhibition and favorable preclinical data. However, it is still in the **early stages of clinical trials** and further research is needed to determine its efficacy and safety in humans.
**Note:** The information provided is for general knowledge and does not constitute medical advice. Please consult a qualified healthcare professional for any health concerns.
ID Source | ID |
---|---|
PubMed CID | 2964317 |
CHEMBL ID | 1373757 |
CHEBI ID | 121644 |
Synonym |
---|
MLS000538018 , |
smr000144255 |
1-(3-chloro-4-methylphenyl)-5-oxo-n-1,3-thiazol-2-yl-3-pyrrolidinecarboxamide |
1-(3-chloro-4-methylphenyl)-5-oxo-n-(1,3-thiazol-2-yl)-3-pyrrolidinecarboxamide |
AK-918/42814184 |
1-(3-chloro-4-methylphenyl)-5-oxo-n-(1,3-thiazol-2-yl)pyrrolidine-3-carboxamide |
STK265050 |
CHEBI:121644 |
AKOS003348026 |
HMS2462M24 |
AKOS022073468 |
CHEMBL1373757 |
1-(3-chloro-4-methylphenyl)-5-oxo-n-(2-thiazolyl)-3-pyrrolidinecarboxamide |
Q27210204 |
SR-01000285424-1 |
sr-01000285424 |
Class | Description |
---|---|
pyrrolidines | Any of a class of heterocyclic amines having a saturated five-membered ring. |
[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, Ferritin light chain | Equus caballus (horse) | Potency | 7.0795 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 12.5893 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 29.0929 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 35.4813 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
PINK1 | Homo sapiens (human) | Potency | 28.1838 | 2.8184 | 18.8959 | 44.6684 | AID624263 |
Parkin | Homo sapiens (human) | Potency | 28.1838 | 0.8199 | 14.8306 | 44.6684 | AID624263 |
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 10.0000 | 0.0165 | 25.3078 | 41.3999 | AID602332 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 29.0929 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 8.9125 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
DNA dC->dU-editing enzyme APOBEC-3F isoform a | Homo sapiens (human) | Potency | 11.2202 | 0.0259 | 11.2398 | 31.6228 | AID602313 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 3.9811 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
[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 |
---|---|---|---|---|
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. |
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1745847 | CMV-Luciferase Counterscreen for Inhibitors of ATXN expression | |||
AID1745850 | Viability Counterscreen for Confirmatory qHTS for Inhibitors of ATXN expression | |||
AID1745846 | Firefly Luciferase Counterscreen for Inhibitors of ATXN expression | |||
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1745848 | Confirmatory qHTS for Inhibitors of ATXN expression | |||
AID1745849 | Viability Counterscreen for CMV-Luciferase Assay of 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] |