Information on EC 3.4.22.56 - caspase-3

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
3.4.22.56
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RECOMMENDED NAME
GeneOntology No.
caspase-3
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REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
strict requirement for an Asp residue at positions P1 and P4. It has a preferred cleavage sequence of Asp-Xaa-Xaa-Asp-/- with a hydrophobic amino-acid residue at P2 and a hydrophilic amino-acid residue at P3, although Val or Ala are also accepted at this position
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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CAS REGISTRY NUMBER
COMMENTARY hide
169592-56-7
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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Manually annotated by BRENDA team
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Manually annotated by BRENDA team
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SwissProt
Manually annotated by BRENDA team
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UniProt
Manually annotated by BRENDA team
Balb/c mice
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Manually annotated by BRENDA team
strain C3H/An
SwissProt
Manually annotated by BRENDA team
C57B1/6
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Manually annotated by BRENDA team
C57BL/6 mice
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Manually annotated by BRENDA team
C57Bl6 mice
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Manually annotated by BRENDA team
HL-1 mice
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Manually annotated by BRENDA team
cultivar Pampeana INTA
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Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
19 S proteasome + H2O
?
show the reaction diagram
5'-tetramethylrhodamine-5(6)-carboxamide-DEVD-cyanine 5 + H2O
?
show the reaction diagram
-
-
-
-
?
70kDa U1 small ribonucleoprotein + H2O
?
show the reaction diagram
-
cleavage site is DGPD-/-
-
-
?
Ac-DEVD-4-methylcoumarin 7-amide + H2O
Ac-DEVD + 7-amino-4-methylcoumarin
show the reaction diagram
-
an artificial caspase-3 substrate
-
-
?
Ac-DEVD-4-nitroanilide + H2O
Ac-DEVD + 4-nitroaniline
show the reaction diagram
Ac-DEVD-7-amido-4-methylcoumarin + H2O
Ac-DEVD + 7-amino-4-methylcoumarin
show the reaction diagram
Ac-IETD-4-nitroanilide + H2O
Ac-IETD + 4-nitroaniline
show the reaction diagram
an artificial caspase-8 substrate, low activity
-
-
?
Ac-LEHD-4-nitroanilide + H2O
Ac-LEHD + 4-nitroaniline
show the reaction diagram
an artificial caspase-9 substrate, low activity
-
-
?
acetyl-Asp-Glu-Val-Asp-4-nitroanilide + H2O
acetyl-Asp-Glu-Val-Asp + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-Asp-Glu-Val-Asp-7-amido-4-trifluoromethylcoumarin + H2O
acetyl-Asp-Glu-Val-Asp + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
acetyl-Asp-Glu-Val-Asp-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
acetyl-Asp-Glu-Val-Asp-p-nitroanilide + H2O
acetyl-Asp-Glu-Val-Asp + p-nitroaniline
show the reaction diagram
acetyl-CDEVDK + H2O
acetyl-CDEVD + Lys
show the reaction diagram
-
-
-
-
?
acetyl-DEVD-4-methylcoumarin-7-amide + H2O
acetyl-DEVD + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
acetyl-DEVD-4-nitroanilide + H2O
acetyl-DEVD + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-DEVD-4-trifluoromethylcoumarin-7-amide + H2O
?
show the reaction diagram
-
-
-
-
?
acetyl-DEVD-7-amido-4-methylcoumarin + H2O
acetyl-DEVD + 7-amino-4-methylcoumarin
show the reaction diagram
acetyl-DQMD-4-nitroanilide + H2O
acetyl-DQMD + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-IETD-7-amido-4-methylcoumarin + H2O
acetyl-IETD + 7-amino-4-methylcoumarin
show the reaction diagram
-
low activity towards the caspase-6 and caspase-8 substrate
-
-
?
acetyl-L-Asp-L-Glu-L-Val-L-Asp-4-nitroanilide + H2O
acetyl-L-Asp-L-Glu-L-Val-L-Asp + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-L-Asp-L-Glu-L-Val-L-Asp-7-amido-4-methylcoumarin + H2O
acetyl-L-Asp-L-Glu-L-Val-L-Asp + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
acetyl-L-Asp-L-Met-L-Gln-L-Asp-4-nitroanilide + H2O
acetyl-L-Asp-L-Met-L-Gln-L-Asp + 4-nitroaniline
show the reaction diagram
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-
-
-
?
acetyl-L-Asp-L-Val-L-Ala-L-Asp-4-nitroanilide + H2O
acetyl-L-Asp-L-Val-L-Ala-L-Asp + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
acetyl-L-Leu-L-Asp-L-Val-L-Ala-L-Asp-4-nitroanilide + H2O
acetyl-L-Leu-L-Asp-L-Val-L-Ala-L-Asp + 4-nitroaniline
show the reaction diagram
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-
-
-
?
acetyl-L-Val-L-Asp-L-Val-L-Ala-L-Asp-4-nitroanilide + H2O
acetyl-L-Val-L-Asp-L-Val-L-Ala-L-Asp + 4-nitroaniline
show the reaction diagram
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-
-
-
?
acetyl-LEHD-4-methylcoumarin-7-amide + H2O
acetyl-LEHD + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
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?
acetyl-LEHD-7-amido-4-methylcoumarin + H2O
acetyl-LEHD + 7-amino-4-methylcoumarin
show the reaction diagram
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low activity towards the caspase-9 substrate
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?
acetyl-VDQMDGW-amide + H2O
?
show the reaction diagram
acetyl-VDQQD-4-nitroanilide + H2O
acetyl-VDQQD + 4-nitroaniline
show the reaction diagram
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-
-
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?
acetyl-VDVAD-4-nitroanilide + H2O
acetyl-VAVAD + 4-nitroaniline
show the reaction diagram
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-
-
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?
acetyl-VEID-4-methylcoumarin-7-amide + H2O
acetyl-VEID + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
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?
acetyl-VEID-4-nitroanilide + H2O
acetyl-VEID + 4-nitroaniline
show the reaction diagram
-
-
-
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?
acetyl-VQVD-4-nitroanilide + H2O
acetyl-VQVD + 4-nitroaniline
show the reaction diagram
-
-
-
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?
acetyl-YEVD-4-nitroanilide + H2O
acetyl-YEVD + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
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
-
low activity towards the caspase-1 substrate
-
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?
alpha-spectrin + H2O
?
show the reaction diagram
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production of a 120 kDa fragment
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?
anamorsin + H2O
?
show the reaction diagram
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specifically cleaved by caspase-3 at DSVD209 L generating 25- and 10-kDa fragments
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?
