1-[[4-[(3,4-dichlorophenyl)thio]-3-pyridinyl]sulfonyl]-3-propylurea, also known as **L-735,524**, is a potent and selective **inhibitor of the enzyme carbonic anhydrase IX (CA IX)**.
**Carbonic anhydrase IX (CA IX)** is an enzyme that plays a crucial role in the growth and survival of tumor cells. It is overexpressed in various types of cancers, particularly those that are hypoxic (low oxygen levels). CA IX helps tumor cells adapt to these harsh conditions by regulating the pH of the tumor microenvironment.
**Why is L-735,524 important for research?**
* **Anti-cancer drug development:** L-735,524 has shown promising anti-cancer activity in preclinical studies. By inhibiting CA IX, it can slow down tumor growth and potentially improve the efficacy of other cancer therapies.
* **Understanding the role of CA IX in cancer:** L-735,524 acts as a valuable tool to investigate the role of CA IX in cancer progression and metastasis.
* **Development of new CA IX inhibitors:** Understanding the mechanism of action of L-735,524 can guide the development of more potent and selective CA IX inhibitors for future therapeutic applications.
**Key features of L-735,524:**
* **High potency:** It exhibits strong inhibition of CA IX with a Ki value in the nanomolar range.
* **Selectivity:** It is highly selective for CA IX over other isoforms of carbonic anhydrase.
* **Good pharmacokinetic properties:** It has favorable bioavailability and pharmacokinetic profile, making it suitable for in vivo studies.
**However, it is important to note that L-735,524 is not currently used clinically. Further research is needed to assess its safety and efficacy in human patients.**
ID Source | ID |
---|---|
PubMed CID | 1825804 |
CHEMBL ID | 1472183 |
CHEBI ID | 112888 |
Synonym |
---|
MLS000539686 |
smr000162110 |
AJ-333/25006003 |
4-[(3,4-dichlorophenyl)sulfanyl]-3-({[(propylamino)carbonyl]amino}sulfonyl)pyridine |
CHEBI:112888 |
1-[4-(3,4-dichlorophenyl)sulfanylpyridin-3-yl]sulfonyl-3-propylurea |
HMS2303H13 |
CHEMBL1472183 |
1-[[4-[(3,4-dichlorophenyl)thio]-3-pyridinyl]sulfonyl]-3-propylurea |
Q27193351 |
Class | Description |
---|---|
aryl sulfide | Any organic sulfide in which the sulfur is attached to at least one aromatic group. |
[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 | 28.1838 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
ClpP | Bacillus subtilis | Potency | 22.3872 | 1.9953 | 22.6730 | 39.8107 | AID651965 |
phosphopantetheinyl transferase | Bacillus subtilis | Potency | 63.0957 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 56.2341 | 0.1000 | 22.9075 | 100.0000 | AID485364 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 3.1623 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 0.7079 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
pyruvate kinase | Leishmania mexicana mexicana | Potency | 25.1189 | 0.3981 | 13.7447 | 31.6228 | AID1721; AID1722 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 22.3872 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
huntingtin isoform 2 | Homo sapiens (human) | Potency | 35.4813 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 11.9173 | 0.1683 | 16.4040 | 67.0158 | AID720504 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 100.0000 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
lethal(3)malignant brain tumor-like protein 1 isoform I | Homo sapiens (human) | Potency | 0.0891 | 0.0752 | 15.2253 | 39.8107 | AID485360 |
Endothelin receptor type B | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 0.5623 | 15.1609 | 31.6228 | AID1721 |
Endothelin-1 receptor | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 0.5623 | 15.1609 | 31.6228 | AID1721 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1745845 | 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. |
[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] |