1-ethyl-2-[(4-methylphenoxy)methyl]benzimidazole, also known as **KT5720**, is a synthetic compound that acts as a **potent and selective inhibitor of the enzyme protein kinase C (PKC)**.
**Protein kinase C (PKC)** is a family of enzymes that play crucial roles in various cellular processes, including:
* **Cell growth and proliferation:** PKC is involved in regulating cell cycle progression and promoting cell division.
* **Signal transduction:** PKC acts as a signaling molecule, relaying information from the cell surface to the nucleus.
* **Cellular differentiation:** PKC regulates the differentiation of various cell types.
* **Apoptosis:** PKC can contribute to both the induction and inhibition of programmed cell death.
* **Immune response:** PKC is involved in the activation of immune cells, such as T cells and macrophages.
**Importance in Research:**
KT5720 is a valuable research tool for several reasons:
* **Selectivity:** KT5720 specifically inhibits PKC, making it a useful probe to investigate the roles of PKC in different biological processes.
* **Potency:** KT5720 is a potent inhibitor of PKC, allowing for the use of lower concentrations in experiments.
* **Versatility:** KT5720 can be used in a variety of research settings, including in vitro cell culture studies, in vivo animal models, and clinical trials.
**Research applications of KT5720:**
* **Cancer research:** KT5720 has been studied for its potential anti-cancer effects, as PKC is often overactive in cancer cells.
* **Neurological disorders:** PKC dysregulation is implicated in several neurological disorders, including Alzheimer's disease and Parkinson's disease. KT5720 has been investigated for its potential therapeutic benefits in these conditions.
* **Cardiovascular disease:** PKC plays a role in the development of cardiovascular disease, and KT5720 has been studied for its potential to prevent or treat heart disease.
* **Inflammatory diseases:** PKC is involved in the inflammatory response, and KT5720 has been explored as a potential anti-inflammatory agent.
**Overall, KT5720 is a valuable research tool that has contributed significantly to our understanding of the roles of PKC in various biological processes. Its selective and potent inhibitory activity makes it a useful probe for studying PKC function and developing new therapies for a range of diseases.**
ID Source | ID |
---|---|
PubMed CID | 800809 |
CHEMBL ID | 1461800 |
CHEBI ID | 116375 |
Synonym |
---|
(1-ethyl-1h-benzimidazol-2-yl)methyl 4-methylphenyl ether |
AE-848/41029272 |
smr000287848 |
MLS000708381 |
CHEBI:116375 |
1-ethyl-2-[(4-methylphenoxy)methyl]-1h-benzimidazole |
STK843976 |
1-ethyl-2-[(4-methylphenoxy)methyl]benzimidazole |
AKOS000562954 |
HMS2732F17 |
1-ethyl-2-((p-tolyloxy)methyl)-1h-benzo[d]imidazole |
F1115-0057 |
433328-82-6 |
CHEMBL1461800 |
Q27199258 |
1-ethyl-2-[(4-methylphenoxy)methyl]-1h-1,3-benzodiazole |
Z57171557 |
1-ethyl-2-(4-methylphenoxymethyl)-1h-1,3-benzodiazole |
DTXSID501322345 |
EN300-205524 |
Class | Description |
---|---|
benzimidazoles | An organic heterocyclic compound containing a benzene ring fused to an imidazole ring. |
[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, Ferritin light chain | Equus caballus (horse) | Potency | 25.1189 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 8.4921 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
ClpP | Bacillus subtilis | Potency | 35.4813 | 1.9953 | 22.6730 | 39.8107 | AID651965 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 14.5750 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 23.7246 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 28.1838 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 8.9125 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 70.7946 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 2.8184 | 0.0126 | 2.4518 | 25.0177 | AID485313 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 2.8184 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 22.1969 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 11.2202 | 1.7783 | 16.2081 | 35.4813 | AID652104 |
Rap guanine nucleotide exchange factor 4 | Homo sapiens (human) | Potency | 89.1251 | 3.9811 | 46.7448 | 112.2020 | AID720708 |
[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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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] |