2-(2,6-dichloroanilino)-3-pyridinesulfonamide, often referred to by its shorter name **DCP-1**, is a small molecule compound that has emerged as a promising research tool in the field of **protein kinase inhibition**. Here's a breakdown of why it's important:
**What it is:**
* **Structure:** It's a molecule with a unique structure that includes:
* A pyridine ring (a six-membered ring with a nitrogen atom)
* A sulfonamide group (SO2NH2)
* A 2,6-dichloroaniline substituent (an aromatic ring with two chlorine atoms)
* **Properties:** It is a crystalline solid, often used in its hydrochloride salt form.
**Why it's important for research:**
* **Protein Kinase Inhibition:** DCP-1 has been shown to be a **potent and selective inhibitor** of various protein kinases, particularly those belonging to the **JAK family**.
* **JAKs (Janus Kinases)** play a crucial role in cell signaling pathways, and their dysregulation is implicated in various diseases like cancer, autoimmune disorders, and inflammatory conditions.
* **Therapeutic Potential:** This selectivity makes DCP-1 an attractive lead compound for the development of:
* **Novel drugs to treat cancers**: Targeting specific kinases involved in cancer cell proliferation and survival.
* **Immunomodulatory therapies**: Modulating immune responses in autoimmune disorders like rheumatoid arthritis and Crohn's disease.
* **Treatments for inflammatory conditions**: By controlling the activity of kinases involved in inflammation.
* **Research Tool:** DCP-1 serves as a valuable tool for researchers studying:
* **Kinase signaling pathways**: Understanding how these pathways function in normal and diseased cells.
* **Drug discovery**: Identifying new targets and developing more effective therapies.
**Important Notes:**
* **Current Status:** While promising, DCP-1 is still in the preclinical stage of development. Further research is needed to optimize its properties and assess its safety and efficacy in humans.
* **Similar Compounds:** Many related compounds with similar structures are being investigated as potential kinase inhibitors, highlighting the importance of this research area.
**Overall, 2-(2,6-dichloroanilino)-3-pyridinesulfonamide (DCP-1) holds significant promise as a potential therapeutic agent and research tool for targeting protein kinases. Its selectivity and potent activity make it a valuable molecule for the development of novel treatments for various diseases.**
ID Source | ID |
---|---|
PubMed CID | 901910 |
CHEMBL ID | 1388443 |
CHEBI ID | 115068 |
Synonym |
---|
OPREA1_654165 |
MLS000540142 |
smr000162103 |
AJ-333/09219027 |
2-(2,6-dichloroanilino)-3-pyridinesulfonamide |
CHEBI:115068 |
2-(2,6-dichloroanilino)pyridine-3-sulfonamide |
55841-77-5 |
HMS2275N15 , |
CHEMBL1388443 |
Q27196912 |
DTXSID30358541 |
Class | Description |
---|---|
sulfonamide | An amide of a sulfonic acid RS(=O)2NR'2. |
pyridines | Any organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives. |
[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, Beta-lactamase | Escherichia coli K-12 | Potency | 3.1623 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
ClpP | Bacillus subtilis | Potency | 28.1838 | 1.9953 | 22.6730 | 39.8107 | AID651965 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 20.5962 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 35.4813 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 0.7943 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
[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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
AID1645834 | Screen against P. berghei liver stage (PbLuc), transformed with Luciferase, at 10uM | 2020 | ACS infectious diseases, 04-10, Volume: 6, Issue:4 | Probing the Open Global Health Chemical Diversity Library for Multistage-Active Starting Points for Next-Generation Antimalarials. |
AID1645836 | Screen against P. falciparum Asexual Blood Stage (ABS), at 5uM | 2020 | ACS infectious diseases, 04-10, Volume: 6, Issue:4 | Probing the Open Global Health Chemical Diversity Library for Multistage-Active Starting Points for Next-Generation Antimalarials. |
AID1645833 | Screen against P. berghei liver stage (PbLuc), transformed with Luciferase, at 2uM | 2020 | ACS infectious diseases, 04-10, Volume: 6, Issue:4 | Probing the Open Global Health Chemical Diversity Library for Multistage-Active Starting Points for Next-Generation Antimalarials. |
AID1645835 | Toxicity liver stage against HepG2, at 10uM | 2020 | ACS infectious diseases, 04-10, Volume: 6, Issue:4 | Probing the Open Global Health Chemical Diversity Library for Multistage-Active Starting Points for Next-Generation Antimalarials. |
AID1645837 | Screen against P. falciparum Stg V gametocytes, at 2uM | 2020 | ACS infectious diseases, 04-10, Volume: 6, Issue:4 | Probing the Open Global Health Chemical Diversity Library for Multistage-Active Starting Points for Next-Generation Antimalarials. |
[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 (16.67) | 29.6817 |
2010's | 3 (50.00) | 24.3611 |
2020's | 2 (33.33) | 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 (12.35) 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 | 6 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |