Information on EC 3.4.22.36 - caspase-1

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The expected taxonomic range for this enzyme is: Coelomata

EC NUMBER
COMMENTARY hide
3.4.22.36
-
RECOMMENDED NAME
GeneOntology No.
caspase-1
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
Strict requirement for an Asp residue at position P1 and has a preferred cleavage sequence of Tyr-Val-Ala-Asp-/-
show the reaction diagram
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
122191-40-6
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
greater wax moth
UniProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
Mus musculus BALB/c
Balb/c mice
-
-
Manually annotated by BRENDA team
Mus musculus BALB/cJ
BALB/cJ mice
-
-
Manually annotated by BRENDA team
Mus musculus C3H/An
strain C3H/An
SwissProt
Manually annotated by BRENDA team
Mus musculus C57BL/6
C57BL/6 mice
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
UniProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
-
caspase-1 is required for nuclear translocation of intracellular interleukin-37 and for secretion of mature interleukin-37
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(Z-LEHD)2-R110 tetrapeptide + H2O
?
show the reaction diagram
-
-
-
-
?
4-[[4'-(dimethylamino)phenyl]azo]-benzoic acid-YVADAPV-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid + H2O
4-[[4'-(dimethylamino)phenyl]azo]-benzoic acid-YVADAPV + 5-[(2-aminoethyl)-amino]naphthalenesulfonic acid
show the reaction diagram
-
-
-
?
Ac-LEHD-7-amido-4-methylcoumarin + H2O
Ac-LEHD + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Ac-Trp-Glu-His-Asp-7-amino-4-trifluoromethylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-YVAD-4-nitroanilide + H2O
Ac-YVAD + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-DEVD-4-nitroanilide + H2O
acetyl-DEVD + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-DQMD-4-nitroanilide + H2O
acetyl-DQMD + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-L-Leu-L-Glu-L-His-L-Asp-7-amido-4-methylcoumarin + H2O
acetyl-L-Leu-L-Glu-L-His-L-Asp + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
acetyl-L-Trp-L-Glu-L-His-L-Asp-7-amido-4-methylcoumarin + H2O
acetyl-L-Trp-L-Glu-L-His-L-Asp + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
acetyl-VEID-4-nitroanilide + H2O
acetyl-VEID + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-VQVD-4-nitroanilide + H2O
acetyl-VQVD + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-WEHD-7-amido-4-methylcoumarin + H2O
acetyl-WEHD + 7-amino-4-methylcoumarin
show the reaction diagram
acetyl-YEVD-4-nitroanilide + H2O
acetyl-YEVD + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-YEVDGW-amide + H2O
?
show the reaction diagram
-
preferred peptide substrate
-
-
?
acetyl-YVAD-4-nitroanilide + H2O
acetyl-YVAD + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-YVAD-7-amido-4-methylcoumarin + H2O
acetyl-YVAD + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
Assc2 peptide + H2O
?
show the reaction diagram
-
-
-
-
?
ataxin-3 + H2O
?
show the reaction diagram
-
-
-
-
?
Bap31 protein + H2O
?
show the reaction diagram
-
-
-
-
?
Bcl-xL + H2O
?
show the reaction diagram
-
-
-
-
?
beta-actin + H2O
?
show the reaction diagram
calpastatin + H2O
?
show the reaction diagram
-
-
-
-
?
carboxyfluorescein-YVAD-fluoromethylketone + H2O
?
show the reaction diagram
-
-
-
-
?
caspase-1 + H2O
?
show the reaction diagram
-
-
-
-
?
cPLA2 peptide + H2O
?
show the reaction diagram
-
-
-
-
?
cyclin G-associated kinase + H2O
?
show the reaction diagram
-
-
-
-
?
DNA replication licensing factor MCM4 + H2O
?
show the reaction diagram
-
-
-
-
?
elF-4H peptide + H2O
?
show the reaction diagram
-
-
-
-
?
endoplasmin + H2O
?
show the reaction diagram
-
-
-
-
?
epidermal growth factor receptor + H2O
?
show the reaction diagram
eukaryotic translation initiation factor 3 subunit J + H2O
?
show the reaction diagram
-
-
-
-
?
FLP-1 peptide + H2O
?
show the reaction diagram
-
-
-
-
?
FYN-binding protein + H2O
?
show the reaction diagram
-
-
-
-
?
GADPH + H2O
?
show the reaction diagram
-
-
-
-
?
gamma-actin + H2O
?
show the reaction diagram
-
-
-
-
?
gasdermin D + H2O
?
show the reaction diagram
-
-
-
-
?
GIT2 peptide + H2O
?
show the reaction diagram
-
-
-
-
?
heat shock protein 60 + H2O
?
show the reaction diagram
-
-
-
-
?
histone E3 peptide + H2O
?
show the reaction diagram
-
-
-
-
?
HnRNP + H2O
?
show the reaction diagram
-
-
-
-
?
Hsp90 + H2O
?
show the reaction diagram
-
-
-
-
?
IL-1 beta + H2O
?
show the reaction diagram
-
-
-
-
?
IL-18 + H2O
?
show the reaction diagram
-
-
-
-
?
IL1F7 + H2O
?
show the reaction diagram
-
-
-
-
?
interferon-gamma inducing factor + H2O
?
show the reaction diagram
-
cleavage site: LESD-/-
-
-
?
interleukin-1 + H2O
interleukin-1beta
show the reaction diagram
-
-
-
-
?
interleukin-18 + H2O
?
show the reaction diagram
-
caspase-1 is required for control of oral infection with wild-type Salmonella in mice, as well as for resistance to septic shock following systemic challenge with live attenuated Salmonella enterica serovar typhimurium. Furthermore host defense against Salmonella enterica serovar typhimurium requires both caspase-1 substrates IL-1beta and IL-18
-
-
?
interleukin-1beta + H2O
?
show the reaction diagram
-
caspase-1 is required for control of oral infection with wild-type Salmonella in mice, as well as for resistance to septic shock following systemic challenge with live attenuated Salmonella enterica serovar typhimurium. Furthermore host defense against Salmonella enterica serovar typhimurium requires both caspase-1 substrates IL-1beta and IL-18
-
-
?
ligatin + H2O
?
show the reaction diagram
-
-
-
-
?
LMNA Isoform + H2O
?
show the reaction diagram
-
-
-
-
?
MAP-tau Isoform + H2O
?
show the reaction diagram
-
-
-
-
?
MCM3 peptide + H2O
?
show the reaction diagram
-
-
-
-
?
MyD88 adaptor-like + H2O
?
show the reaction diagram
N-acetyl-Asp-Glu-Val-Asp-7-amido-4-methylcoumarin + H2O
N-acetyl-Asp-Glu-Val-Asp + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
N-acetyl-DEVD-7-amido-4-methylcoumarin + H2O
N-acetyl-DEVD + 7-amino-4-methylcoumarin
show the reaction diagram
-
preferred substrate
-
-
?
N-acetyl-IETD-7-amido-4-methylcoumarin + H2O
N-acetyl-IETD + 7-amino-4-methylcoumarin
show the reaction diagram
-
negligible activity
-
-
?
