Page last updated: 2024-12-08

pefabloc

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

Cross-References

ID SourceID
PubMed CID186136
SCHEMBL ID25973
MeSH IDM0042466

Synonyms (69)

Synonym
MLS002153464
smr001230821
AKOS015847774
EU-0100132 ,
4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride, >=97%
aebsf
aebsf, hydrochloride
pefabloc
nsc-727364
nsc727364
30827-99-7
pefabloc sc
4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride
NCGC00093623-01
4-(2-aminoethyl) benzenesulfonyl fluoride hydrochloride
A-5440
4-(2-aminoethyl)-benzenesulfonylfluoride hydrochloride
A 8456
dha6vl95hl ,
nsc 727364
benzenesulfonyl fluoride, 4-(2-aminoethyl)-, hydrochloride
4-(2-aminoethyl)benzenesulfonylfluoride hydrochloride
benzenesulfonyl fluoride, p-(2-aminoethyl)-, hydrochloride
unii-dha6vl95hl
M01245
aebsf hcl biochemistry grade
4-(2-aminoethyl)benzenesulfonyl fluoride hcl
4-(2-aminoethyl)benzenesulphonyl fluoride hydrochloride
A820639
aebsf hydrochloride
FT-0616512
LP00132
S7378
CCG-207883
4-(2-aminoethyl)benzene-1-sulfonyl fluoride hydrochloride
SCHEMBL25973
NCGC00260817-01
tox21_500132
pefabloc, antibiotic for culture media use only
P-1195
2-aminoethylphenylsulfonehydrochloride
aebsf hcl
aebsf (hydrochloride)
HY-12821
mfcd00132962
aebsf.hcl
pefabloc(r) sc, analytical standard
DTXSID60184830
benzenesulfonyl fluoride, 4-(2-aminoethyl)-, hydrochloride (1:1)
pefabloc(r) sc, certified reference material, tracecert(r)
SR-01000075690-1
4-(2-aminoethyl)benzenesulfonylfluoridehydrochloride
30827-99-7 (hcl)
4-(2-aminoethyl)benzenesulfonyl fluoride, hcl
SW219355-1
aebsf-hydrochloride
EX-A2487
FS-5456
A14270
BCP32155
SY007034
4-(2-aminoethyl)benzenesulfonyl fluoride;hydrochloride
T70748
4-(2-aminoethyl)benzenesulfonyl fluoride hcl [for biochemical research]
4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride [for biochemical research]
EN300-6762645
(2-aminoethyl)benzenesulfonyl fluoride hydrochloride
AC-36097
Z1741982548
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency6.30960.044717.8581100.0000AID485294
ATAD5 protein, partialHomo sapiens (human)Potency20.58780.004110.890331.5287AID504466
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency6.51310.00419.984825.9290AID504444
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency0.25120.01789.637444.6684AID588834
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency50.01120.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency16.39730.004611.374133.4983AID624296; AID624297
DNA polymerase kappa isoform 1Homo sapiens (human)Potency100.00000.031622.3146100.0000AID588579
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ProthrombinHomo sapiens (human)IC50 (µMol)62.00000.00000.710710.0000AID706153
PlasminogenHomo sapiens (human)IC50 (µMol)240.00000.02503.628010.0000AID706154
Chymotrypsin-like elastase family member 1Sus scrofa (pig)IC50 (µMol)160.00002.18525.171310.0000AID706156
Cathepsin GHomo sapiens (human)IC50 (µMol)250.00000.01372.42247.4130AID706155
Chymotrypsin-like elastase family member 2ASus scrofa (pig)IC50 (µMol)160.00002.18522.34262.5000AID706156
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (70)

