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.**
ID Source | ID |
---|---|
PubMed CID | 1475518 |
CHEMBL ID | 1528316 |
CHEBI ID | 120650 |
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 |
Class | Description |
---|---|
ring assembly | Two 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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 31.6228 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 56.2341 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 50.1187 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
TDP1 protein | Homo sapiens (human) | Potency | 9.4765 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Smad3 | Homo sapiens (human) | Potency | 3.9811 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 29.9349 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
PINK1 | Homo sapiens (human) | Potency | 10.0000 | 2.8184 | 18.8959 | 44.6684 | AID624263 |
Parkin | Homo sapiens (human) | Potency | 10.0000 | 0.8199 | 14.8306 | 44.6684 | AID624263 |
bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 50.1187 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
IDH1 | Homo sapiens (human) | Potency | 35.4813 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 12.5893 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
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 | 5.8048 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
lethal(3)malignant brain tumor-like protein 1 isoform I | Homo sapiens (human) | Potency | 25.1189 | 0.0752 | 15.2253 | 39.8107 | AID485360 |
geminin | Homo sapiens (human) | Potency | 12.4347 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 31.6228 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID651635 | Viability Counterscreen for Primary qHTS 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. |
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. |
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. |
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. |
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 | |||
[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] |