N-acetyl-LEHD-7-amido-4-methylcoumarin + H2O
N-acetyl-LEHD + 7-amino-4-methylcoumarin
show the reaction diagram
-
negligible activity
-
-
?
N-acetyl-WEHD-7-amido-4-trifluoromethylcoumarin + H2O
N-acetyl-WEHD + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
Nedd4 + H2O
?
show the reaction diagram
-
-
-
-
?
nuclear immunophilin FKBP46 + H2O
?
show the reaction diagram
-
-
-
?
p35 + H2O
100000 Da fragment + 25000 Da fragment
show the reaction diagram
cleavage at Asp87
-
?
parkin + H2O
?
show the reaction diagram
PARP + H2O
?
show the reaction diagram
-
-
-
-
?
periphilin-1 + H2O
?
show the reaction diagram
-
-
-
-
?
PLA2G4A + H2O
?
show the reaction diagram
-
-
-
-
?
poly(ADP-ribose)polymerase + H2O
?
show the reaction diagram
-
-
-
?
PPARgamma + H2O
?
show the reaction diagram
-
-
-
-
?
pre-interleukin-18 + H2O
interleukin-18 + ?
show the reaction diagram
pre-interleukin-1beta + H2O
17000 Da fragment + 28000 Da fragment
show the reaction diagram
pre-interleukin-1beta + H2O
interleukin-1beta + ?
show the reaction diagram
PREL-1 peptide + H2O
?
show the reaction diagram
-
-
-
-
?
pro-caspase-7 + H2O
caspase-7 + ?
show the reaction diagram
pro-caspase-7 + H2O
caspase-7 + amino-terminal procaspase-7 peptide
show the reaction diagram
-
consensus caspase-7 recognition sequence DEVD, caspase-1 cleaves caspase-7 at the canonical activation sites Asp23 and Asp198, D23A/D198A double caspase-7 mutant is no substrate
-
-
?
pro-interleukin-18 + H2O
interleukin-18 + ?
show the reaction diagram
pro-interleukin-18 + H2O
interleukin-18 propeptide
show the reaction diagram
pro-interleukin-18 + H2O
mature interleukin-18
show the reaction diagram
pro-interleukin-18 + H2O
mature interleukin-18 + ?
show the reaction diagram
pro-interleukin-1beta + H2O
17000 Da fragment + 28000 Da fragment
show the reaction diagram
pro-interleukin-1beta + H2O
interleukin-1beta + ?
show the reaction diagram
pro-interleukin-1beta + H2O
interleukin-1beta propeptide
show the reaction diagram
pro-interleukin-1beta + H2O
mature interleukin-1beta
show the reaction diagram
pro-interleukin-1beta + H2O
mature interleukin-1beta + ?
show the reaction diagram
pro-interleukin-33 + H2O
interleukin-33 + ?
show the reaction diagram
pro-interleukin-33 + H2O
mature interleukin-33 + ?
show the reaction diagram
-
recombinant pro-interleukin-33 is cleaved by recombinant caspase-1 in vitro
-
-
?
pro-interleukin-37 + H2O
interleukin-37 propeptide
show the reaction diagram
-
caspase-1 processing at position D20 activates interleukin-37
-
-
?
PSEN1 + H2O
?
show the reaction diagram
-
-
-
-
?
PSEN2 + H2O
?
show the reaction diagram
-
-
-
-
?
pyrin + H2O
?
show the reaction diagram
SMG7 peptide + H2O
?
show the reaction diagram
-
-
-
-
?
sphingosine kinase 2 + H2O
?
show the reaction diagram
-
-
-
-
?
splicing factor U2AF 65-kDa subunit + H2O
?
show the reaction diagram
-
-
-
-
?
SPTAN1 + H2O
?
show the reaction diagram
-
-
-
-
?
succinyl-YVAD-4-nitroanilide + H2O
succinyl-YVAD + 4-nitroaniline
show the reaction diagram
succinyl-YVAD-7-amido-4-methylcoumarin + H2O
succinyl-YVAD + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
synapse-associated protein 1 + H2O
?
show the reaction diagram
-
-
-
-
?
target of Myb protein 1 pepitde + H2O
?
show the reaction diagram
-
-
-
-
?
TF AP-2alpha + H2O
?
show the reaction diagram
-
-
-
-
?
TIF1b peptide + H2O
?
show the reaction diagram
-
-
-
-
?
Trp-Glu-His-Asp-p-nitroanilide + H2O
Trp-Glu-His-Asp + p-nitroaniline
show the reaction diagram
-
-
-
-
?
Vsp72 peptide + H2O
?
show the reaction diagram
-
-
-
-
?
WEDH + H2O
?
show the reaction diagram
-
-
-
-
?
zyxin + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
Bap31 protein + H2O
?
show the reaction diagram
-
-
-
-
?
epidermal growth factor receptor + H2O
?
show the reaction diagram
-
cleavage during apoptosis
-
-
?
interferon-gamma inducing factor + H2O
?
show the reaction diagram
-
cleavage site: LESD-/-
-
-
?
interleukin-1 + H2O
interleukin-1beta
show the reaction diagram
-
-
-
-
?
interleukin-18 + H2O
?
show the reaction diagram
-
caspase-1 is required for control of oral infection with wild-type Salmonella in mice, as well as for resistance to septic shock following systemic challenge with live attenuated Salmonella enterica serovar typhimurium. Furthermore host defense against Salmonella enterica serovar typhimurium requires both caspase-1 substrates IL-1beta and IL-18
-
-
?
interleukin-1beta + H2O
?
show the reaction diagram
-
caspase-1 is required for control of oral infection with wild-type Salmonella in mice, as well as for resistance to septic shock following systemic challenge with live attenuated Salmonella enterica serovar typhimurium. Furthermore host defense against Salmonella enterica serovar typhimurium requires both caspase-1 substrates IL-1beta and IL-18
-
-
?
MyD88 adaptor-like + H2O
?
show the reaction diagram
nuclear immunophilin FKBP46 + H2O
?
show the reaction diagram
P89116
-
-
-
?
p35 + H2O
100000 Da fragment + 25000 Da fragment
show the reaction diagram
P89116
cleavage at Asp87
-
?
parkin + H2O
?
show the reaction diagram
-
cleavage at Asp126-Ser127. Caspase-1 and caspase-8 dependent parkin cleavage in sporadic Parkinsons disease may play an important role in the degenerative process by initiating a vicious circle that leads to the accumulation of toxic parkin substrates, e.g. alpha-synuclein
-
-
?
pre-interleukin-18 + H2O
interleukin-18 + ?
show the reaction diagram
pre-interleukin-1beta + H2O
interleukin-1beta + ?
show the reaction diagram
pro-caspase-7 + H2O
caspase-7 + ?
show the reaction diagram
pro-interleukin-18 + H2O
interleukin-18 + ?
show the reaction diagram
pro-interleukin-18 + H2O
interleukin-18 propeptide
show the reaction diagram
pro-interleukin-18 + H2O
mature interleukin-18
show the reaction diagram
pro-interleukin-18 + H2O
mature interleukin-18 + ?
show the reaction diagram
pro-interleukin-1beta + H2O
17000 Da fragment + 28000 Da fragment
show the reaction diagram
pro-interleukin-1beta + H2O
interleukin-1beta + ?