Processvia Protein(s)Taxonomy
positive regulation of protein phosphorylationProthrombinHomo sapiens (human)
proteolysisProthrombinHomo sapiens (human)
acute-phase responseProthrombinHomo sapiens (human)
cell surface receptor signaling pathwayProthrombinHomo sapiens (human)
G protein-coupled receptor signaling pathwayProthrombinHomo sapiens (human)
blood coagulationProthrombinHomo sapiens (human)
positive regulation of cell population proliferationProthrombinHomo sapiens (human)
regulation of cell shapeProthrombinHomo sapiens (human)
response to woundingProthrombinHomo sapiens (human)
negative regulation of platelet activationProthrombinHomo sapiens (human)
platelet activationProthrombinHomo sapiens (human)
regulation of blood coagulationProthrombinHomo sapiens (human)
positive regulation of blood coagulationProthrombinHomo sapiens (human)
positive regulation of cell growthProthrombinHomo sapiens (human)
positive regulation of insulin secretionProthrombinHomo sapiens (human)
positive regulation of collagen biosynthetic processProthrombinHomo sapiens (human)
fibrinolysisProthrombinHomo sapiens (human)
negative regulation of proteolysisProthrombinHomo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATProthrombinHomo sapiens (human)
negative regulation of astrocyte differentiationProthrombinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolProthrombinHomo sapiens (human)
regulation of cytosolic calcium ion concentrationProthrombinHomo sapiens (human)
cytolysis by host of symbiont cellsProthrombinHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionProthrombinHomo sapiens (human)
negative regulation of fibrinolysisProthrombinHomo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptideProthrombinHomo sapiens (human)
neutrophil-mediated killing of gram-negative bacteriumProthrombinHomo sapiens (human)
positive regulation of lipid kinase activityProthrombinHomo sapiens (human)
negative regulation of cytokine production involved in inflammatory responseProthrombinHomo sapiens (human)
positive regulation of protein localization to nucleusProthrombinHomo sapiens (human)
positive regulation of phospholipase C-activating G protein-coupled receptor signaling pathwayProthrombinHomo sapiens (human)
ligand-gated ion channel signaling pathwayProthrombinHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processProthrombinHomo sapiens (human)
proteolysisPlasminogenHomo sapiens (human)
blood coagulationPlasminogenHomo sapiens (human)
negative regulation of cell population proliferationPlasminogenHomo sapiens (human)
negative regulation of cell-substrate adhesionPlasminogenHomo sapiens (human)
extracellular matrix disassemblyPlasminogenHomo sapiens (human)
tissue regenerationPlasminogenHomo sapiens (human)
fibrinolysisPlasminogenHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationPlasminogenHomo sapiens (human)
myoblast differentiationPlasminogenHomo sapiens (human)
muscle cell cellular homeostasisPlasminogenHomo sapiens (human)
tissue remodelingPlasminogenHomo sapiens (human)
biological process involved in interaction with symbiontPlasminogenHomo sapiens (human)
negative regulation of fibrinolysisPlasminogenHomo sapiens (human)
positive regulation of fibrinolysisPlasminogenHomo sapiens (human)
trophoblast giant cell differentiationPlasminogenHomo sapiens (human)
labyrinthine layer blood vessel developmentPlasminogenHomo sapiens (human)
mononuclear cell migrationPlasminogenHomo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmissionPlasminogenHomo sapiens (human)
negative regulation of cell-cell adhesion mediated by cadherinPlasminogenHomo sapiens (human)
proteolysisCathepsin GHomo sapiens (human)
angiotensin maturationCathepsin GHomo sapiens (human)
monocyte chemotaxisCathepsin GHomo sapiens (human)
protein phosphorylationCathepsin GHomo sapiens (human)
proteolysisCathepsin GHomo sapiens (human)
immune responseCathepsin GHomo sapiens (human)