Asp-Glu-Val-Asp-4-nitroanilide + H2O
Asp-Glu-Val-Asp + 4-nitroaniline
show the reaction diagram
benzoyl-L-Asp-L-Glu-L-Val-L-Asp-7-amido-4-methylcoumarin + H2O
benzoyl-L-Asp-L-Glu-L-Val-L-Asp + 7-amino-4-methylcoumarin
show the reaction diagram
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-
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?
benzyloxycarbonyl-DEVD-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-DEVD + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
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?
beta-catenin + H2O
?
show the reaction diagram
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processing of beta-catenin, production of a 70000 Da fragment
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?
beta-N-acetylglucosaminidase + H2O
?
show the reaction diagram
Bid peptide + H2O
?
show the reaction diagram
biotinylated acetyl-CDEVDK + H2O
biotinylated acetyl-CDEVD + Lys
show the reaction diagram
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-
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-
?
caspase 9 + H2O
?
show the reaction diagram
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cleavage by caspase 3 does not result in activation of caspase 9, but enhances apoptosis by alleviating XIAP inhibition of the apical caspase
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?
cytokeratine 18 + H2O
?
show the reaction diagram
D4 G-protein dissociation inhibitor + H2O
?
show the reaction diagram
-
cleavage site is DELD-/-
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?
D4-GDI(Rho-GDI 2) + H2O
?
show the reaction diagram
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differential regulation of the homologous GDP dissociation inhibitors Rho-GDI 1 and D4-GDI during drug-induced apoptosis by proteolysis mediated by caspase-3
-
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?
DEVD-4-nitroanilide + H2O
DEVD + 4-nitroaniline
show the reaction diagram
DEVD-7-amido-4-fluoromethylcoumarin + H2O
DEVD + 7-amino-4-fluoromethylcoumarin
show the reaction diagram
DEVD-7-amido-4-methylcoumarin + H2O
DEVD + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
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?
DEVD-7-amido-4-trifluoromethylcoumarin + H2O
DEVD + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
DEVD-FQ + H2O
N2-acetyl-L-lysyl-L-lysyl-L-lysyl-L-arginyl-L-lysyl-L-valyl-beta-alanyl-N6-[[1-([2-[(3E)-3-(2,3-dihydro-1H-indolium-1-ylidene)-6-(2,3-dihydro-1H-indol-1-yl)-3H-xanthen-9-yl]phenyl]sulfonyl)piperidin-4-yl]carbonyl]-L-lysyl-N-[(2R)-2-(carboxymethyl)-3-[[(2S)-1-[[(1S)-1,2-dicarboxyethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-oxopropyl]-D-phenylalaninamide + L-alanyl-N-[2-[(6-[3,3-dimethyl-2-[(1E,3E,5E)-5-(1,3,3-trimethyl-1,3-dihydro-2H-indol-2-ylidene)penta-1,3-dien-1-yl]-3H-indolium-1-yl]hexanoyl)amino]ethyl]-L-prolinamide
show the reaction diagram
-
highly selective substrate for caspase-3
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?
DEVD-NucView488 + H2O
?
show the reaction diagram
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the highly cell-permeable caspase-3 substrate is obtained by linking a fluorogenic DNA-binding dye to the caspase-3 recognition sequence that renders the dye nonfunctional. On substrate cleavage, the dye is released and becomes highly fluorescent on binding to DNA. DEVD-NucView488 detects caspase-3 activation within a live-cell population much earlier and with higher sensitivity compared with other apoptosis reagents. Cells incubated with DEVD-NucView488 exhibit no toxicity and normal apoptotic progression. DEVD-NucView488 is an ideal substrate for kinetic studies of caspase-3 activation because it detects caspase-3 activity in real-time and also efficiently labels DNA in nuclei of caspase-3-activated cells for real-time fluorescent visualization of apoptotic morphology
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?
DNA-dependent protein kinase CS + H2O
?
show the reaction diagram
-
cleavage site is DEVD-/-
-
-
?
DW3-FQ + H2O
N2-acetyl-L-lysyl-L-lysyl-L-lysyl-L-arginyl-L-lysyl-L-valyl-beta-alanyl-N6-[[1-([2-[(3E)-3-(2,3-dihydro-1H-indolium-1-ylidene)-6-(2,3-dihydro-1H-indol-1-yl)-3H-xanthen-9-yl]phenyl]sulfonyl)piperidin-4-yl]carbonyl]-L-lysyl-N-[(2R)-2-(carboxymethyl)-3-[[(3S)-1-[[(2S)-1-[[(1S)-1,2-dicarboxyethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-methyl-1-oxohexan-3-yl]amino]-3-oxopropyl]-D-phenylalaninamide + L-alanyl-N-[2-[(6-[3,3-dimethyl-2-[(1E,3E,5E)-5-(1,3,3-trimethyl-1,3-dihydro-2H-indol-2-ylidene)penta-1,3-dien-1-yl]-3H-indolium-1-yl]hexanoyl)amino]ethyl]-L-prolinamide
show the reaction diagram
-
-
-
-
?
eIF4G + H2O
?
show the reaction diagram
epidermal growth factor receptor + H2O
?
show the reaction diagram
glutaredoxin-1 + H2O
?
show the reaction diagram
-
murine or human protein substrate, the putative cleavage site of caspase-3, amino acids 56-59 EFVD and 56-59 AIQD, which has predicted affiffinity toward glutamic and aspartic acid residues
cleavage produces a 8 kDA fragment
-
?
huntingtin + H2O
?
show the reaction diagram
ICAD + H2O
?
show the reaction diagram
IETD-4-nitroanilide + H2O
IETD + 4-nitroaniline
show the reaction diagram
IETD-7-amido-4-fluoromethylcoumarin + H2O
IETD + 7-amino-4-fluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
Ile-Glu-Thr-Asp-4-nitroanilide + H2O
Ile-Glu-Thr-Asp + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
LLVY-4-methylcoumarin 7-amide + H2O
LLVY + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
mammalian sterile 20-like kinase 1 + H2O
?
show the reaction diagram
Mcl-1 + H2O
?
show the reaction diagram
MDM2 oncoprotein + H2O
?
show the reaction diagram
myeloid cell leukemia 1 + H2O
?
show the reaction diagram
-
i.e. Mcl-1, apoptosis induced by tumor necrosis factor-related apoptosis-inducing ligand requires specific cleavage of Mcl-1 at D127 and D157 by enzyme. Removal of N-terminal domain of Mcl-1 by enzyme allows for the maximal mitochondrial perturbation that potentiates apoptosis
-
-
?
N-acetyl-Asp-Glu-Val-Asp 4-nitroanilide + 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-Asp-Glu-Val-Asp-7-amido-4-trifluoromethylcoumarin + H2O
N-acetyl-Asp-Glu-Val-Asp + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
N-acetyl-DEVD-4-trifluoromethylcoumarin 7-amide + H2O
N-acetyl-DEVD + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
N-acetyl-DEVD-7-amido-4-fluoromethylcoumarin + H2O
N-acetyl-DEVD + 7-amino-4-fluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
N-acetyl-DEVD-7-amido-4-methylcoumarin + H2O
N-acetyl-DEVD + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-acetyl-DEVD-N'-morpholinecarbonyl-rhodamine 110 + H2O
?
show the reaction diagram
-
-
-
-
?