show the reaction diagram
pro-interleukin-1beta + H2O
interleukin-1beta propeptide
show the reaction diagram
pro-interleukin-1beta + H2O
mature interleukin-1beta
show the reaction diagram
pro-interleukin-1beta + H2O
mature interleukin-1beta + ?
show the reaction diagram
pro-interleukin-33 + H2O
interleukin-33 + ?
show the reaction diagram
-
-
-
-
?
pro-interleukin-33 + H2O
mature interleukin-33 + ?
show the reaction diagram
-
recombinant pro-interleukin-33 is cleaved by recombinant caspase-1 in vitro
-
-
?
pro-interleukin-37 + H2O
interleukin-37 propeptide
show the reaction diagram
-
caspase-1 processing at position D20 activates interleukin-37
-
-
?
pyrin + H2O
?
show the reaction diagram
-
caspase-1 cleaves pyrin at Asp330, Familial Mediterranean fever-associated mutants are cleaved more than wild-type pyrin by caspase-1. Pyrin itself regulates caspase-1 activation and interleukin-1beta production through interaction of its N-terminal PYD motif with the ASC adapterprotein, and also modulates interleukin-1beta production by interaction of its C-terminal B30.2 domain with the catalytic domains of caspase-1
-
-
?
sphingosine kinase 2 + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
K+
-
high extracellular K+ levels inhibit Asc-dependent caspase-1 activation, whereas Ipaf-dependent activation was unaffected by potassium treatment
Zn2+
-
pannexin-1-dependent caspase-1 activation is regulated by zinc and induced by ATP, molecular mechanism
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1S,9S)-N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-9-[(isoquinolin-1-ylcarbonyl)amino]-6,10-dioxooctahydro-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxamide
-
good selectivity against the related enzymes caspase-3 and caspase-8
(3)-4-oxo-3-([6-(([4-(quinoxalin-2-yloxy)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
(3S)-3-((6-[((4-[(6-chloropyrazin-2-yl)amino]phenyl)carbonyl)amino]-2-thiophen-2-ylhexanoyl)amino)-4-oxobutanoic acid
-
-
(3S)-3-((6-[((4-[(6-methylquinoxalin-2-yl)amino]phenyl)carbonyl)amino]-2-thiophen-2-ylhexanoyl)amino)-4-oxobutanoic acid
-
-
(3S)-3-([2-(2-fluorophenyl)-6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)-4-oxobutanoic acid
-
-
(3S)-3-([2-ethyl-6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)-4-oxobutanoic acid
-
-
(3S)-3-([6-(([3-methyl-4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)-2-thiophen-2-ylhexanoyl]amino)-4-oxobutanoic acid
-
-
(3S)-3-[([(1S,9S)-9-[(isoquinolin-1-ylcarbonyl)amino]-6,10-dioxooctahydro-6H-pyridazino[1,2-a][1,2]diazepin-1-yl]carbonyl)amino]-4-oxobutanoic acid
-
-
(3S)-3-[([(3S,6S,9aR)-6-[(isoquinolin-1-ylcarbonyl)amino]-5-oxo-2,3,5,6,9,9a-hexahydro-1H-pyrrolo[1,2-a]azepin-3-yl]carbonyl)amino]-4-oxobutanoic acid
-
-
(3S)-3-[([(4S,7S,10aS)-7-[(isoquinolin-1-ylcarbonyl)amino]-6-oxo-3,4,6,7,10,10a-hexahydro-1H-[1,4]oxazino[4,3-a]azepin-4-yl]carbonyl)amino]-4-oxobutanoic acid
-
-
(3S)-4-oxo-3-([2-phenyl-6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
(3S)-4-oxo-3-([4-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)butanoyl]amino)butanoic acid
-
-
(3S)-4-oxo-3-([5-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)pentanoyl]amino)butanoic acid
-
-
(3S)-4-oxo-3-([6-(([4-(pyrazin-2-ylamino)phenyl]carbonyl)amino)-2-thiophen-2-ylhexanoyl]amino)butanoic acid
-
-
(3S)-4-oxo-3-([6-(([4-(pyrazin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
(3S)-4-oxo-3-([6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
(3S)-4-oxo-3-([6-(([4-(quinoxalin-2-yloxy)phenyl]carbonyl)amino)-2-thiophen-2-ylhexanoyl]amino)butanoic acid
-
-
(3S)-4-oxo-3-([6-(([4-(quinoxalin-2-yloxy)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
(3S)-4-oxo-3-([7-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)heptanoyl]amino)butanoic acid
-
-
(3S)-4-oxo-3-[((4-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]phenyl)carbonyl)amino]butanoic acid
-
-
(3S)-4-oxo-3-[((4-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-2-yl)carbonyl)amino]butanoic acid
-
-
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]-2,3-dihydropyrazin-2-yl)carbonyl)amino]butanoic acid
-
-
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]furan-2-yl)carbonyl)amino]butanoic acid
-
-
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-2-yl)acetyl)amino]butanoic acid
-
-
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-2-yl)carbonyl)amino]butanoic acid
-
-
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-3-yl)carbonyl)amino]butanoic acid
-
-
(3S)-4-oxo-3-[((6-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]pyridin-3-yl)carbonyl)amino]butanoic acid
-
-
(3S)-4-oxo-3-[((trans-4-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]cyclohexyl)carbonyl)amino]butanoic acid
-
-
(3S)-4-oxo-3-[(7-oxo-7-([4-(quinoxalin-2-ylamino)phenyl]amino)heptanoyl)amino]butanoic acid
-
-
(S)-2-(4'-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
(S)-3-((S)-2-((S)-2-(2-naphthamido)-3-methylbutanamido)-propanamido)-4-(2-hydroxy)benzylaminobutanoic acid
-
-
(S)-3-(2'-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
(S)-3-(2-naphthalen-1-yl-benzenesulfonylamino)-4-oxo-butyric acid
-
-
(S)-3-(3'-acetylamino-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
(S)-3-(3'-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
(S)-3-(6-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
(S)-3-(biphenyl-2-sulfonylamino)-4-oxobutyric acid
-
-
(S)-3-benzenesulfonylamino-4-oxo-5-(3-phenyl-propylsulfanyl)-pentanoic acid
-
-
(S)-3-benzenesulfonylamino-4-oxo-9-phenyl-nonanoic acid
-
-
(S)-3-benzyloxycarbonylamino-4-oxo-5-(3-phenyl-propylsulfanyl)-pentanoic acid
-
-
(S)-3-benzyloxycarbonylamino-4-oxo-9-phenyl-nonanoic acid
-
-
(S)-3-benzynesulfonylamino-4-oxo-butyric acid
-
-
1-([2-[(2,6-dimethoxyphenyl)carbonyl]hydrazino]carbonyl)-N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]cyclohexanecarboxamide
-
-
2,5-dichloro-N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]benzamide
-
-
3-(benzyloxycarbonylamino)-5-((2,3-dihydro-1H-inden-1-yl)methylsulfanylamido)-4-oxopentanoic acid
-
-
3-([(benzyloxy)carbonyl]amino)-4-oxo-9-phenylnonanoic acid
-
-
3-([(benzyloxy)carbonyl]amino)-5-([(2-cyclohexylethyl)(dihydroxy)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(2-naphthalen-1-ylethyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(3-phenylpropyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(naphthalen-1-yl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(phenyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
3-chloro-N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]benzamide
-
-
3-[[(benzyloxy)carbonyl]amino]-5-[[(2-cyclohexylethyl)sulfonyl]amino]-4-oxopentanoic acid
-
-
4-hydroxy-4,5-dicarboxypentadecanoic acid
-
-
-
5-([benzyl(dihydroxy)-lambda4-sulfanyl]amino)-3-([(benzyloxy)carbonyl]amino)-4-oxopentanoic acid
