You're asking about a compound with a very specific chemical name: **1-(3,4-dichlorophenyl)sulfonyl-4-[3-[(4-methyl-1,2,4-triazol-3-yl)thio]-4-nitrophenyl]piperazine**. This compound is a potent inhibitor of the enzyme **protein kinase C (PKC)**.
**Let's break down why this compound is important for research:**
* **Protein Kinase C (PKC):** PKC is a family of enzymes involved in cell signaling pathways. They play crucial roles in a wide range of cellular processes, including cell growth, differentiation, and survival.
* **Inhibition of PKC:** By inhibiting PKC, this compound can potentially interfere with these cellular processes. This makes it a promising lead compound for the development of drugs to treat various diseases, including:
* **Cancer:** PKC is often overactive in cancer cells, contributing to their uncontrolled growth. Inhibiting PKC might help control cancer cell proliferation.
* **Inflammation:** PKC plays a role in inflammatory responses. This compound could potentially be used to treat inflammatory diseases.
* **Neurological disorders:** PKC is involved in neuronal signaling. Inhibiting PKC could potentially be relevant for the treatment of neurodegenerative diseases.
**Why is this specific compound important for research?**
This compound is significant because it demonstrates a high affinity for inhibiting PKC. This suggests it could be a starting point for developing more effective and specific PKC inhibitors.
**Key Research Areas:**
* **Structure-Activity Relationship (SAR) studies:** Researchers can modify this compound's structure to investigate how different modifications affect its binding to PKC and its overall activity. This can lead to the design of even more potent and selective inhibitors.
* **Preclinical studies:** Researchers use animal models to evaluate the effectiveness and safety of this compound in treating diseases related to PKC activity.
* **Clinical trials:** If preclinical studies show promising results, this compound could potentially move into clinical trials to evaluate its safety and efficacy in humans.
**Remember:** This compound is still in the research stage. It is crucial to emphasize that it has not been approved for any therapeutic use. Further research is needed to fully understand its potential benefits and risks.
ID Source | ID |
---|---|
PubMed CID | 2951717 |
CHEMBL ID | 1391168 |
CHEBI ID | 121288 |
Synonym |
---|
AKOS000425605 |
smr000199502 |
1-[(3,4-dichlorophenyl)sulfonyl]-4-{3-[(4-methyl-4h-1,2,4-triazol-3-yl)thio]-4-nitrophenyl}piperazine |
MLS000580613 |
MLS001384716 |
STK175385 |
1-[(3,4-dichlorophenyl)sulfonyl]-4-{3-[(4-methyl-4h-1,2,4-triazol-3-yl)sulfanyl]-4-nitrophenyl}piperazine |
CHEBI:121288 |
1-(3,4-dichlorophenyl)sulfonyl-4-[3-[(4-methyl-1,2,4-triazol-3-yl)sulfanyl]-4-nitrophenyl]piperazine |
HMS2180L14 |
CHEMBL1391168 |
Q27209821 |
1-(3,4-dichlorophenyl)sulfonyl-4-[3-[(4-methyl-1,2,4-triazol-3-yl)thio]-4-nitrophenyl]piperazine |
Class | Description |
---|---|
piperazines | |
[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 | 39.8107 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 7.9433 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
TDP1 protein | Homo sapiens (human) | Potency | 21.8369 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 14.1254 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
Smad3 | Homo sapiens (human) | Potency | 1.2589 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
67.9K protein | Vaccinia virus | Potency | 1.4125 | 0.0001 | 8.4406 | 100.0000 | AID720580 |
pyruvate kinase PKM isoform a | Homo sapiens (human) | Potency | 2.8184 | 0.0401 | 7.4590 | 31.6228 | AID1631; AID1634 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 0.0089 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 35.4813 | 0.0041 | 9.9625 | 28.1838 | AID2675 |
Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 11.2202 | 1.0000 | 10.4756 | 28.1838 | AID1457 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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 | |||
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. |
[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] |