N-acetyl-L-Asp-L-Glu-L-Val-L-Asp-N'-morpholinecarbonyl-rhodamine 110 + H2O
?
show the reaction diagram
-
cell-permeable substrate, high turnover rate and sensitivity both in enzyme solution and in living cells
-
-
?
N-acetyl-LDEVD-7-amido-4-methylcoumarin + H2O
N-acetyl-LDEVD + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-carbobenzyloxy-DEVD-R110 + H2O
?
show the reaction diagram
-
a fluorescent substrate
-
-
?
nuclear mitotic apparatus protein + H2O
?
show the reaction diagram
p65/RelA + H2O
?
show the reaction diagram
PAK2 + H2O
?
show the reaction diagram
-
caspase-3 is mainly responsible for the apoptotic cleavage of PAK2 in Fas-stimulated Jurkat cells
-
-
?
poly(ADP-ribose) polymerase + H2O
85000 Da fragment + ?
show the reaction diagram
poly(ADP-ribose) polymerase + H2O
?
show the reaction diagram
pre-interleukin-18 + H2O
interleukin-18 + ?
show the reaction diagram
-
-
-
-
?
pro-caspase-6 + H2O
?
show the reaction diagram
-
caspase-8 activates caspase-3, and caspase-3 in turn activates caspase-6. Caspase 3 has a major role in nuclear apoptosis
-
-
?
pro-interleukin-18 + H2O
IL18 + ?
show the reaction diagram
-
virus infection by influenzy A or Sendai virus induces proteolytic processing of IL-18 in human macrophages via caspase-1 and caspase-3 activation
-
-
?
pro-Mch2alpha + H2O
?
show the reaction diagram
pro-Mch6 + H2O
?
show the reaction diagram
procaspase-3 + H2O
caspase-3 + ?
show the reaction diagram
procaspase-6 + H2O
caspase-6 + ?
show the reaction diagram
protein kinase Cdelta + H2O
?
show the reaction diagram
protein kinase Czeta + H2O
?
show the reaction diagram
protein phosphatase-1 inhibitor-3 + H2O
?
show the reaction diagram
RelB + H2O
?
show the reaction diagram
-
the Asp205 site in RelB is specifically cleaved by caspase-3 in vinblastine-treated HAT-1080 cells
-
-
?
RFC140 + H2O
?
show the reaction diagram
Rho-GDI 1 + H2O
?
show the reaction diagram
-
differential regulation of the homologous GDP dissociation inhibitors Rho-GDI 1 and D4-GDI during drug-induced apoptosis by proteolysis mediated by caspase-3
-
-
?
Rpt2 + H2O
?
show the reaction diagram
-
-
-
-
?
Rpt5 + H2O
?
show the reaction diagram
Rpt6 + H2O
?
show the reaction diagram
-
-
-
-
?
SETbeta + H2O
?
show the reaction diagram
-
-
-
-
?
sterol regulatory element-binding protein + H2O
?
show the reaction diagram
-
cleavage site is DEPD-/-
-
-
?
topoisomerase I + H2O
?
show the reaction diagram
-
cleavage at DDVD146-/-Y and EEED170-/-G
-
-
?
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
19 S proteasome + H2O
?
show the reaction diagram
-
caspase-3 specifically cleaves the 19 S component of 26 S proteasome Rpt2, Rpt6, and Rpn2 in skeletal muscle stimulating proteasome activity
-
-
?
anamorsin + H2O
?
show the reaction diagram
-
specifically cleaved by caspase-3 at DSVD209 L generating 25- and 10-kDa fragments
-
-
?
beta-catenin + H2O
?
show the reaction diagram
-
processing of beta-catenin, production of a 70000 Da fragment
-
-
?
beta-N-acetylglucosaminidase + H2O
?
show the reaction diagram
-
cleavage during apoptosis into two fragments during apoptosis, an N-terminal fragment containing the O-GlcNAcase active site and a C-terminal fragment containing a region with homology to GCN5 histone acetyltransferases, mutation D413A abrogates cleavage by caspase-3 both in vitro and in vivo. O-GlcNAcase activity is not affected by caspase-3 cleavage because the N- and C-terminal O-GlcNAcase fragments remain associated after the cleavage
-
-
?
Bid peptide + H2O
?
show the reaction diagram
caspase 9 + H2O
?
show the reaction diagram
-
cleavage by caspase 3 does not result in activation of caspase 9, but enhances apoptosis by alleviating XIAP inhibition of the apical caspase
-
-
?
cytokeratine 18 + H2O
?
show the reaction diagram
-
caspase-induced cytokeratine 18 cleavage in apoptotic cell populations
-
-
?
D4-GDI(Rho-GDI 2) + H2O
?
show the reaction diagram
-
differential regulation of the homologous GDP dissociation inhibitors Rho-GDI 1 and D4-GDI during drug-induced apoptosis by proteolysis mediated by caspase-3
-
-
?
eIF4G + H2O
?
show the reaction diagram
-
caspase 3 is capable of cleaving eIF4G as part of the translationally active complex eIF4F, thereby inactivating this complex and subsequently causing inhibition of translation in apoptotic cells
-
-
?
epidermal growth factor receptor + H2O
?
show the reaction diagram
-
cleavage during apoptosis
-
-
?
ICAD + H2O
?
show the reaction diagram
-
activity of caspase-activated deoxyribonuclease, CAD, is affected by the caspase 3-mediated cleavage of the CAD inhibitor, ICAD
-
-
?
mammalian sterile 20-like kinase 1 + H2O
?
show the reaction diagram
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i.e. Mst1. Caspase 3 preferentially activates extracellular signal-regulated kinase preferentially through 36000 Da cleaved forms of Mst1. The 36000 Da form of Mst1 selectively phosphorylates extracellular signal-regulated kinase
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-
?
Mcl-1 + H2O
?
show the reaction diagram
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antiapoptotic protein. Caspase-3 -mediated Mcl-1 downregulation appears to be responsible for the pro-apoptotic effects of EXEL-0862 on FIP1L1-PDGFRalpha-expressing cells
-
-
?
MDM2 oncoprotein + H2O
?
show the reaction diagram
-
because MDM2 functions as a negative regulator of the p53 tumor suppressor and because p53 induces apoptosis in response to a variety of stimuli, this cleavage of MDM2 by CPP32-like proteases may result in deregulation of p53 and contribute directly to the process of apoptotic cell death
-
-
?
myeloid cell leukemia 1 + H2O
?
show the reaction diagram
-
i.e. Mcl-1, apoptosis induced by tumor necrosis factor-related apoptosis-inducing ligand requires specific cleavage of Mcl-1 at D127 and D157 by enzyme. Removal of N-terminal domain of Mcl-1 by enzyme allows for the maximal mitochondrial perturbation that potentiates apoptosis
-
-
?