-
-
Ac-WEHD-CHO
-
active-site inhibitor
Ac-YVAD-chloromethyl ketone
-
-
Ac-YVAD-chloromethylketone
-
inhibition of caspase-1 with Ac-YVAD-CMK prevents SphK2 cleavage
Ac-YVAD-CHO
-
a caspase-1 inhibitor
acetyl-AEVD-aldehyde
-
-
acetyl-Ala-Pro-Nle-Asp-aldehyde
-
-
acetyl-DEVD-aldehyde
-
-
acetyl-DEVS-aldehyde
-
-
acetyl-IETD-aldehyde
-
-
acetyl-L-Leu-L-Glu-L-His-L-Asp-CHO
-
-
acetyl-L-Tyr-L-Val-L-Ala-L-Asp
-
-
acetyl-L-Tyr-L-Val-L-Ala-L-Asp-2,6-dimethylbenzoyloxymethylketone
-
-
acetyl-Tyr-Val-Ala-Asp chloromethyl ketone
-
inhibition of caspase-1 in rat brain reduces spontaneous nonrapid eye movement sleep and nonrapid eye movement sleep enhancement induced by lipopolysaccharide
acetyl-Tyr-Val-Ala-Asp-chloromethylketone
acetyl-Tyr-Val-Ala-Asp-CHO
-
-
acetyl-Tyr-Val-Ala-Asp-CO-(CH2)5-Ph
-
-
acetyl-WEHD-aldehyde
-
-
acetyl-YVAD-aldehyde
acetyl-YVAD-chloromethylketone
-
-
acetyl-YVAD-CHO
-
caspase-1 specific inhibitor
AWP28
-
-
-
benzyloxycarbonyl-Pro-Nle-Asp-aldehyde
-
-
-
benzyloxycarbonyl-VAD-CHO
-
-
benzyloxycarbonyl-VAD-fluoromethylketone
-
t1/2 at 0.001 mM is 2.5 s
benzyloxycarbonyl-Val-Ala-Asp-fluoromethylketone
benzyloxycarbonyl-YVAD-fluoromethylketone
-
-
berkedrimane A
-
-
-
berkedrimane B
-
-
-
butyloxycarbonyl-Asp-chloromethylketone
-
-
butyloxycarbonyl-Asp-fluoromethylketone
-
-
CA-074Me
-
the caspase-1 activation is inhibited by CA-074Me, marked inhibition at 0.05 mM
carbobenzoxy-L-valyl-L-alanyl-L-aspartyl-[O-methyl]-fluoromethylketone
-
caspase-1-specific inhibitor
carbobenzoxy-valylalanyl-aspartyl-fluoromethylketone
-
-
carbobenzyloxy-Asp-Glu-Val-Asp-fluoromethyl ketone
-
specific to suppress the activity of Sf-caspase-1 by blocking amplification of Sfcaspase-1
carbobenzyloxy-Trp-Glu-His-Asp-fluoromethylketone
-
-
carbobenzyloxy-VAD-fluoromethyl ketone
carbobenzyloxy-Val-Ala-Asp-fluoromethyl ketone
-
a broad-spectrum inhibitor of initiator caspase
carbobenzyloxy-WEHD-fluoromethyl ketone
-
caspase-1-specific inhibitor
carboxyfluorescein-YVAD-fluoromethylketone
-
-
-
Cbz-Val-Asp-fluoromethylketone
-
increase in IL-1beta protein levels in a liver injury mouse model is completely prevented with the pan-caspase inhibitor demonstrating the efficacy of Cbz-Val-Asp-fluoromethylketone to block caspase-1 activity
cowpox serpin CrmA
-
-
-
CrmA protein
-
-
-
DEVD-fluoromethylketone
-
-
Disulfiram
E-64d
-
the caspase-1 activation is inhibited by E-64d, marked inhibition at 0.05 mM
flightless-I
-
inhibits caspase-1 as a pseudosubstrate. Flightless-I might function as an inhibitor of caspase-1 in living cells through a mechanism similar to that of CrmA
-
geranylgeranyl diphosphate
-
the isoprenyl intermediate of non-sterol isoprenoid biosynthesis blocks activation of caspase-1
Glu-Val-Asp-aldehyde
-
-
IDN-6556
iodoacetamide
-
-
kaempferol
-
-
L-Tyr-L-Val-L-Ala-L-Asp-chloromethylketone
-
-
L-Tyr-L-Val-L-Ala-L-Asp-CHO
-
caspase-1-specific inhibitor
L-Tyr-L-Val-L-Ala-L-Asp-CN
-
-
luteolin
-
-
minocycline
-
-
myricetin
-
-
N-((S,Z)-1-((R)-1-((3S)-2-hydroxy-5-oxo-tetrahydrofuran-3-ylamino)-1-oxopropan-2-yl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl)-2-naphthamide
-
-
N-((S,Z)-1-((S)-1-((3S)-2-ethoxy-5-oxo-tetrahydrofuran-3-ylamino)-1-oxopropan-2-yl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl)-2-naphthamide
-
good oral bioavailability (more than 50%) when administered as prodrug
N-((S,Z)-1-((S)-1-((3S)-2-hydroxy-5-oxo-tetrahydrofuran-3-ylamino)-1-oxopropan-2-yl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl)-2-naphthamide
-
-
N-((S,Z)-1-(2-((3S)-2-ethoxy-5-oxo-tetrahydrofuran-3-ylamino)-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl)-2-naphthamide
-
good oral bioavailability (more than 50%) when administered as prodrug
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2R)-1-carboxy-5-phenylpentan-2-yl]-L-alaninamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-(benzylamino)-3-carboxypropan-2-yl]-L-alaninamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-(cyclohexylamino)propan-2-yl]-L-alaninamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-oxopropan-2-yl]-L-alaninamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[(2-fluorobenzyl)amino]propan-2-yl]-L-alaninamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[(2-methoxybenzyl)amino]propan-2-yl]-L-alaninamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[(4-hydroxybenzyl)amino]propan-2-yl]-L-alaninamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[methyl(phenyl)amino]propan-2-yl]-L-alaninamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-[(1,3-benzodioxol-5-ylmethyl)amino]-3-carboxypropan-2-yl]-L-alaninamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-[(4-carbamoylbenzyl)amino]-3-carboxypropan-2-yl]-L-alaninamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-[benzyl(methyl)amino]-3-carboxypropan-2-yl]-L-alaninamide
-
-
N-([4-(quinoxalin-2-ylamino)phenyl]carbonyl)-L-valyl-N-[(1S)-2-carboxy-1-formylethyl]-L-alaninamide
-
-
N-acetyl-L-tyrosyl-alpha-glutamyl-N-[1-(carboxymethyl)-3-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-2-oxopropyl]-L-alaninamide
-
-
N-acetyl-L-tyrosylvalyl-N-[1-(carboxymethyl)-2-oxo-7-phenylheptyl]-L-alaninamide
-
-
N-acetyl-YVAD-CHO
-
-
-
N-benzyloxycarbonyl-Tyr-Val-Ala-Asp-fluoromethyl ketone
-
-
N-benzyloxycarbonyl-Val-Ala-Asp(O-Me) fluoromethylketone
-
-
-
N-carbobenzyloxy-Val-Ala-Asp-fluoromethylketone
-
i.e. Z-VAD-FMK, active-site inhibitor
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]-1-benzothiophene-2-carboxamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]-3-(trifluoromethyl)benzamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]-3-methoxybenzamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]benzamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]isoquinoline-1-carboxamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-6-[[(phenylcarbonyl)amino]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-6-[[(phenylsulfonyl)amino]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-([[(2-methoxyphenyl)carbonyl]amino]methyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-([[(3-methoxyphenyl)carbonyl]amino]methyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-([[(4-methoxyphenyl)carbonyl]amino]methyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
-
-
