1-ethyl-3-[(1-oxo-2-phenylethyl)amino]thiourea, also known as **EPTU**, is a synthetic compound that acts as a potent and selective inhibitor of **ornithine decarboxylase (ODC)**.
Here's why it's important for research:
**ODC and its role in cell growth and proliferation:**
* ODC is a key enzyme in the biosynthesis of polyamines, which are essential for cell growth, proliferation, and differentiation.
* ODC catalyzes the decarboxylation of ornithine to putrescine, the first step in the polyamine biosynthetic pathway.
* Elevated ODC activity is associated with various cancers and other proliferative diseases.
**EPTU as a research tool:**
* **Inhibiting ODC activity:** EPTU acts as a mechanism-based inhibitor of ODC, meaning it forms a stable covalent complex with the enzyme, effectively shutting down its activity. This makes EPTU a valuable tool for studying the role of ODC in various biological processes.
* **Investigating polyamine metabolism:** EPTU allows researchers to manipulate polyamine levels in cells and organisms, enabling them to study the effects of these changes on cell growth, proliferation, and other biological functions.
* **Developing new anti-cancer drugs:** The potent ODC inhibitory activity of EPTU has led to its investigation as a potential anti-cancer agent. EPTU itself has not progressed to clinical use, but its structure has served as inspiration for the development of other ODC inhibitors.
**EPTU is not a drug currently used in human therapy.** However, it remains a crucial research tool for understanding the role of ODC in cell growth, proliferation, and disease. Its use has contributed to the development of new insights into polyamine metabolism and its potential therapeutic targets.
ID Source | ID |
---|---|
PubMed CID | 1817063 |
CHEMBL ID | 1599810 |
CHEBI ID | 109665 |
Synonym |
---|
1-ethyl-3-[(2-phenylacetyl)amino]thiourea |
MLS000543824 , |
smr000161283 |
n-ethyl-2-(phenylacetyl)hydrazinecarbothioamide |
AO-476/40219263 |
STK422167 |
CHEBI:109665 |
AKOS002222165 |
HMS2181B09 |
CHEMBL1599810 |
31409-13-9 |
Q27188832 |
1-ethyl-3-[(1-oxo-2-phenylethyl)amino]thiourea |
n-ethyl-2-(phenylacetyl)hydrazine-1-carbothioamide |
Class | Description |
---|---|
acetamides | Compounds with the general formula RNHC(=O)CH3. |
[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) |
---|---|---|---|---|---|---|---|
TDP1 protein | Homo sapiens (human) | Potency | 29.0929 | 0.0008 | 11.3822 | 44.6684 | AID686978 |
Smad3 | Homo sapiens (human) | Potency | 1.4125 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 79.4328 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 35.4813 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
[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) |
---|---|---|---|---|---|---|---|
glycogen synthase kinase-3 alpha | Homo sapiens (human) | AC50 | 300.0000 | 0.0135 | 29.7434 | 171.7000 | AID463203 |
[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. |
AID1745845 | 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. |
AID651635 | Viability Counterscreen for 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. |
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] |