N-acetyl-DEVD-7-amido-4-methylcoumarin + H2O
N-acetyl-DEVD + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
nuclear mitotic apparatus protein + H2O
?
show the reaction diagram
-
-
-
-
?
p65/RelA + H2O
?
show the reaction diagram
-
caspase-3-mediated carboxy-terminal fragment of p65/RelA production, cells producing this truncated p65/RelA do not undergo apoptosis but show a high viability, in spite of caspase-3 activation, overview. The substrate translocate to the nucleus, associates with NF-kappaB1/p50 and IkappaBalpha, but cannot bind -kappaB consensus sites
-
-
?
PAK2 + H2O
?
show the reaction diagram
-
caspase-3 is mainly responsible for the apoptotic cleavage of PAK2 in Fas-stimulated Jurkat cells
-
-
?
poly(ADP-ribose) polymerase + H2O
85000 Da fragment + ?
show the reaction diagram
pro-caspase-6 + H2O
?
show the reaction diagram
-
caspase-8 activates caspase-3, and caspase-3 in turn activates caspase-6. Caspase 3 has a major role in nuclear apoptosis
-
-
?
pro-interleukin-18 + H2O
IL18 + ?
show the reaction diagram
-
virus infection by influenzy A or Sendai virus induces proteolytic processing of IL-18 in human macrophages via caspase-1 and caspase-3 activation
-
-
?
pro-Mch2alpha + H2O
?
show the reaction diagram
-
the enzyme processes pro-Mch2alpha at three aspartate processing sites, Asp23, Asp179, and Asp193, to produce the large p18 and small p11 subunits of the mature Mch2alpha enzyme. Mch2alpha is a downstream protease activated in CPP32- and granzyme B-mediated apoptosis
-
-
?
pro-Mch6 + H2O
?
show the reaction diagram
-
the enzyme processes proMch6 preferentially at Asp330 to generate two subunits of molecular masses 37000 Da and 10000 Da. Mch6 is a downstream protease activated in CPP32- and granzyme B-mediated apoptosis
-
-
?
procaspase-3 + H2O
caspase-3 + ?
show the reaction diagram
procaspase-6 + H2O
caspase-6 + ?
show the reaction diagram
protein kinase Cdelta + H2O
?
show the reaction diagram
-
protein kinase Cdelta plays a major role in the regulation of cell apoptosis and survival. PKCdelta is cleaved by caspase 3 to generate a constitutively active catalytic domain that mediates both its apoptotic and anti-apoptotic effects. The phosphorylation of Tyr332 is necessary for the caspase 3-dependent cleavage of protein kinase Cdelta
-
-
?
protein kinase Czeta + H2O
?
show the reaction diagram
-
major cleavage site EETD-/-G, also cleaves at DGMD-/-G and DSED-/-L. Caspase-3 is involved in processing of protein kinase Czeta to carboxyl-terminal fragments that are catalytically active and that are degraded by the ubiquitin-proteasome pathway
-
-
?
protein phosphatase-1 inhibitor-3 + H2O
?
show the reaction diagram
-
the substrate is an in vivo target of caspase-3 and participates in the apoptotic response to induction by actinomycin D, overview
-
-
?
RelB + H2O
?
show the reaction diagram
-
the Asp205 site in RelB is specifically cleaved by caspase-3 in vinblastine-treated HAT-1080 cells
-
-
?
RFC140 + H2O
?
show the reaction diagram
-
cleavage of RFC140 during apoptosis inactivates its function in DNA replication and generates truncated forms that further inhibit DNA replication
-
-
?
Rho-GDI 1 + H2O
?
show the reaction diagram
-
differential regulation of the homologous GDP dissociation inhibitors Rho-GDI 1 and D4-GDI during drug-induced apoptosis by proteolysis mediated by caspase-3
-
-
?
Rpt2 + H2O
?
show the reaction diagram
-
-
-
-
?
Rpt5 + H2O
?
show the reaction diagram
-
in myoblasts, Rpt5 is sensitive to caspase-3-induced cleavage but in myotubes, it is not sensitive. Caspase-3 cleavage of Rpt5 is responsible for the difference in the patterns of proteasome subunit cleavage in myoblasts compared with myotubes
-
-
?
Rpt6 + H2O
?
show the reaction diagram
-
-
-
-
?
SETbeta + H2O
?
show the reaction diagram
-
-
-
-
?
topoisomerase I + H2O
?
show the reaction diagram
-
cleavage at DDVD146-/-Y and EEED170-/-G
-
-
?
additional information
?
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(3R)-3-ethyl-1-[methyl(octyl)amino]-6-[3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]octane-2,5-dione
-
50% inhibition at 9 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells
(3R)-3-ethyl-6-[2-oxo-3-[(1,3-thiazol-5-ylmethyl)amino]pyrazin-1(2H)-yl]-1-(phenylsulfanyl)octane-2,5-dione
-
50% inhibition at 12 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells
(3R)-3-ethyl-6-[3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]-1-(phenylsulfanyl)octane-2,5-dione
-
50% inhibition at 7.9 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells
(3R)-3-ethyl-6-[5-ethyl-3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]-1-[hexyl(methyl)amino]octane-2,5-dione
-
50% inhibition at 6 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells
(3R)-6-[5-tert-butyl-3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]-3-ethyl-1-[hexyl(methyl)amino]octane-2,5-dione
-
i.e. M826, 50% inhibition at 6 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells
(3R)-6-[5-tert-butyl-3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]-3-ethyl-1-[methyl(pentyl)amino]octane-2,5-dione
-
i.e. M867, 50% inhibition at 0.1 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells
(3S)-3-([[(4-fluorophenyl)amino](oxo)acetyl]amino)-4-oxopentanoic acid
-
-
(3S)-3-([[2-(3-carboxypropyl)-1,3-dioxo-8-(2-phenylethyl)-2,3,5,8-tetrahydro-1H-[1,2,4]triazolo[1,2-a]pyridazin-5-yl]carbonyl]amino)-5-[(2,6-dichlorobenzoyl)oxy]-4-oxopentanoic acid
-
-
(3S)-3-([[2-(3-carboxypropyl)-1,3-dioxo-8-(pyridin-3-yl)-2,3,5,8-tetrahydro-1H-[1,2,4]triazolo[1,2-a]pyridazin-5-yl]carbonyl]amino)-5-[(2,6-dichlorobenzoyl)oxy]-4-oxopentanoic acid
-
-
(3S)-3-([[2-(3-carboxypropyl)-1,3-dioxo-8-[2-[(thiophen-2-ylacetyl)amino]ethyl]-2,3,5,8-tetrahydro-1H-[1,2,4]triazolo[1,2-a]pyridazin-5-yl]carbonyl]amino)-5-[(2,6-dichlorobenzoyl)oxy]-4-oxopentanoic acid
-
-
(3S)-3-([[2-(3-carboxypropyl)-8-(2-[[(4-chlorophenyl)acetyl]amino]ethyl)-1,3-dioxo-2,3,5,8-tetrahydro-1H-[1,2,4]triazolo[1,2-a]pyridazin-5-yl]carbonyl]amino)-5-[(2,6-dichlorobenzoyl)oxy]-4-oxopentanoic acid
-
-
(3S)-3-([[2-[2-[(1H-benzimidazol-6-ylcarbonyl)amino]ethyl]-7-(cyclohexylmethyl)-1,3-dioxo-2,3,5,8-tetrahydro-1H-[1,2,4]triazolo[1,2-a]pyridazin-5-yl]carbonyl]amino)-5-[(2,6-dichlorobenzoyl)oxy]-4-oxopentanoic acid
