Page last updated: 2024-12-09

1-methyl-5-[(4-methylphenyl)thio]-3-phenyl-4-pyrazolecarbonitrile

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

1-methyl-5-[(4-methylphenyl)thio]-3-phenyl-4-pyrazolecarbonitrile, also known as **MC136**, is a potent and selective **inhibitor of the enzyme HDAC6**.

**HDAC6** (Histone Deacetylase 6) is a member of the histone deacetylase family of enzymes. It plays a crucial role in regulating various cellular processes, including:

* **Protein degradation**: HDAC6 is involved in the ubiquitin-proteasome pathway, which is responsible for degrading damaged or unnecessary proteins.
* **Microtubule stability**: HDAC6 can deacetylate tubulin, a protein that forms microtubules, influencing their stability and dynamics.
* **Inflammation**: HDAC6 has been implicated in inflammatory responses.

**Why is MC136 important for research?**

MC136's selective inhibition of HDAC6 makes it a valuable tool for researchers studying the role of this enzyme in different biological processes. Specifically, it is used to:

* **Investigate the role of HDAC6 in various diseases**: MC136 has been used to study the involvement of HDAC6 in diseases such as cancer, neurodegenerative disorders, and inflammatory diseases.
* **Develop novel therapeutic strategies**: Targeting HDAC6 with inhibitors like MC136 has shown promise as a therapeutic strategy for these diseases.
* **Uncover the mechanisms of action of HDAC6**: By studying the effects of MC136 on cells and tissues, researchers can gain insights into the specific mechanisms by which HDAC6 exerts its effects.

**Current research on MC136 focuses on:**

* Its potential therapeutic applications in cancer treatment, particularly in multiple myeloma and leukemia.
* Its ability to protect against neuronal damage in neurodegenerative disorders like Alzheimer's and Parkinson's disease.
* Its role in modulating inflammatory responses and potentially treating autoimmune diseases.

**Overall, MC136 is a valuable research tool that has contributed significantly to our understanding of HDAC6 and its role in various physiological and pathological processes. It holds promise for the development of new therapies for a wide range of diseases.**

Cross-References

ID SourceID
PubMed CID1475518
CHEMBL ID1528316
CHEBI ID120650

Synonyms (12)

Synonym
MLS000326292 ,
1-methyl-5-[(4-methylphenyl)sulfanyl]-3-phenyl-1h-pyrazole-4-carbonitrile
smr000178895
CHEBI:120650
AKOS005075393
1-methyl-5-(4-methylphenyl)sulfanyl-3-phenylpyrazole-4-carbonitrile
HMS2495I07
10L-581S
321998-34-9
CHEMBL1528316
Q27208782
1-methyl-5-[(4-methylphenyl)thio]-3-phenyl-4-pyrazolecarbonitrile
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
ring assemblyTwo or more cyclic systems (single rings or fused systems) which are directly joined to each other by double or single bonds are named ring assemblies when the number of such direct ring junctions is one less than the number of cyclic systems involved.
pyrazoles
[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 (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency31.62280.004023.8416100.0000AID485290
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency56.23410.631035.7641100.0000AID504339
Chain A, Ferritin light chainEquus caballus (horse)Potency50.11875.623417.292931.6228AID485281
TDP1 proteinHomo sapiens (human)Potency9.47650.000811.382244.6684AID686978; AID686979
Smad3Homo sapiens (human)Potency3.98110.00527.809829.0929AID588855
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency29.93490.707912.194339.8107AID720542
PINK1Homo sapiens (human)Potency10.00002.818418.895944.6684AID624263
ParkinHomo sapiens (human)Potency10.00000.819914.830644.6684AID624263
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency50.11870.707936.904389.1251AID504333
IDH1Homo sapiens (human)Potency35.48130.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency12.58930.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency79.43280.006026.168889.1251AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency5.80480.00419.984825.9290AID504444
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency25.11890.075215.225339.8107AID485360
gemininHomo sapiens (human)Potency12.43470.004611.374133.4983AID624296; AID624297
lamin isoform A-delta10Homo sapiens (human)Potency31.62280.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
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.
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.
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.
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]

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]