Page last updated: 2024-12-04

1-(5-isoquinolinylsulfonyl)-3-methylpiperazine

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

Description

1-(5-isoquinolinylsulfonyl)-3-methylpiperazine, also known as **Lu AF21934**, is a potent and selective **inhibitor of the enzyme glycogen synthase kinase 3 beta (GSK-3β)**.

Here's why it's important for research:

* **GSK-3β plays a critical role in various cellular processes:** It's involved in regulating cell growth, differentiation, inflammation, and neuronal function. Its dysregulation has been linked to several diseases including Alzheimer's disease, cancer, diabetes, and bipolar disorder.
* **Lu AF21934 is a valuable tool for studying GSK-3β:** Its high potency and selectivity make it a powerful research tool for studying the role of GSK-3β in various disease models. Researchers can use it to:
* **Investigate the role of GSK-3β in specific disease pathways:** By blocking GSK-3β, researchers can observe its effects on disease progression and identify potential therapeutic targets.
* **Develop new drugs targeting GSK-3β:** Lu AF21934 can serve as a lead compound for designing and optimizing new GSK-3β inhibitors with improved pharmacological properties.
* **Potential therapeutic applications:** Lu AF21934 has shown promising results in preclinical studies for treating various diseases, including Alzheimer's disease, cancer, and diabetes. However, further research is needed to evaluate its safety and efficacy in humans.

**In summary, 1-(5-isoquinolinylsulfonyl)-3-methylpiperazine is a potent GSK-3β inhibitor that holds significant promise for research into the role of GSK-3β in various diseases and the development of new therapeutic agents.**

1-(5-isoquinolinylsulfonyl)-3-methylpiperazine: a positional isomer of H-7; inhibits protein kinase and cAMP-dependent protein kinase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1352
CHEMBL ID1555085
SCHEMBL ID1165362
MeSH IDM0215081

Synonyms (29)

Synonym
1-(6-isoquinolylsulfonyl)-3-methylpiperazine
nsc683547
iso-h7
5-(3-methylpiperazin-1-yl)sulfonylisoquinoline
nsc-683547
1-(5-isoquinolinylsulfonyl)-3-methylpiperazine
piperazine, 1-(5-isoquinolinylsulfonyl)-3-methyl-
iso-h-7
1-(5-isoquinolinesulfonyl)-3-methylpiperazine
OPREA1_059623
LOPAC0_000662
NCGC00162215-01
84477-73-6
1-(5-isoquinolinesulfonyl)-3-methylpiperazine, >=98.0% (hplc)
NCGC00015561-03
AKOS009158819
CCG-204748
1-(5-isoquinolinesulfonyl)-2-methylpiperazine.2hcl
cas_140663-38-3
bdbm86727
NCGC00015561-02
SCHEMBL1165362
CHEMBL1555085
1-(5-isoquinolinylsulfonyl)-3-methyl-piperazine
SDCCGSBI-0050641.P002
5-((3-methylpiperazin-1-yl)sulfonyl)isoquinoline
5-(3-methylpiperazine-1-sulfonyl)isoquinoline
DTXSID701004755
Z1262449272

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" There is no dosage and time dependence of PKC inhibitor in regulating eosinophil apoptosis of nasal polyps."( [The influence of protein kinase C inhibitor in eosinophil apoptosis of nasal polyps].
Li, MH; Yang, ZQ; Yin, WZ, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency42.28410.100020.879379.4328AID488772; AID588456
ATAD5 protein, partialHomo sapiens (human)Potency20.58780.004110.890331.5287AID493107
regulator of G-protein signaling 4Homo sapiens (human)Potency0.08440.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency25.11890.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency56.23410.006026.168889.1251AID488953
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (22)

Assay IDTitleYearJournalArticle
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
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.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (39)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's24 (61.54)18.2507
2000's5 (12.82)29.6817
2010's5 (12.82)24.3611
2020's5 (12.82)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.89

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 Index10.89 (24.57)
Research Supply Index3.71 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.89)

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%
Other40 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]