protein processingCathepsin GHomo sapiens (human)
cytokine-mediated signaling pathwayCathepsin GHomo sapiens (human)
protein metabolic processCathepsin GHomo sapiens (human)
antibacterial humoral responseCathepsin GHomo sapiens (human)
extracellular matrix disassemblyCathepsin GHomo sapiens (human)
platelet activationCathepsin GHomo sapiens (human)
purinergic nucleotide receptor signaling pathwayCathepsin GHomo sapiens (human)
neutrophil activationCathepsin GHomo sapiens (human)
positive regulation of immune responseCathepsin GHomo sapiens (human)
defense response to Gram-negative bacteriumCathepsin GHomo sapiens (human)
defense response to Gram-positive bacteriumCathepsin GHomo sapiens (human)
defense response to fungusCathepsin GHomo sapiens (human)
negative regulation of T cell activationCathepsin GHomo sapiens (human)
neutrophil-mediated killing of gram-positive bacteriumCathepsin GHomo sapiens (human)
cellular response to lipopolysaccharideCathepsin GHomo sapiens (human)
biofilm matrix disassemblyCathepsin GHomo sapiens (human)
positive regulation of platelet aggregationCathepsin GHomo sapiens (human)
regulation of gene expressionTransmembrane protease serine 4Homo sapiens (human)
negative regulation of growth rateTransmembrane protease serine 4Homo sapiens (human)
proteolysisTransmembrane protease serine 4Homo sapiens (human)
response to woundingTransmembrane protease serine 4Homo sapiens (human)
protein processingTransmembrane protease serine 4Homo sapiens (human)
positive regulation of viral entry into host cellTransmembrane protease serine 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingProthrombinHomo sapiens (human)
serine-type endopeptidase activityProthrombinHomo sapiens (human)
signaling receptor bindingProthrombinHomo sapiens (human)
calcium ion bindingProthrombinHomo sapiens (human)
protein bindingProthrombinHomo sapiens (human)
growth factor activityProthrombinHomo sapiens (human)
heparin bindingProthrombinHomo sapiens (human)
thrombospondin receptor activityProthrombinHomo sapiens (human)
protease bindingPlasminogenHomo sapiens (human)
endopeptidase activityPlasminogenHomo sapiens (human)
serine-type endopeptidase activityPlasminogenHomo sapiens (human)
signaling receptor bindingPlasminogenHomo sapiens (human)
protein bindingPlasminogenHomo sapiens (human)
serine-type peptidase activityPlasminogenHomo sapiens (human)
enzyme bindingPlasminogenHomo sapiens (human)
kinase bindingPlasminogenHomo sapiens (human)
protein domain specific bindingPlasminogenHomo sapiens (human)
apolipoprotein bindingPlasminogenHomo sapiens (human)
protein-folding chaperone bindingPlasminogenHomo sapiens (human)
protein antigen bindingPlasminogenHomo sapiens (human)
serine-type endopeptidase activityCathepsin GHomo sapiens (human)
protein bindingCathepsin GHomo sapiens (human)
heparin bindingCathepsin GHomo sapiens (human)
peptidase activityCathepsin GHomo sapiens (human)
serine-type peptidase activityCathepsin GHomo sapiens (human)
receptor ligand activityCathepsin GHomo sapiens (human)
caspase bindingCathepsin GHomo sapiens (human)
serine-type endopeptidase activityTransmembrane protease serine 4Homo sapiens (human)
protein bindingTransmembrane protease serine 4Homo sapiens (human)
serine-type peptidase activityTransmembrane protease serine 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
external side of plasma membraneProthrombinHomo sapiens (human)
collagen-containing extracellular matrixProthrombinHomo sapiens (human)
extracellular regionProthrombinHomo sapiens (human)
extracellular spaceProthrombinHomo sapiens (human)
endoplasmic reticulum lumenProthrombinHomo sapiens (human)
Golgi lumenProthrombinHomo sapiens (human)
plasma membraneProthrombinHomo sapiens (human)
extracellular exosomeProthrombinHomo sapiens (human)
blood microparticleProthrombinHomo sapiens (human)
collagen-containing extracellular matrixProthrombinHomo sapiens (human)
extracellular spaceProthrombinHomo sapiens (human)