-
-
(3S)-3-([[2-[2-[(cyclohexylcarbonyl)amino]ethyl]-7-(cyclohexylmethyl)-1,3-dioxo-2,3,5,8-tetrahydro-1H-[1,2,4]triazolo[1,2-a]pyridazin-5-yl]carbonyl]amino)-5-[(2,6-dichlorobenzoyl)oxy]-4-oxopentanoic acid
-
-
(3S)-3-[(2-[3-[(N-acetyl-L-alpha-aspartyl)amino]-2-oxopyridin-1(2H)-yl]butanoyl)amino]-5-(benzylsulfanyl)-4-oxopentanoic acid
-
50% inhibition at 52 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer
(3S)-3-[(2-[3-[(N-acetyl-L-alpha-aspartyl)amino]-2-oxopyridin-1(2H)-yl]butanoyl)amino]-5-[(2-chloro-6-fluorobenzyl)sulfanyl]-4-oxopentanoic acid
-
50% inhibition at 0.3 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer
(3S)-3-[[(2-[4-carboxy-2-[(phenylacetyl)amino]butyl]-1,3-dioxo-2,3,5,7,8,9,10,10a-octahydro-1H-[1,2,4]triazolo[1,2-a]cinnolin-5-yl)carbonyl]amino]-5-[(2,6-dichlorobenzoyl)oxy]-4-oxopentanoic acid
-
-
(3S)-3-[[(2R)-2-[3-[(naphthalen-2-ylcarbonyl)amino]-2-oxopyridin-1(2H)-yl]-2-phenylacetyl]amino]-4-oxo-5-phenoxypentanoic acid
-
-
(3S)-5-(2,6-difluorophenoxy)-3-([[(2-methoxyphenyl)amino](oxo)acetyl]amino)-4-oxopentanoic acid
-
-
(3S)-5-(2,6-difluorophenoxy)-3-([[(3-methylphenyl)amino](oxo)acetyl]amino)-4-oxopentanoic acid
-
-
(3S)-5-(2,6-difluorophenoxy)-3-([[(4-methylphenyl)amino](oxo)acetyl]amino)-4-oxopentanoic acid
-
-
(3S)-5-(benzylsulfanyl)-3-([N-[(2,5-dimethoxyphenyl)acetyl]-L-valyl]amino)-4-oxopentanoic acid
-
50% inhibition at 48 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer
(3S)-5-(benzylsulfanyl)-3-[(N-[[2-ethoxy-5-(2-methoxy-2-oxoethoxy)phenyl]acetyl]-L-valyl)amino]-4-oxopentanoic acid
-
50% inhibition at 86 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer
(3S)-5-fluoro-3-([[(4-fluorophenyl)amino](oxo)acetyl]amino)-4-oxopentanoic acid
-
-
(3S)-5-[(2,6-dichlorobenzoyl)oxy]-3-[([1,3-dioxo-2-[2-(1H-tetrazol-5-yl)ethyl]-2,3,5,7,8,9,10,10a-octahydro-1H-[1,2,4]triazolo[1,2-a]cinnolin-5-yl]carbonyl)amino]-4-oxopentanoic acid
-
-
(3S)-5-[(2-chloro-6-fluorobenzyl)sulfanyl]-3-[(N-[[2-ethoxy-5-(2-methoxy-2-oxoethoxy)phenyl]acetyl]-L-valyl)amino]-4-oxopentanoic acid
-
50% inhibition at 53 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer
(4S,7S,10S,13S)-7-(2-carboxyethyl)-4-(carboxymethyl)-13-(cyclobutylcarbonyl)-10-(1-methylethyl)-2,5,8,11-tetraoxo-3,6,9,12-tetraazapentadecan-15-oic acid
-
non-preferred name, comparison with inhibition of caspase-7
(R)-5-[1-(2-methoxymethyl)pyrrolidinylsulfonyl]isatin
-
IC50: 0.018 mM
(R)-5-[1-[2-(anilinomethyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 0.0055 mM
(S)-(+)-5-[1-[2-(thiophenoxymethyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 44 nM
(S)-1-((1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1H-1,2,3-triazol-4-yl)methyl)-5-((2-(methoxymethyl)pyrrolidin-1-yl)sulfonyl)indoline-2,3-dione
-
-
(S)-1-(11,11-difluoroundecyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-(2-fluoroallyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-(2-fluoroethyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-(3-chloro-2-hydroxypropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-(3-chloropropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-(3-fluorobutyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-(3-fluoropropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-(3-hydroxypropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-(4-fluorobutyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-(4-hydroxybutyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-(4-pyridinylmethyl)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonal]isatin
-
IC50: 4.2 nM
(S)-1-(carboxymethyl)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 170 nM
(S)-1-(cyclohexylmethyl)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonal]isatin
-
IC50: 5.2 nM
(S)-1-allyl-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 4.6 nM
(S)-1-benzyl-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 2.5 nM
(S)-1-butyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-ethyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-methyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-methyl-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 30 nM
(S)-1-propyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-isatin
-
-
(S)-1-[(tert-butyloxycarbonyl)methyl]-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 3.1 nM
(S)-1-[3-(3-fluoropropoxy)propyl]-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-[3-(3-hydroxypropoxy)propyl]-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-1-[3-[3-(2-fluoroethoxy)propoxy]propyl]-5-[1-(2-methoxymethylpyrrolidinyl)-sulfonyl]isatin
-
-
(S)-3,3-difluoro-1-(3-fluoropropyl)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]indolin-2-one
-
-
(S)-3,3-difluoro-1-propyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]indolin-2-one
-
-
(S)-3,5-bis-trifluoromethylbenzyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-3-[3-[5-(1-(2-methoxymethylpyrrolidinyl)sulfonyl)-2,3-dioxoindolin-1-yl]propoxy]-propyl methanesulfonate
-
-
(S)-3-[5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-2,3-dioxoindolin-1-yl]propanoic acid
-
-
(S)-3-[5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-2,3-dioxoindolin-1-yl]propyl methanesulfonate
-
-
(S)-3-[[5-(1-carboxymethyl-2-oxo-ethylcarbamoyl)-pyridin-2-ylmethyl]sulfamoyl]benzoic acid
-
-
(S)-3-[[6-(benzenesulfonylamino-methyl)pyridine-3-carbonyl]amino]-4-oxo-butyric acid
-
-
(S)-3-[[6-[(3-acetylsulfamoyl-benzenesulfonylamino)-methyl]pyridine-3-carbonyl]amino]-4-oxo-butyric acid
-
-
(S)-3-[[6-[(3-methanesulfonyl-benzenesulfonylamino)-methyl]pyridine-3-carbonyl]amino]-4-oxo-butyric acid
-
-
(S)-3-[[6-[(3-methanesulfonylamino-benzenesulfonylamino)methyl]pyridine-3-carbonyl]amino]-4-oxo-butyric acid
-
-
(S)-3-[[6-[(3-methanesulfonylaminocarbonyl-benzenesulfonylamino)methyl]-pyridine-3-carbonyl]amino]-4-oxobutyric acid
-
-
(S)-3-[[6-[(4-hydroxy-benzenesulfonylamino)methyl]-pyridine-3-carbonyl]amino]-4-oxo-butyric acid
-
-
(S)-3-[[6-[(4-methanesulfonylamino-benzenesulfonylamino)methyl]pyridien-3-carbonyl]amino]-4-oxo-butyric acid
-
-
