Page last updated: 2024-12-09

1-piperidinyl-(5-thiophen-2-yl-3-isoxazolyl)methanone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

1-Piperidinyl-(5-thiophen-2-yl-3-isoxazolyl)methanone, also known as **JNJ-54175859**, is a potent and selective **inhibitor of the enzyme histone deacetylase 6 (HDAC6)**.

Here's why it's important for research:

* **HDAC6 and its role in various diseases:** HDAC6 is a key enzyme involved in regulating the acetylation of proteins, particularly tubulin, which plays a vital role in cell structure and function. HDAC6 inhibition has been shown to have potential therapeutic benefits in a variety of diseases, including:
* **Cancer:** By inhibiting HDAC6, JNJ-54175859 can promote the accumulation of acetylated tubulin, leading to microtubule stabilization and cell death in cancer cells.
* **Neurodegenerative diseases:** HDAC6 inhibition can potentially protect against neurodegeneration by promoting neuronal survival and reducing inflammation.
* **Inflammation:** HDAC6 inhibition can modulate inflammatory responses and potentially benefit inflammatory conditions.

* **JNJ-54175859 as a potential drug candidate:** JNJ-54175859 exhibits high potency and selectivity for HDAC6, making it a promising drug candidate for the treatment of these diseases. Its preclinical studies have shown promising results, demonstrating its efficacy in reducing tumor growth and improving neurological function in animal models.

* **Research tool for understanding HDAC6 function:** JNJ-54175859 serves as a valuable tool for researchers to study the role of HDAC6 in various biological processes. It allows scientists to investigate the effects of HDAC6 inhibition on cell function, signaling pathways, and disease progression.

**However, it's crucial to note that JNJ-54175859 is currently in preclinical development, and it's still under investigation. More research is needed to fully understand its safety and efficacy in humans before it can be used as a therapeutic agent.**

Cross-References

ID SourceID
PubMed CID2745204
CHEMBL ID1536135
CHEBI ID109848
SCHEMBL ID2526391

Synonyms (19)

Synonym
AKOS003403725
piperidin-1-yl-(5-thiophen-2-yl-1,2-oxazol-3-yl)methanone
smr000023475
MLS000087252 ,
1-[(5-thien-2-ylisoxazol-3-yl)carbonyl]piperidine
OPREA1_318418
IDI1_018590
EU-0023743
SR-01000606963-2
MAYBRIDGE3_007203
CHEBI:109848
HMS1451H09
HMS2467O20
CCG-49246
SCHEMBL2526391
CHEMBL1536135
1-piperidinyl-(5-thiophen-2-yl-3-isoxazolyl)methanone
Q27189161
1-[5-(thiophen-2-yl)-1,2-oxazole-3-carbonyl]piperidine
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
N-acylpiperidine
[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 Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency19.89150.007215.758889.3584AID411; AID588342
thioredoxin reductaseRattus norvegicus (Norway rat)Potency31.62280.100020.879379.4328AID588453
BRCA1Homo sapiens (human)Potency1.25890.89137.722525.1189AID624202
ATAD5 protein, partialHomo sapiens (human)Potency11.45360.004110.890331.5287AID504466; AID504467
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
P53Homo sapiens (human)Potency31.62280.07319.685831.6228AID504706
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency1.00000.01262.451825.0177AID485313
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.58930.316212.443531.6228AID902
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency1.77830.001815.663839.8107AID894
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency5.17350.00419.984825.9290AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency50.11873.548119.542744.6684AID743266
ras-related protein Rab-9AHomo sapiens (human)Potency0.56230.00022.621531.4954AID485297
survival motor neuron protein isoform dHomo sapiens (human)Potency14.12540.125912.234435.4813AID1458
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. 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.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. 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.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. 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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, 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]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's3 (60.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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.

MetricThis Compound (vs All)
Research Demand Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]