Page last updated: 2024-12-11

gi 129471

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Description

GI 129471: metalloprotease inhibitor that blocks TNF-alpha secretion; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5748217
CHEMBL ID114427
SCHEMBL ID6838720
MeSH IDM0234631

Synonyms (15)

Synonym
butanediamide, n4-hydroxy-n1-(2-(methylamino)-2-oxo-1-(phenylmethyl)ethyl)-2-(2-methylpropyl)-3-((phenylthio)methyl)-, (2r-(1(s*),2r*,3s*))-
130370-59-1
gi-129471
(2r-(1(s*),2r*,3s*))-n4-hydroxy-n1-(2-(methylamino)-2-oxo-1-(phenylmethyl)ethyl)-2-(2-methylpropyl)-3-((phenylthio)methyl)butanediamide
gi 129471
gw9471
CHEMBL114427 ,
(2s,3r)-n-hydroxy-n'-[(2s)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)-2-(phenylsulfanylmethyl)butanediamide
gw-9471
bdbm50069608
(2r,3s)-n*4*-hydroxy-2-isobutyl-n*1*-((s)-1-methylcarbamoyl-2-phenyl-ethyl)-3-phenylsulfanylmethyl-succinamide
SCHEMBL6838720
DTXSID60156496
gi129471
(2r,3s)-n4-hydroxy-n1-[(1s)-2-(methylamino)-2-oxo-1-(phenylmethyl)ethyl]-2-(2-methylpropyl)-3-[(phenylthio)methyl]butanediamide
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Interstitial collagenaseHomo sapiens (human)IC50 (µMol)0.02000.00020.850210.0000AID73284
Low affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)IC50 (µMol)0.04000.04000.31001.0000AID44539
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)IC50 (µMol)5.30000.00021.014010.0000AID215604
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (55)

Processvia Protein(s)Taxonomy
proteolysisInterstitial collagenaseHomo sapiens (human)
protein metabolic processInterstitial collagenaseHomo sapiens (human)
extracellular matrix disassemblyInterstitial collagenaseHomo sapiens (human)
collagen catabolic processInterstitial collagenaseHomo sapiens (human)
positive regulation of protein-containing complex assemblyInterstitial collagenaseHomo sapiens (human)
cellular response to UV-AInterstitial collagenaseHomo sapiens (human)
extracellular matrix organizationInterstitial collagenaseHomo sapiens (human)
B cell antigen processing and presentationLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
positive regulation of humoral immune response mediated by circulating immunoglobulinLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
Fc-epsilon receptor signaling pathwayLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
macrophage activationLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
positive regulation of nitric-oxide synthase activityLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
positive regulation of killing of cells of another organismLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
Fc receptor-mediated immune complex endocytosisLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
biological process involved in interspecies interaction between organismsLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
immune responseLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to hypoxiaDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
neutrophil mediated immunityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
germinal center formationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of leukocyte chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane protein ectodomain proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch receptor processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell population proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to xenobiotic stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of T cell chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
signal releaseDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
B cell differentiationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell growthDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to lipopolysaccharideDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of chemokine productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
regulation of mast cell apoptotic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
T cell differentiation in thymusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesion mediated by integrinDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
wound healing, spreading of epidermal cellsDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
spleen developmentDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell motilityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
defense response to Gram-positive bacteriumDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cellular response to high density lipoprotein particle stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
commissural neuron axon guidanceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of cold-induced thermogenesisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
endopeptidase activityInterstitial collagenaseHomo sapiens (human)
metalloendopeptidase activityInterstitial collagenaseHomo sapiens (human)
serine-type endopeptidase activityInterstitial collagenaseHomo sapiens (human)
peptidase activityInterstitial collagenaseHomo sapiens (human)
zinc ion bindingInterstitial collagenaseHomo sapiens (human)
protease bindingLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
integrin bindingLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
protein bindingLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
low-affinity IgE receptor activityLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
IgE bindingLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
metal ion bindingLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
carbohydrate bindingLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
endopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
interleukin-6 receptor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
integrin bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
peptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metallopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
SH3 domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytokine bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
PDZ domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
tumor necrosis factor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metal ion bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

Processvia Protein(s)Taxonomy
extracellular regionInterstitial collagenaseHomo sapiens (human)
extracellular matrixInterstitial collagenaseHomo sapiens (human)
extracellular spaceInterstitial collagenaseHomo sapiens (human)
plasma membraneLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
extracellular exosomeLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
external side of plasma membraneLow affinity immunoglobulin epsilon Fc receptorHomo sapiens (human)
cell-cell junctionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
focal adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
ruffle membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Golgi membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
endoplasmic reticulum lumenDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell surfaceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
actin cytoskeletonDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
apical plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane raftDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID215604Inhibition of TNF(tumor necrosis factor) in human blood1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.
AID73284Inhibitory activity towards human recombinant fibroblast collagenase1998Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
Selective inhibition of low affinity IgE receptor (CD23) processing.
AID44539Tested for inhibition against CD23 (IgE receptor) proteolysis in membranes derived from RPM18866 cells ( a human B-cell line); value ranges from 40-801998Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
Selective inhibition of low affinity IgE receptor (CD23) processing.
AID215431Inhibitory activity against Tumor necrosis factor alpha-converting enzyme (TACE) in blood.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's7 (70.00)18.2507
2000's3 (30.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.80

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 Index11.80 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.80)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (10.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (90.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]