(S)-4-fluorobenzyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-4-oxo-3-[[6-[[3-(1H-tetrazol-5-yl)benzenesulfonylamino]methyl]pyridine-3-carbonyl]amino]butyric acid
-
-
(S)-4-oxo-3-[[6-[[3-(5-oxo-4,5-dihydro[1,2,4]oxadiazol-3-yl)benzenesulfonylamino]methyl]pyridien-3-carbonyl]amino]butyric acid
-
-
(S)-4-trifluoromethylbenzyl-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
(S)-4-[5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-2,3-dioxoindolin-1-yl]butyl 4-methyl-benzenesulfonate
-
-
(S)-4-[[4-(hydroxy-3-methyl-benzenesulfonylamino)methyl]thiophene]-2-carboxylic acid [3-(2-chloro-benzylsulfanyl)-1-ethyl-2-oxo-propyl]amide
-
-
(S)-5-[1-(2-methoxymethyl)pyrrolidinylsulfonyl]isatin
-
IC50: 120 nM
(S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(3,3,3-trifluoropropyl)isatin
-
-
(S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(3,4,4-trifluorobut-3-enyl)isatin
-
-
(S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(4,4,4-trifluorobutyl)isatin
-
-
(S)-5-[1-[(2-methoxycarbonyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 170 nM
(S)-5-[1-[(2-tert-butoxycarbonyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 70 nM
(S)-5-[1-[2-(anilinomethyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 31 nM
(S)-5-[1-[2-(phenoxymethyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 44 nM
(S)-5-[1-[2-(phenylaminocarbonyl)pyrrolidinyl]sulfonyl]isatin
-
IC50: 140 nM
(S)-5-[1-[[2-(dimethylamino)carbonyl]pyrrolidinyl]sulfonyl]isatin
-
IC50: 410 nM
(S)-5-[[3-(1-carboxymethyl-2-oxo-ethylcarbamoyl)isooxazol-5-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[3-[1-carboxymethyl-3-(2-chloro-benzylsulfanyl)-2-oxo-propylcarbamoyl]isoxazol-5-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[4-(1-carboxymethyl-2-oxo-ethylcarbamoyl)-thiophen-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-(1-carboxymethyl-2-oxo-ethylcarbamoyl)-4-methyl-thiophen-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-(1-carboxymethyl-2-oxo-ethylcarbamoyl)-furan-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-(1-carboxymethyl-2-oxo-ethylcarbamoyl)-pyrazin-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-(1-carboxymethyl-2-oxo-ethylcarbamoyl)-thiazol-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-(1-carboxymethyl-2-oxo-ethylcarbamoyl)-thiophen-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-(1-carboxymethyl-2-oxo-ethylcarbamoyl)-thiophen-3-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-(1-carboxymethyl-2-oxo-ethylcarbamoyl)pyridin-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-(1-carboxymethyl-2-oxo-ethylcarbamoyl)pyrimidin-2-ylmethyl]sulfamoyl]-2-hydroxybenzoic acid
-
-
(S)-5-[[5-(1-carboxymethyl-3-methylsulfanyl-2-oxo-propylcarbamoyl)pyridin-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-2-oxo-3-(pyridin-3-ylmethylsulfanyl)propylcarbamoyl]thiophen-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-2-oxo-3-(pyridin-4-ylmethylsulfanyl)propylcarbamoyl]thiophen-2-ylmethyl]-sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-3-(2-chloro-benzylsulfanyl)-2-oxo-propylcarbamoyl]-4-methyl-thiophen-2-ylmethyl]-sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-3-(2-chloro-benzylsulfanyl)-2-oxo-propylcarbamoyl]furan-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-3-(2-chloro-benzylsulfanyl)-2-oxo-propylcarbamoyl]pyrazin-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-3-(2-chloro-benzylsulfanyl)-2-oxo-propylcarbamoyl]pyridin-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-3-(2-chloro-benzylsulfanyl)-2-oxo-propylcarbamoyl]pyrimidin-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-3-(2-chloro-benzylsulfanyl)-2-oxo-propylcarbamoyl]thiazol-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-3-(2-chloro-benzylsulfanyl)-2-oxo-propylcarbamoyl]thiophen-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-3-(2-chloro-benzylsulfanyl)-2-oxo-propylcarbamoyl]thiophen-3-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
(S)-5-[[5-[1-carboxymethyl-5-(2-chloro-phenyl)-2-oxopentylcarbamoyl]thiophen-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
1,2-benzisothiazol-3-one
-
-
-
1,2-butanedithiol
-
60% inhibition
1,4-dihydroxy-2-naphthoic acid
-
-
1-(3-oxo-1,2-benzothiazol-2(3H)-yl)-4-(thiophen-2-yl)butane-1,4-dione
-
-
1-methyl-5-nitro-1H-indole-2,3-dione
-
-
1-methyl-5-[[(2S)-2-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione
-
-
1-methyl-5-[[(3R)-3-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione
-
i.e. GSK-31, inhibitory effect is greatest in presence of 2-mercaptoethanol and decreases 2fold by substitution of 2-mercaptoethanol with dithiothreitol
1-[[1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1H-1,2,3-triazol-5-yl]methyl]-5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione
-
-
1-[[1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl]methyl]-5-[[(2S)-2-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione
-
-
1-[[1-(biphenyl-4-yl)-1H-1,2,3-triazol-4-yl]methyl]-5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione
-
-
1-[[1-(biphenyl-4-yl)-1H-1,2,3-triazol-5-yl]methyl]-5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione
-
-
2,4-dimethyl-8-(morpholin-4-ylsulfonyl)-1H-pyrrolo[3,4-c]quinoline-1,3(2H)-dione
-
50% inhibition at 0.000044 mM
2-(1,3-dihydro-2-benzofuran-5-ylacetyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(2,6-dihydroxyphenyl)-4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
2-(2-hydroxyethyl)-4-methyl-8-[(4-methylpiperidin-1-yl)sulfonyl]-1H-pyrrolo[3,4-c]quinoline-1,3(2H)-dione
-
i.e. CD-001-0011, 50% inhibition at 130 nM, reversible, inhibitory effect is greatest in presence of dithiothreitol and decreases 3-4fold by substitution of dithiothreitol with 2-mercaptoethanol
2-(2-phenylethyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-[4-(1H-pyrrol-1-yl)phenyl]acetamide
-
-
2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-[4-(piperidin-1-yl)phenyl]acetamide
-
-
2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-[4-(pyridin-2-yl)phenyl]acetamide
-
-
