1-(4-chlorophenyl)-3-[2-(2-furanylmethyl)cyclohexyl]urea, often referred to as **compound 1**, is a chemical compound that has shown potential as a **potent and selective inhibitor of histone deacetylase 6 (HDAC6)**.
**Why is HDAC6 inhibition important for research?**
HDAC6 is an enzyme that plays a crucial role in various cellular processes, including:
* **Protein degradation:** HDAC6 is involved in the removal of ubiquitinated proteins from the cytoplasm, preventing their degradation by the proteasome.
* **Microtubule dynamics:** HDAC6 regulates microtubule stability and dynamics, influencing cell migration and cell division.
* **Inflammation and immune responses:** HDAC6 is implicated in the regulation of inflammatory responses and immune cell function.
**Importance of HDAC6 inhibitors in research:**
Inhibition of HDAC6 has been shown to have potential therapeutic benefits in a variety of diseases, including:
* **Cancer:** HDAC6 inhibitors can induce apoptosis (programmed cell death) in cancer cells and enhance the efficacy of chemotherapy.
* **Neurodegenerative diseases:** HDAC6 inhibition may protect neurons from damage in conditions like Alzheimer's disease and Parkinson's disease.
* **Inflammation and autoimmune diseases:** HDAC6 inhibitors can suppress inflammation and modulate immune responses.
**Specifically, compound 1:**
* Shows **high selectivity** for HDAC6 over other HDAC isoforms.
* Exhibits **potent inhibitory activity** against HDAC6.
* Has been shown to have **promising preclinical efficacy** in various disease models.
**Ongoing research:**
Compound 1 is currently being investigated in preclinical studies to evaluate its therapeutic potential in different disease settings. The research aims to:
* Further explore its mechanism of action.
* Determine its pharmacokinetic properties.
* Evaluate its safety and efficacy in animal models.
**Overall, 1-(4-chlorophenyl)-3-[2-(2-furanylmethyl)cyclohexyl]urea (compound 1) is a promising HDAC6 inhibitor that holds potential for the development of new therapeutic strategies for various diseases.** However, more research is needed to fully understand its potential and limitations.
ID Source | ID |
---|---|
PubMed CID | 3829272 |
CHEMBL ID | 1417524 |
CHEBI ID | 122035 |
Synonym |
---|
OPREA1_262488 |
1-(4-chlorophenyl)-3-[2-(furan-2-ylmethyl)cyclohexyl]urea |
1-(4-chloro-phenyl)-3-(2-furan-2-ylmethyl-cyclohexyl)-urea |
MLS000555963 , |
smr000147480 |
CHEBI:122035 |
HMS2341P15 |
1-(4-chlorophenyl)-3-[2-(2-furfuryl)cyclohexyl]urea |
cid_3829272 |
bdbm76170 |
1-(4-chlorophenyl)-3-[2-(2-furanylmethyl)cyclohexyl]urea |
CHEMBL1417524 |
Q27210661 |
Class | Description |
---|---|
ureas | |
[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 | 6.3096 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 10.0000 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
TDP1 protein | Homo sapiens (human) | Potency | 23.7246 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
PINK1 | Homo sapiens (human) | Potency | 50.1187 | 2.8184 | 18.8959 | 44.6684 | AID624263 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 12.5893 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
67.9K protein | Vaccinia virus | Potency | 25.2855 | 0.0001 | 8.4406 | 100.0000 | AID720579; AID720580 |
Parkin | Homo sapiens (human) | Potency | 50.1187 | 0.8199 | 14.8306 | 44.6684 | AID624263 |
IDH1 | Homo sapiens (human) | Potency | 29.0929 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
lysosomal alpha-glucosidase preproprotein | Homo sapiens (human) | Potency | 11.2202 | 0.0366 | 19.6376 | 50.1187 | AID1466; AID2242 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 50.1187 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 29.0929 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
huntingtin isoform 2 | Homo sapiens (human) | Potency | 35.4813 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 35.4813 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 35.4813 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
geminin | Homo sapiens (human) | Potency | 20.5962 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
Glycoprotein hormones alpha chain | Homo sapiens (human) | Potency | 28.1838 | 4.4668 | 8.3448 | 10.0000 | AID624291 |
Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 11.2202 | 3.5481 | 18.0395 | 35.4813 | AID1466 |
Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 11.2202 | 3.5481 | 18.0395 | 35.4813 | AID1466 |
Alpha-synuclein | Homo sapiens (human) | Potency | 35.4813 | 0.5623 | 9.3985 | 25.1189 | AID652106 |
[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) |
---|---|---|---|---|---|---|---|
calpain II, partial | Sus scrofa (pig) | IC50 (µMol) | 2.6877 | 1.7742 | 4.9338 | 7.7087 | AID1420 |
alkaline phosphatase, intestinal | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.5650 | 12.9050 | 66.3000 | AID488876 |
alkaline phosphatase, tissue-nonspecific isozyme isoform 1 preproprotein | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.1250 | 16.2603 | 74.8000 | AID488906 |
intestinal alkaline phosphatase precursor | Mus musculus (house mouse) | IC50 (µMol) | 12.2000 | 0.2590 | 11.8708 | 60.3000 | AID488785 |
alkaline phosphatase, germ cell type preproprotein | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.1100 | 11.3862 | 67.2000 | AID488879 |
[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) |
---|---|---|---|---|---|---|---|
G protein-activated inward rectifier potassium channel 2 | Homo sapiens (human) | POTENCY_uM | 4.1435 | 2.2518 | 9.6973 | 30.0000 | AID623909 |
G protein-activated inward rectifier potassium channel 1 | Homo sapiens (human) | POTENCY_uM | 4.1435 | 2.2518 | 9.6973 | 30.0000 | AID623909 |
[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. |
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 | |||
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
[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] |