1-Cyclohexyl-3-[4-[(5-methyl-3-isoxazolyl)sulfamoyl]phenyl]urea, often referred to by its shorter name **SU5416**, is a small-molecule drug that acts as a potent and selective **inhibitor of vascular endothelial growth factor receptor (VEGFR) tyrosine kinases**.
Here's why it's important for research:
**1. Anti-angiogenic Potential:**
VEGFRs play a crucial role in angiogenesis, the process of new blood vessel formation. SU5416 blocks the activation of these receptors, inhibiting angiogenesis. This makes it a potential therapeutic agent for:
* **Cancer:** Preventing tumor growth by inhibiting the formation of new blood vessels that supply oxygen and nutrients to the tumor.
* **Ocular Diseases:** Treating diseases like diabetic retinopathy and macular degeneration, where abnormal angiogenesis leads to vision loss.
**2. Research Tool:**
SU5416 has been extensively used as a research tool to study the role of angiogenesis in various biological processes. It provides researchers with a valuable tool to:
* **Investigate the mechanisms of angiogenesis.**
* **Screen for new anti-angiogenic drugs.**
* **Develop models for studying angiogenesis in various diseases.**
**3. Historical Significance:**
SU5416 was one of the first potent and selective VEGFR inhibitors developed. Its discovery paved the way for the development of a new class of anti-angiogenic drugs, significantly impacting the field of cancer treatment and other related fields.
**4. Current Status:**
Although SU5416 itself is not currently approved for clinical use, its development has led to the approval of other VEGFR inhibitors like **sunitinib** and **pazopanib** for treating various cancers.
**Important Considerations:**
* **Toxicity:** Like many targeted therapies, SU5416 can have side effects, including hypertension and bleeding.
* **Resistance:** Tumors can develop resistance to VEGFR inhibitors, highlighting the need for ongoing research to develop new and effective treatments.
Overall, SU5416 is a highly significant compound in the field of anti-angiogenic research. Its discovery and subsequent research have led to important advances in our understanding of angiogenesis and the development of new therapies for a wide range of diseases.
ID Source | ID |
---|---|
PubMed CID | 1093288 |
CHEMBL ID | 1585402 |
CHEBI ID | 105665 |
Synonym |
---|
AN-329/42294977 |
CBKINASE1_020089 |
CBKINASE1_007689 |
MLS000050366 , |
4-{[(cyclohexylamino)carbonyl]amino}-n-(5-methyl-3-isoxazolyl)benzenesulfonamide |
smr000077643 |
CHEBI:105665 |
AKOS000496723 |
STL069050 |
4-[(cyclohexylcarbamoyl)amino]-n-(5-methyl-1,2-oxazol-3-yl)benzenesulfonamide |
BRD-K48093976-001-01-2 |
1-cyclohexyl-3-[4-[(5-methyl-1,2-oxazol-3-yl)sulfamoyl]phenyl]urea |
AB00357583-05 |
MLS002546870 |
HMS2436D03 |
CHEMBL1585402 |
Q27183422 |
1-cyclohexyl-3-[4-[(5-methyl-3-isoxazolyl)sulfamoyl]phenyl]urea |
708994-99-4 |
4-(3-cyclohexylureido)-n-(5-methylisoxazol-3-yl)benzenesulfonamide |
Class | Description |
---|---|
sulfonamide | An amide of a sulfonic acid RS(=O)2NR'2. |
[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) |
---|---|---|---|---|---|---|---|
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 0.8913 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
[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 |
---|---|---|---|---|
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1244251 | Antimicrobial activity against Yersinia pseudotuberculosis after 20 hrs | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Design, synthesis and evaluation of novel polypharmacological antichlamydial agents. |
AID1244245 | Cytotoxicity against human HeLa cells assessed as cell viability at 50 uM after 48 hrs by resazurin based fluorescence assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Design, synthesis and evaluation of novel polypharmacological antichlamydial agents. |
AID1244244 | Antichlamydial activity against Chlamydia pneumoniae T45 infected in human HeLa cells assessed as growth inhibition at 50 uM after 24 to 48 hrs by microscopic analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Design, synthesis and evaluation of novel polypharmacological antichlamydial agents. |
AID1244243 | Antichlamydial activity against Chlamydia trachomatis L2 serovar VR-902B infected in human HeLa cells assessed as growth inhibition at 50 uM after 24 to 48 hrs by microscopic analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Design, synthesis and evaluation of novel polypharmacological antichlamydial agents. |
[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 | 4 (66.67) | 24.3611 |
2020's | 1 (16.67) | 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] |