2-(3-phenylpropanoyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(4-fluorobenzyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(4-methoxybenzyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(4-methylphenyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(4-phenylbutanoyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(5-phenylpentanoyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(biphenyl-4-ylacetyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(chloroacetyl)-4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
2-(naphthalen-2-ylacetyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(phenylacetyl)-1,2-benzothiazol-3(2H)-one
-
-
2-(prop-2-en-1-yl)-1,2-benzothiazol-3(2H)-one
-
-
2-(thiophen-2-ylacetyl)-1,2-benzothiazol-3(2H)-one
-
-
2-amino-4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
2-benzyl-1,2-benzothiazol-3(2H)-one
-
-
2-chloro-N-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)acetamide
-
50% inhibition at 92 nM
2-ethyl-1,2-benzothiazol-3(2H)-one
-
-
2-methoxy-N-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-5-yl)benzamide
-
50% inhibition at 96 nM
2-methoxy-N-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)benzamide
-
50% inhibition at 103 nM
2-methyl-1,2-benzothiazol-3(2H)-one
-
-
2-nitro-N-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)benzamide
-
50% inhibition at 62 nM
2-phenyl-1,2-benzothiazol-3(2H)-one
-
-
2-[(2,6-dihydroxyphenyl)amino]-4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
2-[(2-chlorophenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(2-fluorophenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(2-hydroxyphenyl)amino]-4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
2-[(2-methoxyphenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(2-methylphenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(3,4-dichlorophenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(3,5-diamino-4-hydroxyphenyl)amino]-4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
2-[(3-chlorophenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(3-fluorophenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(3-methoxyphenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(3-methylphenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(4-chlorophenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(4-fluorophenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(4-hydroxyphenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(4-hydroxyphenyl)amino]-4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
2-[(4-methoxyphenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[(4-methylphenyl)acetyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[3-(2-chlorophenyl)propanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[3-(2-fluorophenyl)propanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[3-(2-methoxyphenyl)propanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[3-(3-fluorophenyl)propanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[3-(3-methoxyphenyl)propanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[3-(3-methylphenyl)propanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[3-(4-chlorophenyl)propanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[3-(4-fluorophenyl)propanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[3-(4-methoxyphenyl)propanoyl]-1,2-benzothiazol-3(2H)-one
-
most potent inhibitor
2-[3-(4-methylphenyl)propanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[3-(trifluoromethyl)phenyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[4-(4-methoxyphenyl)butanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[4-(4-methylphenyl)butanoyl]-1,2-benzothiazol-3(2H)-one
-
-
2-[4-(thiophen-2-yl)butanoyl]-1,2-benzothiazol-3(2H)-one
-
-
3,3-dimethyl-8-[[(2S)-2-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl]-3,4-dihydropyrimido[1,2-a]indol-10(2H)-one
-
-
3-({2-[5-tert-butyl-3-{[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino}-2-oxopyrazin-1(2H)-yl]butanoyl}amino)-5-[methyl(pentyl)amino]-4-oxopentanoic acid
3-chloro-N-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)propanamide
-
50% inhibition at 83 nM, comparison with inhibitory effect on caspase-2, caspase-6, caspase-7, caspase-8, papain, proteasome, trypsin and thrombin
3-hydroxyl-anthranilamide
-
inhibits caspase-3, the compound is isolated from Streptomyces sp., a mangrove actinomycete, strain 061316
3-morpholinosydnonimine
-
i.e. SIN-1, 1 mM, complete inhibition
3-nitro-N-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-5-yl)benzamide
-
50% inhibition at 53 nM
3-oxo-N-(1-phenylethyl)-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-(2-phenylethyl)-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-(3-phenylpropyl)-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-phenyl-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-[2-(pyridin-2-yl)ethyl]-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-[2-(thiophen-2-yl)ethyl]-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-[4-(1H-pyrrol-1-yl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-[4-(piperidin-1-yl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-[4-(piperidin-1-ylsulfonyl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-[4-(pyridin-2-yl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-[4-(pyrrolidin-1-yl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-oxo-N-[4-(pyrrolidin-1-ylsulfonyl)phenyl]-1,2-benzothiazole-2(3H)-carboxamide
-
-
3-[[(2-methyl-1H-indol-1-yl)acetyl]amino]-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid
-
-
3-[[(5-bromo-1H-indol-1-yl)acetyl]amino]-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid
-
-
3-[[(5-bromo-1H-indol-1-yl)acetyl]amino]-5-(2,6-difluorophenoxy)-4-oxopentanoic acid
-
-
3-[[(5-bromo-1H-indol-1-yl)acetyl]amino]-5-fluoro-4-oxopentanoic acid
-
-
3-[[(5-chloro-1H-indol-1-yl)acetyl]amino]-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid
-
-
3-[[(5-chloro-1H-indol-1-yl)acetyl]amino]-5-(2,6-difluorophenoxy)-4-oxopentanoic acid
-
-
3-[[(5-chloro-1H-indol-1-yl)acetyl]amino]-5-fluoro-4-oxopentanoic acid
-
-
3-[[(5-fluoro-1H-indol-1-yl)acetyl]amino]-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid
-
-
3-[[(5-methoxy-1H-indol-1-yl)acetyl]amino]-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid
-
-
4-(ethoxycarbonylmethoxy)-1-hydroxy-2-naphthoic acid
-