extracellular regionPlasminogenHomo sapiens (human)
extracellular spacePlasminogenHomo sapiens (human)
plasma membranePlasminogenHomo sapiens (human)
external side of plasma membranePlasminogenHomo sapiens (human)
cell surfacePlasminogenHomo sapiens (human)
platelet alpha granule lumenPlasminogenHomo sapiens (human)
collagen-containing extracellular matrixPlasminogenHomo sapiens (human)
extracellular exosomePlasminogenHomo sapiens (human)
blood microparticlePlasminogenHomo sapiens (human)
Schaffer collateral - CA1 synapsePlasminogenHomo sapiens (human)
glutamatergic synapsePlasminogenHomo sapiens (human)
extracellular spacePlasminogenHomo sapiens (human)
collagen-containing extracellular matrixCathepsin GHomo sapiens (human)
extracellular regionCathepsin GHomo sapiens (human)
extracellular spaceCathepsin GHomo sapiens (human)
nucleusCathepsin GHomo sapiens (human)
lysosomeCathepsin GHomo sapiens (human)
cytosolCathepsin GHomo sapiens (human)
plasma membraneCathepsin GHomo sapiens (human)
cytoplasmic stress granuleCathepsin GHomo sapiens (human)
membraneCathepsin GHomo sapiens (human)
secretory granuleCathepsin GHomo sapiens (human)
azurophil granule lumenCathepsin GHomo sapiens (human)
collagen-containing extracellular matrixCathepsin GHomo sapiens (human)
extracellular exosomeCathepsin GHomo sapiens (human)
cytoplasmCathepsin GHomo sapiens (human)
intracellular membrane-bounded organelleCathepsin GHomo sapiens (human)
extracellular spaceTransmembrane protease serine 4Homo sapiens (human)
plasma membraneTransmembrane protease serine 4Homo sapiens (human)
membraneTransmembrane protease serine 4Homo sapiens (human)
secretory granuleTransmembrane protease serine 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID706156Inhibition of porcine pancreatic elastase assessed as hydrolysis of N-succinyl-Ala-Ala-Ala-p-nitroanilide incubated for 2 hrs measured for 20 mins by microplate reader analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.
AID706154Inhibition of plasmin assessed as hydrolysis of H-D-Val-L-Leu-L-Lys-p-nitroanilide incubated for 2 hrs measured for 20 mins by microplate reader analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.
AID706155Inhibition of cathepsin G assessed as hydrolysis of N-succinyl-Ala-Ala-Pro-Phe-p-nitroanilide incubated for 2 hrs measured for 20 mins by microplate reader analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.
AID706157Inhibition of chymotrypsin assessed as hydrolysis of N-succinyl-Ala-Ala-Pro-Phe-p-nitroanilide incubated for 2 hrs measured for 20 mins by microplate reader analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.
AID706153Inhibition of thrombin assessed as hydrolysis of H-D-Pro-L-Phe-L-Arg-p-nitroanilide incubated for 2 hrs measured for 20 mins by microplate reader analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID730377Inhibition of N-terminal His6-tagged recombinant TMPRSS4 (unknown origin) fused with enterokinase cleavage sequence DYKDDDGDYKDDDDK expressed in Escherichia coli BL21 (DE3) using Z-Phe-Arg-7-amido-4-methylcoumarin hydrochloride as substrate by fluorometri2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Discovery of novel 2-hydroxydiarylamide derivatives as TMPRSS4 inhibitors.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID706158Inhibition of trypsin assessed as hydrolysis of H-D-Pro-L-Phe-L-Arg-p-nitroanilide incubated for 2 hrs measured for 20 mins by microplate reader analysis2012Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (18.18)29.6817
2010's7 (63.64)24.3611
2020's2 (18.18)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 38.78

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index38.78 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index51.07 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (38.78)

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%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]