1-(1,1-dioxo-1,2-benzothiazol-3-yl)-N-(2-methylphenyl)-4-piperidinecarboxamide, also known as **S104**, is a **potent and selective inhibitor of the enzyme glycogen synthase kinase 3 beta (GSK-3β)**. Here's why it's important for research:
**GSK-3β: A Key Player in Many Biological Processes**
GSK-3β is a serine/threonine kinase involved in various cellular processes, including:
* **Cell growth and proliferation**
* **Apoptosis (programmed cell death)**
* **Inflammation**
* **Insulin signaling**
* **Neurotransmission**
**GSK-3β and Disease:**
* **Altered GSK-3β activity has been implicated in several diseases, including:**
* **Alzheimer's disease:** GSK-3β plays a role in tau protein phosphorylation, which is a hallmark of Alzheimer's.
* **Diabetes:** Dysregulation of GSK-3β is associated with insulin resistance.
* **Cancer:** GSK-3β can promote both tumor growth and apoptosis, depending on the context.
* **Mental health disorders:** GSK-3β has been linked to bipolar disorder, depression, and schizophrenia.
* **Therefore, GSK-3β is a promising therapeutic target for a variety of diseases.**
**S104: A Powerful Tool for Research**
S104, as a selective inhibitor of GSK-3β, serves as a valuable tool for researchers studying the role of GSK-3β in various diseases:
* **Understanding GSK-3β's function:** S104 helps scientists understand the complex roles of GSK-3β in different cell types and tissues.
* **Drug discovery:** It can be used to screen for and develop new drugs that target GSK-3β for therapeutic purposes.
* **Disease modeling:** S104 can be used in animal models to study the effects of GSK-3β inhibition on disease progression and to test potential treatments.
**In summary:** S104 is an important research tool because it provides a means to manipulate GSK-3β activity and gain insights into its role in disease. This knowledge could lead to the development of new therapies for a range of conditions.
ID Source | ID |
---|---|
PubMed CID | 2570923 |
CHEMBL ID | 1302814 |
CHEBI ID | 119979 |
Synonym |
---|
1-(1,1-dioxo-1,2-benzothiazol-3-yl)-n-(2-methylphenyl)piperidine-4-carboxamide |
MLS000773872 |
smr000364624 |
CHEBI:119979 |
HMS2717A09 |
CHEMBL1302814 |
Q27207764 |
1-(1,1-dioxo-1,2-benzothiazol-3-yl)-n-(2-methylphenyl)-4-piperidinecarboxamide |
AKOS034161016 |
Class | Description |
---|---|
benzothiazoles | |
[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) |
---|---|---|---|---|---|---|---|
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 5.0119 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 0.1778 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
[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] |