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-methyl-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methoxyphenyl)carbonyl]hydrazino]carbonyl)cyclohexanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methoxyphenyl)carbonyl]hydrazino]carbonyl)cyclopentanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methylphenyl)carbonyl]hydrazino]carbonyl)cyclohexanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methylphenyl)carbonyl]hydrazino]carbonyl)cyclopentanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(2-methylbenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(2-naphthoyl)hydrazino]carbonyl]cyclopropanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(3-methoxybenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(3-methylbenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(4-methylbenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]cyclobutanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]cyclohexanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]cyclopentanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]cyclobutanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]cyclohexanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]cyclopentanecarboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-2-([2-[(3-methylphenyl)carbonyl]hydrazino]carbonyl)-2,3-dihydro-1H-indene-2-carboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-2-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]-2,3-dihydro-1H-indene-2-carboxamide
-
-
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-2-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]-2,3-dihydro-1H-indene-2-carboxamide
-
-
N-[(3S)-6-(hydroxymethyl)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
-
-
N-[(3S,5Z)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-1,2,3,4,7,8-hexahydroazocin-3-yl]isoquinoline-1-carboxamide
-
-
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]-1-benzothiophene-2-carboxamide
-
good selectivity against the related enzymes caspase-3 and caspase-8
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]benzamide
-
good selectivity against the related enzymes caspase-3 and caspase-8
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]isoquinoline-1-carboxamide
-
good selectivity against the related enzymes caspase-3 and caspase-8
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]naphthalene-2-carboxamide
-
good selectivity against the related enzymes caspase-3 and caspase-8
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]-1-benzothiophene-2-carboxamide
-
good selectivity against the related enzymes caspase-3 and caspase-8
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]-3-(trifluoromethyl)benzamide
-
good selectivity against the related enzymes caspase-3 and caspase-8
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]benzamide
-
good selectivity against the related enzymes caspase-3 and caspase-8
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]isoquinoline-1-carboxamide
-
good selectivity against the related enzymes caspase-3 and caspase-8
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]naphthalene-2-carboxamide
-
good selectivity against the related enzymes caspase-3 and caspase-8
N-[(benzyloxy)carbonyl]-alpha-glutamyl-N-[1-(carboxymethyl)-3-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-2-oxopropyl]-L-alaninamide
-
-
N-[(benzyloxy)carbonyl]valyl-N-[1-(carboxymethyl)-3-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-2-oxopropyl]-L-alaninamide
-
-
NCGC00183434
-
i.e. (S)-3-((S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)pyrrolidine-2-carboxamido)-3-cyanopropanoic acid, competitive inhibition
NCGC00183681
-
i.e. (S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((S)-1-cyano-2-(1H-tetrazol-5-yl)ethyl)pyrrolidine-2-carboxamide
NCGC00185682
-
i.e. 3-((S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)pyrrolidine-2-carboxamido)-3-cyanopropanoate
p35
IC50: 0.5 nM
-
pralnacasan
quercetin
-
-
ritonavir
secospiculisporic acid
-
-
-
serpin proteinase inhibitor 9
-
endogenous inhibitor of caspase-1 activity in human vascular smooth muscle cells
-
spiculisporic acid
-
-
superoxide
-
superoxide production decreases the cellular redox potential and specifically inhibites caspase-1 by reversible oxidation and glutathionylation of the redox-sensitive cysteine residues Cys397 and Cys362
tetracycline
-
-
Val-Ala-Asp
-
-
-
VRT-043198
-
-
YN-1234
-
i.e. N-2-naphthoyl-L-valyl-N-[(1S)-2-carboxy-1-formylethyl]-L-prolinamide
YVAD
-
-
YVAD-chloromethyl ketone
-
-
YVAD-chloromethylketone
-
-
Z-L-Tyr-L-Val-L-Ala-L-Asp-fluoromethylketone
-
specific inhibitor for caspase-1, complete inhibition at 0.05 mM
Z-L-Val-L-Ala-L-Asp-(O-methyl)-fluoromethylketone
-
-
Z-L-Val-L-Ala-L-Asp-fluoromethylketone
-
broad-spectrum caspase inhibitor
Z-Trp-Glu-His-Asp-fluoromethylketone
-
-
Z-Val-Ala-Asp-fluoromethylketone
Z-WEHD-fluoromethylketone
-
-
Z-YVAD-fluoromethylketone
-
-
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
adapter protein Asc
-
is important for caspase-1 activation during Legionella pneumophila infection, mechanism, overview. Activation of caspase-1 through Asc does not require the flagellin-sensing pathway involving the host nucleotide-binding domain and leucine-rich repeat-containing protein Ipaf, NLRC4. Asc-dependent caspase-1 activation is inhibited by high extracellular potassium levels
-
alendronate
-
a nitrogen-containing bisphosphonate, activates caspase-1, activation is inhibited by clodronate. Pretreatment of cells with alendronate augments interleukin-1beta production stimulated by Toll-like receptor ligands, augmentation is inhibited by clodronate
anthrax lethal toxin
-
rapidly activates caspase-1/interleukin-1beta-converting enzyme and induces extracellular release of interleukin-1beta and interleukin-18
-
cathepsin B
-
cathepsin B can effectively cleave and activate pro-caspase-1 in a cell-free system only at an acidic pH and in THP-1 monocytic cells after stimulation with the microbial toxin nigericin
-
chromogranin A
-
chromogranin A can activate pro-caspase-1 in microglia
-
Ipaf
-
i.e. host nucleotide-binding domain and leucine-rich repeatcontaining protein Ipaf or NLRC4, Ipaf-dependent activation is unaffected by potassium treatment
-
lipopolysaccharide
-
-
monosodium urate
-
-
-
Nalp1b
-
an inflammasome component is required for caspase-1 activation, Nalp1b is a member of the NOD-like receptor family, NLR, a family of cytoplasmic proteins involved in the recognition of microbial products or danger signals. Nalp1b has a caspase recruitment domain, CARD, that allows it to interact with caspase-1
-
NLRC4 inflammasome
-
-
-
NLRP1 inflammasome
-
-
-
NLRP3 inflammasome
-
-
-
NOD2
-
NOD2 through its N-terminal caspase recruitment domain directly binds and activates caspase-1 to trigger interleukin-1beta processing and secretion in muramyl dipeptide-stimulated macrophages, whereas the C-terminal leucine-rich repeats of NOD2 prevent caspase-1 activation in nonstimulated cells
-
poly(dA-dT)
-
-
-
protease activating factor
-
i.e. Ipaf. Cytoplasmic flagellin activates caspase-1 and secretion of interleukin 1beta via Ipaf
-
protease-activating factor
-
activates caspase 1 in p53-dependent apoptosis
-
simvastatin
-
