Page last updated: 2024-12-10

1-(3-chloro-4-methylphenyl)-5-oxo-N-(2-thiazolyl)-3-pyrrolidinecarboxamide

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

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.

Cross-References

ID SourceID
PubMed CID2964317
CHEMBL ID1373757
CHEBI ID121644

Synonyms (16)

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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
pyrrolidinesAny 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 Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency7.07955.623417.292931.6228AID485281
glp-1 receptor, partialHomo sapiens (human)Potency12.58930.01846.806014.1254AID624417
ATAD5 protein, partialHomo sapiens (human)Potency29.09290.004110.890331.5287AID504467
TDP1 proteinHomo sapiens (human)Potency35.48130.000811.382244.6684AID686978; AID686979
PINK1Homo sapiens (human)Potency28.18382.818418.895944.6684AID624263
ParkinHomo sapiens (human)Potency28.18380.819914.830644.6684AID624263
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency10.00000.016525.307841.3999AID602332
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency29.09290.00419.984825.9290AID504444
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency8.91250.00798.23321,122.0200AID2551
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency11.22020.025911.239831.6228AID602313
Guanine nucleotide-binding protein GHomo sapiens (human)Potency3.98111.995325.532750.1187AID624287
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (18)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745847CMV-Luciferase Counterscreen for Inhibitors of ATXN expression
AID1745850Viability Counterscreen for Confirmatory qHTS for Inhibitors of ATXN expression
AID1745846Firefly Luciferase Counterscreen 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
AID1745848Confirmatory qHTS for Inhibitors of ATXN expression
AID1745849Viability 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]

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]

Market Indicators

Research Demand Index: 12.56

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.

MetricThis Compound (vs All)
Research Demand Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

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]