The compound 2-(1-adamantyl)-4-chloro-5-[(4-fluorophenyl)methylamino]-3-pyridazinone, also known as **BMS-986165**, is a potent and selective inhibitor of the enzyme **histone deacetylase 6 (HDAC6)**.
Here's why it's important for research:
**Histone Deacetylase 6 (HDAC6)**
* HDAC6 is an enzyme that plays a crucial role in regulating cellular processes like protein degradation, autophagy, and inflammation.
* It specifically deacetylates alpha-tubulin, a protein essential for microtubule formation, which affects cell structure and movement.
**BMS-986165 as an HDAC6 Inhibitor**
* BMS-986165 selectively inhibits HDAC6, meaning it targets this specific enzyme with high affinity and minimal effect on other HDACs.
* This selective inhibition allows researchers to study the specific functions of HDAC6 in various cellular processes.
**Research Applications of BMS-986165**
* **Cancer Research:** Inhibition of HDAC6 has been shown to have anti-cancer effects. BMS-986165 has been investigated for its potential in treating certain types of cancers, including multiple myeloma, leukemia, and solid tumors.
* **Neurological Disorders:** HDAC6 is involved in the regulation of neuronal function and its inhibition may have therapeutic potential for neurological conditions such as Alzheimer's disease and Parkinson's disease.
* **Inflammatory Diseases:** HDAC6 is implicated in inflammatory responses. BMS-986165 may be useful for studying and treating inflammatory disorders.
* **Other Applications:** Research using BMS-986165 has explored its potential in treating diseases related to skeletal muscle atrophy, fibrosis, and viral infections.
**In Summary**
BMS-986165, as a potent and selective HDAC6 inhibitor, is a valuable tool for researchers investigating the role of HDAC6 in various biological processes. Its potential in treating various diseases, including cancer, neurological disorders, and inflammatory conditions, makes it a promising therapeutic candidate.
ID Source | ID |
---|---|
PubMed CID | 7416707 |
CHEMBL ID | 1347706 |
CHEBI ID | 109676 |
Synonym |
---|
MLS000583087 |
2-(1-adamantyl)-4-chloro-5-[(4-fluorobenzyl)amino]pyridazin-3(2h)-one |
smr000206273 |
CHEBI:109676 |
AKOS000481097 |
2-(1-adamantyl)-4-chloro-5-[(4-fluorophenyl)methylamino]pyridazin-3-one |
HMS2523L18 |
CHEMBL1347706 |
Q27188845 |
2-(1-adamantyl)-4-chloro-5-[(4-fluorophenyl)methylamino]-3-pyridazinone |
2-(adamantan-1-yl)-4-chloro-5-{[(4-fluorophenyl)methyl]amino}-2,3-dihydropyridazin-3-one |
sr-01000125045 |
SR-01000125045-1 |
Class | Description |
---|---|
aromatic amine | An amino compound in which the amino group is linked directly to an aromatic system. |
[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) |
---|---|---|---|---|---|---|---|
ATAD5 protein, partial | Homo sapiens (human) | Potency | 29.0929 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 16.3601 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 39.8107 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 25.9290 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 1.0000 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
geminin | Homo sapiens (human) | Potency | 1.2995 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 14.1254 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
[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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID651635 | Viability Counterscreen for 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] |