blocks inhibition of caspase-1 activation, simvastatin acts synergistically with lipopolysaccharides and causes an impairment of non-sterol isoprenoid biosynthesis, the isoprenyl intermediate GGPP could block activation of caspase-1 and interleukin-1beta release, overview
thalidomide
-
thalidomide inhibits activation and activity of caspase-1 in cultured cells but not in vitro
Urate
-
-
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000134
4-[[4'-(dimethylamino)phenyl]azo]-benzoic acid-YVADAPV-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid
-
pH 7.5
0.045
acetyl-DQMD-4-nitroanilide
-
pH 7.5, 30C
0.0085 - 0.018
acetyl-LEVD-4-nitroanilide
0.046
acetyl-VEID-4-nitroanilide
-
pH 7.5, 30C
0.12
acetyl-VQVD-4-nitroanilide
-
pH 7.5, 30C
0.004
acetyl-WEHD-7-amido-4-methylcoumarin
-
pH 7.5
0.0073
acetyl-YEVD-4-nitroanilide
-
pH 7.5, 30C
0.105
acetyl-YEVDGW-amide
-
pH 7.5, 30C
0.023
acetyl-YVAD-4-nitroanilide
-
pH 7.5, 30C
0.0000115
acetyl-YVAD-7-amido-4-methylcoumarin
-
pH 7.5
0.000004
pro-interleukin-1beta
-
pH 7.5
-
0.0000215 - 0.006
succinyl-YVAD-4-nitroanilide
0.02
succinyl-YVAD-7-amido-4-methylcoumarin
-
pH 7.5, 37C
additional information
additional information
-
wild-type and mutant enzyme kinetics, caspase-1 shows positive cooperativity, a network of 21 hydrogen bonds from nine side chains connecting the active and allosteric sites change partners when going between the on-state and the off-state, an allosteric circuit promotes site-to-site coupling. Arg286 and Glu390, which form a salt bridge, have major effects, causing 100 to 200fold reductions in catalytic efficiency, kcat/Km. Two neighbors, Ser332 and Ser339, have minor effects, causing 4 to 7fold reductions, overview
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.41
4-[[4'-(dimethylamino)phenyl]azo]-benzoic acid-YVADAPV-5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid
Homo sapiens
-
pH 7.5
13
acetyl-WEHD-7-amido-4-methylcoumarin
Homo sapiens
-
pH 7.5
1
acetyl-YVAD-7-amido-4-methylcoumarin
Homo sapiens
-
pH 7.5
1.2
pro-interleukin-1beta
Homo sapiens
-
pH 7.5
-
1 - 1.6
succinyl-YVAD-4-nitroanilide
0.35
succinyl-YVAD-7-amido-4-methylcoumarin
Homo sapiens
-
pH 7.5, 37C
additional information
additional information
Homo sapiens
-
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000054
(3S)-3-((6-[((4-[(6-chloropyrazin-2-yl)amino]phenyl)carbonyl)amino]-2-thiophen-2-ylhexanoyl)amino)-4-oxobutanoic acid
-
-
0.000005
(3S)-3-((6-[((4-[(6-methylquinoxalin-2-yl)amino]phenyl)carbonyl)amino]-2-thiophen-2-ylhexanoyl)amino)-4-oxobutanoic acid
-
-
0.000008
(3S)-3-([2-(2-fluorophenyl)-6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)-4-oxobutanoic acid
-
-
0.000016
(3S)-3-([2-ethyl-6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)-4-oxobutanoic acid
-
-
0.000004
(3S)-3-([6-(([3-methyl-4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)-2-thiophen-2-ylhexanoyl]amino)-4-oxobutanoic acid
-
-
0.000005
(3S)-4-oxo-3-([2-phenyl-6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
0.0052
(3S)-4-oxo-3-([4-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)butanoyl]amino)butanoic acid
-
-
0.0028
(3S)-4-oxo-3-([5-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)pentanoyl]amino)butanoic acid
-
-
0.0001
(3S)-4-oxo-3-([6-(([4-(pyrazin-2-ylamino)phenyl]carbonyl)amino)-2-thiophen-2-ylhexanoyl]amino)butanoic acid
-
-
0.037
(3S)-4-oxo-3-([6-(([4-(pyrazin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
0.00019
(3S)-4-oxo-3-([6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
0.000043 - 0.00032
(3S)-4-oxo-3-([6-(([4-(quinoxalin-2-yloxy)phenyl]carbonyl)amino)-2-thiophen-2-ylhexanoyl]amino)butanoic acid
0.0024
(3S)-4-oxo-3-([6-(([4-(quinoxalin-2-yloxy)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
0.000005 - 0.0026
(3S)-4-oxo-3-([7-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)heptanoyl]amino)butanoic acid
0.0001
(3S)-4-oxo-3-[((4-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]phenyl)carbonyl)amino]butanoic acid
-
-
0.00026
(3S)-4-oxo-3-[((4-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-2-yl)carbonyl)amino]butanoic acid
-
-
0.001
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]-2,3-dihydropyrazin-2-yl)carbonyl)amino]butanoic acid
-
-
0.0021
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]furan-2-yl)carbonyl)amino]butanoic acid
-
-
0.00012
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-2-yl)acetyl)amino]butanoic acid
-
-
0.000035
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-2-yl)carbonyl)amino]butanoic acid
-
-
0.00012
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-3-yl)carbonyl)amino]butanoic acid
-
-
0.000005
(3S)-4-oxo-3-[((6-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]pyridin-3-yl)carbonyl)amino]butanoic acid
-
-
0.00195
(3S)-4-oxo-3-[((trans-4-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]cyclohexyl)carbonyl)amino]butanoic acid
-
-
0.0021
(3S)-4-oxo-3-[(7-oxo-7-([4-(quinoxalin-2-ylamino)phenyl]amino)heptanoyl)amino]butanoic acid
-
-
0.0072
(S)-2-(4'-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
0.000047
(S)-3-((S)-2-((S)-2-(2-naphthamido)-3-methylbutanamido)-propanamido)-4-(2-hydroxy)benzylaminobutanoic acid
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.0068
(S)-3-(2'-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
0.0069
(S)-3-(2-naphthalen-1-yl-benzenesulfonylamino)-4-oxo-butyric acid
-
-
0.0023
(S)-3-(3'-acetylamino-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
0.0031
(S)-3-(3'-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
0.0019
(S)-3-(6-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
0.0016
(S)-3-(biphenyl-2-sulfonylamino)-4-oxobutyric acid
-
-
0.024
(S)-3-benzenesulfonylamino-4-oxo-5-(3-phenyl-propylsulfanyl)-pentanoic acid
0.025
(S)-3-benzyloxycarbonylamino-4-oxo-5-(3-phenyl-propylsulfanyl)-pentanoic acid
-
-
0.119
(S)-3-benzyloxycarbonylamino-4-oxo-9-phenyl-nonanoic acid
-
-
0.0094
(S)-3-benzynesulfonylamino-4-oxo-butyric acid
-
-
0.119
3-([(benzyloxy)carbonyl]amino)-4-oxo-9-phenylnonanoic acid
-
-
0.065
3-([(benzyloxy)carbonyl]amino)-5-([(2,3-dihydro-1H-inden-1-ylmethyl)(dihydroxy)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.016
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(2-naphthalen-1-ylethyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.011
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.0345
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(3-phenylpropyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.022
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(naphthalen-1-yl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.037
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(phenyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.033
3-[[(benzyloxy)carbonyl]amino]-5-[[(2-cyclohexylethyl)sulfonyl]amino]-4-oxopentanoic acid
-
-
0.018
5-([benzyl(dihydroxy)-lambda4-sulfanyl]amino)-3-([(benzyloxy)carbonyl]amino)-4-oxopentanoic acid
-
-
0.083
acetyl-Ala-Pro-Nle-Asp-aldehyde
-
pH 7.5
0.000015 - 0.000018
acetyl-DEVD-aldehyde
0.00002
acetyl-DEVS-aldehyde
-
pH 7.5, 37C
0.000011
acetyl-Tyr-Val-Ala-Asp-CO-(CH2)5-Ph
-
pH 7.5
0.000000056
acetyl-WEHD-aldehyde
-
pH 7.5, 25C
0.00000076 - 0.000006
acetyl-YVAD-aldehyde
0.03
benzyloxycarbonyl-Pro-Nle-Asp-aldehyde
-
pH 7.5
-
0.000008
benzyloxycarbonyl-VAD-CHO
-
-
0.00000001
cowpox serpin CrmA
-
pH 7.5, 25C
-
0.00036
Glu-Val-Asp-aldehyde
-
pH 7.5
0.3
kaempferol
-
pH not specified in the publication, 30C, value above
0.118
luteolin
-
pH not specified in the publication, 30C
0.014
myricetin
-
pH not specified in the publication, 30C
0.05
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2R)-1-carboxy-5-phenylpentan-2-yl]-L-alaninamide
-
IC50 above 0.05 mM, in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.0006
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-(benzylamino)-3-carboxypropan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.000945
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-(cyclohexylamino)propan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.0012
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[(2-fluorobenzyl)amino]propan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.000965
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[(2-methoxybenzyl)amino]propan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.00137
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[(4-hydroxybenzyl)amino]propan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.000128
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[methyl(phenyl)amino]propan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.00029
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-[(1,3-benzodioxol-5-ylmethyl)amino]-3-carboxypropan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.00182
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-[(4-carbamoylbenzyl)amino]-3-carboxypropan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.00189
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-[benzyl(methyl)amino]-3-carboxypropan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30C
0.000004
N-([4-(quinoxalin-2-ylamino)phenyl]carbonyl)-L-valyl-N-[(1S)-2-carboxy-1-formylethyl]-L-alaninamide
0.000014
N-acetyl-L-tyrosylvalyl-N-[1-(carboxymethyl)-2-oxo-7-phenylheptyl]-L-alaninamide
-
-
0.0000239
N-[(benzyloxy)carbonyl]-alpha-glutamyl-N-[1-(carboxymethyl)-3-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-2-oxopropyl]-L-alaninamide
-
-
0.000004
N-[(benzyloxy)carbonyl]valyl-N-[1-(carboxymethyl)-3-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-2-oxopropyl]-L-alaninamide
-
-
0.0000004
NCGC00183434
-
in 50 mM HEPES, pH 7.4, containing 1 M sodium citrate, 100 mM NaCl, 0.1 mM EDTA, 10 mM dithiothreitol, 0.01% (v/v) CHAPS, 1% (v/v) DMSO, and 0.1 mg/ml bovine serum albumin
0.3
quercetin
-
pH not specified in the publication, 30C, value above
additional information
additional information
-
the Ki-value for acetyl-IETD-aldehyde is below 6 nM and the Ki-value for acetyl-AEVD-aldehyde is below 12 nM
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000036
(1S,9S)-N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-9-[(isoquinolin-1-ylcarbonyl)amino]-6,10-dioxooctahydro-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxamide
Homo sapiens
-
good selectivity against the related enzymes caspase-3 and caspase-8
0.000004
(3S)-3-[([(1S,9S)-9-[(isoquinolin-1-ylcarbonyl)amino]-6,10-dioxooctahydro-6H-pyridazino[1,2-a][1,2]diazepin-1-yl]carbonyl)amino]-4-oxobutanoic acid
0.000003
(3S)-3-[([(4S,7S,10aS)-7-[(isoquinolin-1-ylcarbonyl)amino]-6-oxo-3,4,6,7,10,10a-hexahydro-1H-[1,4]oxazino[4,3-a]azepin-4-yl]carbonyl)amino]-4-oxobutanoic acid
Homo sapiens
-
-
0.0007
1-([2-[(2,6-dimethoxyphenyl)carbonyl]hydrazino]carbonyl)-N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000007 - 0.000015
2,5-dichloro-N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]benzamide
0.000008 - 0.000029
3-chloro-N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]benzamide
0.000015
acetyl-L-Leu-L-Glu-L-His-L-Asp-CHO
Homo sapiens
-
in 50 mM HEPES, pH 7.4, containing 1 M sodium citrate, 100 mM NaCl, 0.1 mM EDTA, 10 mM dithiothreitol, 0.01% (v/v) CHAPS, 1% (v/v) DMSO, and 0.1 mg/ml bovine serum albumin
0.1
berkedrimane A
Homo sapiens
-
at 37C, pH not specified in the publication
-
0.09
berkedrimane B
Homo sapiens
-
at 37C, pH not specified in the publication
-
0.00001
L-Tyr-L-Val-L-Ala-L-Asp-CHO
Homo sapiens
-
-
0.0000216
L-Tyr-L-Val-L-Ala-L-Asp-CN
Homo sapiens
-
in 50 mM HEPES, pH 7.4, containing 1 M sodium citrate, 100 mM NaCl, 0.1 mM EDTA, 10 mM dithiothreitol, 0.01% (v/v) CHAPS, 1% (v/v) DMSO, and 0.1 mg/ml bovine serum albumin
0.000001
N-((S,Z)-1-((R)-1-((3S)-2-hydroxy-5-oxo-tetrahydrofuran-3-ylamino)-1-oxopropan-2-yl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl)-2-naphthamide
Homo sapiens
-
-
0.000013
N-((S,Z)-1-((S)-1-((3S)-2-hydroxy-5-oxo-tetrahydrofuran-3-ylamino)-1-oxopropan-2-yl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl)-2-naphthamide
Homo sapiens
-
-
0.00002
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]-1-benzothiophene-2-carboxamide
Homo sapiens
-
-
0.000011
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]-3-(trifluoromethyl)benzamide
Homo sapiens
-
-
0.000053
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]-3-methoxybenzamide
Homo sapiens
-
-
0.000168
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]benzamide
Homo sapiens
-
-
0.000027
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]isoquinoline-1-carboxamide
Homo sapiens
-
-
0.000014
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
Homo sapiens
-
-
0.000002
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-6-[[(phenylcarbonyl)amino]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
Homo sapiens
-
-
0.000003
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-6-[[(phenylsulfonyl)amino]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
Homo sapiens
-
-
0.000002
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-([[(2-methoxyphenyl)carbonyl]amino]methyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
Homo sapiens
-
-
0.000001
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-([[(3-methoxyphenyl)carbonyl]amino]methyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
0.000019
N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-methyl-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
Homo sapiens
-
-
0.00024
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methoxyphenyl)carbonyl]hydrazino]carbonyl)cyclohexanecarboxamide
Homo sapiens
-
-
0.0002
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methoxyphenyl)carbonyl]hydrazino]carbonyl)cyclopentanecarboxamide
Homo sapiens
-
-
0.00043
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methylphenyl)carbonyl]hydrazino]carbonyl)cyclohexanecarboxamide
Homo sapiens
-
-
0.00049
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methylphenyl)carbonyl]hydrazino]carbonyl)cyclopentanecarboxamide
Homo sapiens
-
-
0.00031
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(2-methylbenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide
Homo sapiens
-
-
0.0029
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(2-naphthoyl)hydrazino]carbonyl]cyclopropanecarboxamide
Homo sapiens
-
-
0.00026
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(3-methoxybenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide
Homo sapiens
-
-
0.00015
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(3-methylbenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide
Homo sapiens
-
-
0.00058
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(4-methylbenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide
Homo sapiens
-
-
0.00005
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]cyclobutanecarboxamide
0.0004
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]cyclopentanecarboxamide
Homo sapiens
-
-
0.00024
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]cyclobutanecarboxamide
Homo sapiens
-
-
0.00009
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.00015
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]cyclopentanecarboxamide
Homo sapiens
-
-
0.00043
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-2-([2-[(3-methylphenyl)carbonyl]hydrazino]carbonyl)-2,3-dihydro-1H-indene-2-carboxamide
Homo sapiens
-
-
0.00004
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-2-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]-2,3-dihydro-1H-indene-2-carboxamide
Homo sapiens
-
-
0.00003
N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-2-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]-2,3-dihydro-1H-indene-2-carboxamide
Homo sapiens
-
-
0.000022
N-[(3S)-6-(hydroxymethyl)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide
Homo sapiens
-
-
0.000077
N-[(3S,5Z)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-1,2,3,4,7,8-hexahydroazocin-3-yl]isoquinoline-1-carboxamide
Homo sapiens
-
-
0.00032
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]-1-benzothiophene-2-carboxamide
Homo sapiens
-
good selectivity against the related enzymes caspase-3 and caspase-8
0.0023
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]benzamide
Homo sapiens
-
good selectivity against the related enzymes caspase-3 and caspase-8
0.00013
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]isoquinoline-1-carboxamide
Homo sapiens
-
good selectivity against the related enzymes caspase-3 and caspase-8
0.00015
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]naphthalene-2-carboxamide
Homo sapiens
-
good selectivity against the related enzymes caspase-3 and caspase-8
0.00008
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]-1-benzothiophene-2-carboxamide
Homo sapiens
-
good selectivity against the related enzymes caspase-3 and caspase-8
9
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]-3-(trifluoromethyl)benzamide
Homo sapiens
-
good selectivity against the related enzymes caspase-3 and caspase-8
0.00035
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]benzamide
Homo sapiens
-
good selectivity against the related enzymes caspase-3 and caspase-8
0.00007
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]isoquinoline-1-carboxamide
Homo sapiens
-
good selectivity against the related enzymes caspase-3 and caspase-8
0.00003
N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]naphthalene-2-carboxamide
Homo sapiens
-
good selectivity against the related enzymes caspase-3 and caspase-8
0.000000023
NCGC00183434
Homo sapiens
-
in 50 mM HEPES, pH 7.4, containing 1 M sodium citrate, 100 mM NaCl, 0.1 mM EDTA, 10 mM dithiothreitol, 0.01% (v/v) CHAPS, 1% (v/v) DMSO, and 0.1 mg/ml bovine serum albumin
0.00000258
NCGC00183681
Homo sapiens
-
in 50 mM HEPES, pH 7.4, containing 1 M sodium citrate, 100 mM NaCl, 0.1 mM EDTA, 10 mM dithiothreitol, 0.01% (v/v) CHAPS, 1% (v/v) DMSO, and 0.1 mg/ml bovine serum albumin
0.0000434
NCGC00185682
Homo sapiens
-
in 50 mM HEPES, pH 7.4, containing 1 M sodium citrate, 100 mM NaCl, 0.1 mM EDTA, 10 mM dithiothreitol, 0.01% (v/v) CHAPS, 1% (v/v) DMSO, and 0.1 mg/ml bovine serum albumin
0.0000005
p35
Spodoptera frugiperda
P89116
IC50: 0.5 nM
-
0.0000036
pralnacasan
Homo sapiens
-
-
0.000000204
VRT-043198
Homo sapiens
-
in 50 mM HEPES, pH 7.4, containing 1 M sodium citrate, 100 mM NaCl, 0.1 mM EDTA, 10 mM dithiothreitol, 0.01% (v/v) CHAPS, 1% (v/v) DMSO, and 0.1 mg/ml bovine serum albumin
0.000024
YN-1234
Homo sapiens
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
-
assay at
8
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
30
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
increased enzyme content during pregnancy, women with spontaneous labor at term have a higher median caspase-1 amniotic fluid concentration than women at term without labor
Manually annotated by BRENDA team
-
functional role for caspase-1-mediated myocardial apoptosis contributing to the progression of heart failure
Manually annotated by BRENDA team
-
from peripheral blood
Manually annotated by BRENDA team
-
high activity. Bacterial infection leads to a decrease in the mRNA levels of caspase-1
Manually annotated by BRENDA team
of feeding and wandering larvae. Expression of Hearm caspase-1 in the haemocytes appears to be correlated with the pulse of ecdysone, and it is up-regulated by ecdysone agonist RH-2485, implying that Hearm caspase-1 activation is regulated by ecdysone
Manually annotated by BRENDA team
-
macrophage-like cells
Manually annotated by BRENDA team
-
caspase-1 gene is expressed in 1 day post-hatching larvae and its mRNA levels increases throughout development
Manually annotated by BRENDA team
-
primary leukocyte
Manually annotated by BRENDA team
-
high activity in from peripheral blood of mevalonate kinase deficiency patients
Manually annotated by BRENDA team
-
caspase-1 activity is required for neuronal differentiation of PC12 cells
Manually annotated by BRENDA team
-
bacterial infection leads to a decrease in the mRNA levels of caspase-1
Manually annotated by BRENDA team
-
fibrobalst cell
Manually annotated by BRENDA team
-
caspase-1 is increased in lesional psoriatic skin capared with non-lesional psoriatic skin
Manually annotated by BRENDA team
low activity
Manually annotated by BRENDA team
-
high activity. Bacterial infection leads to a decrease in the mRNA levels of caspase-1
Manually annotated by BRENDA team
additional information