CS4566, a caspase-3-specific small molecular inhibitor, binding mode, overview
4-fluoro-N-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-5-yl)benzamide
-
50% inhibition at 99 nM
4-methyl-1,3-dioxo-2-(1,3,5-trimethyl-1H-pyrazol-4-yl)-2,3-dihydro-1H-pyrrolo[3,4-c]quinoline-8-carbonitrile
-
50% inhibition at 0.000016 mM
4-methyl-1,3-dioxo-2-(1,3,5-trimethyl-1H-pyrazol-4-yl)-2,3-dihydro-1H-pyrrolo[3,4-c]quinoline-8-sulfonamide
-
50% inhibition at 0.000033 mM
4-methyl-1,3-dioxo-2-(1,3,5-trimethyl-1H-pyrazol-4-yl)-2,3-dihydro-1H-pyrrolo[3,4-c]quinoline-8-sulfonic acid
-
50% inhibition at 0.00009 mM
4-methyl-2-(1-methylethyl)-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
4-methyl-8-(morpholin-4-ylsulfonyl)-1H-pyrrolo[3,4-c]quinoline-1,3(2H)-dione
-
50% inhibition at 0.00021 mM
4-methyl-8-(morpholin-4-ylsulfonyl)-2-(1,3,5-trimethyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]quinoline-1,3(2H)-dione
-
50% inhibition at 0.000004 mM
4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-2-(1,3-thiazol-2-yl)-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-2-(2,4,6-trihydroxyphenyl)-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-2-(phenylamino)-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-2-[(2,4,6-trihydroxyphenyl)amino]-1H-cyclopenta[c]quinoline-1,3(2H)-dione
-
-
4-methyl-8-[[(2R)-2-phenoxypyrrolidin-1-yl]sulfonyl]-2-(1,3,5-trimethyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]quinoline-1,3(2H)-dione
-
50% inhibition at 0.000055 mM
4-nitro-N-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)benzamide
-
50% inhibition at 54 nM
4-oxo-4-piperidin-1-yl-N-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)butanamide
-
50% inhibition at 25 nM, comparison with inhibitory effect on caspase-2, caspase-6, caspase-7, caspase-8, papain, proteasome, trypsin and thrombin
4-oxo-4-[(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)amino]butanoic acid
-
50% inhibition at 68 nM, comparison with inhibitory effect on caspase-2, caspase-6, caspase-7, caspase-8, papain, proteasome, trypsin and thrombin
4-[4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-1,3-dioxo-2,3-dihydro-1H-cyclopenta[c]quinolin-2-yl]benzoic acid
-
-
4-[5-([(3S)-1-[(2,6-dichlorobenzoyl)oxy]-2,5-dioxohexan-3-yl]carbamoyl)-1,3-dioxo-8-(thiophen-2-yl)-5,8-dihydro-1H-[1,2,4]triazolo[1,2-a]pyridazin-2(3H)-yl]butanoic acid
-
-
5-(2,6-difluorophenoxy)-3-[[(2-methyl-1H-indol-1-yl)acetyl]amino]-4-oxopentanoic acid
-
-
5-(2,6-difluorophenoxy)-3-[[(5-fluoro-1H-indol-1-yl)acetyl]amino]-4-oxopentanoic acid
-
-
5-(2,6-difluorophenoxy)-3-[[(5-methoxy-1H-indol-1-yl)acetyl]amino]-4-oxopentanoic acid
-
-
5-([(2R)-2-[(2,4-difluorophenoxy)methyl]pyrrolidin-1-yl]sulfonyl)-1-[[1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl]methyl]-1H-indole-2,3-dione
-
-
5-([(2S)-2-[(pyridin-3-yloxy)methyl]pyrrolidin-1-yl]sulfonyl)-1H-indole-2,3-dione
-
-
5-fluoro-3-[[(2-methyl-1H-indol-1-yl)acetyl]amino]-4-oxopentanoic acid
-
-
5-fluoro-3-[[(5-fluoro-1H-indol-1-yl)acetyl]amino]-4-oxopentanoic acid
-
-
5-fluoro-3-[[(5-methoxy-1H-indol-1-yl)acetyl]amino]-4-oxopentanoic acid
-
-
5-oxo-5-[(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)amino]pentanoic acid
-
50% inhibition at 79 nM
5-[1-(azetidinyl)sulfonyl]isatin
-
IC50: 170 nM
5-[1-(hexamethyleneimino)sulfonyl]isatin
-
IC50: 0.0019 mM
5-[1-(piperidinyl)sulfonyl]isatin
-
IC50: 0.0022 mM
5-[1-(pyrrolidinyl)sulfonyl]isatin
-
IC50: 0.0028 mM
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-([1-[4-(trifluoromethyl)phenyl]-1H-1,2,3-triazol-4-yl]methyl)-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-([1-[4-(trifluoromethyl)phenyl]-1H-1,2,3-triazol-5-yl]methyl)-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-[(1-phenoxy-1H-1,2,3-triazol-4-yl)methyl]-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-[(1-phenoxy-1H-1,2,3-triazol-5-yl)methyl]-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-[(1-phenyl-1H-1,2,3-triazol-4-yl)methyl]-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-[(1-phenyl-1H-1,2,3-triazol-5-yl)methyl]-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-[2-(1-phenyl-1H-1,2,3-triazol-4-yl)ethyl]-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-[2-(1-phenyl-1H-1,2,3-triazol-5-yl)ethyl]-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-[[1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl]methyl]-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-[[1-(4-methoxyphenyl)-1H-1,2,3-triazol-5-yl]methyl]-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-[[1-(4-nitrophenyl)-1H-1,2,3-triazol-4-yl]methyl]-1H-indole-2,3-dione
-
-
5-[[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-[[1-(4-nitrophenyl)-1H-1,2,3-triazol-5-yl]methyl]-1H-indole-2,3-dione
-
-
5-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione
-
-
5-[[(2S)-2-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl]-1-phenyl-1H-indole-2,3-dione
-
-
5-[[(2S)-2-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione
-
-
5-[[5-[1-carboxymethyl-2-(7-methyl-benzoxazol-2-yl)-2-oxo-ethylcarbamoyl]thiophen-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
5-[[5-[1-carboxymethyl-2-[5-(2,6-dichloro-phenyl)-oxazol-2-yl]-2-oxo-ethylcarbamoyl]thiophen-2-ylmethyl]sulfamoyl]-2-hydroxy-benzoic acid
-
-
6-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione
-
-
8-hydroxyl-2,4-dioxoquinazoline
-
inhibits caspase-3, the compound is isolated from Streptomyces sp., a mangrove actinomycete, strain 061316
8-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]-3,3-dimethyl-3,4-dihydropyrimido[1,2-a]indol-10(2H)-one
-
-
Ac-Asp-Glu-Val-Asp-H
-
the molecule can be truncated to Z-tLeu-Asp-H retaining nanomolar inhibitory activity in vitro and displaying action in whole cells, overview
Ac-CV3-KE
-
-
Ac-DEVD-7-amido-4-methylcoumarin
-
a caspase-3 inhibitor
Ac-DEVD-CHO
Ac-DMQD-CHO
-
-
Ac-DNLD-CHO
-
from rational computational design, the inhibitor is specific due to the specific interaction of the NLD moiety with the active site of caspase-3, docking mode and site-directed mutagenesis analysis. In the active site of caspase-3, Asn in Ac-DNLDCHO specifically interacts with Ser209 in the S3 subsite, and Leu tightly interacts with the hydrophobic S2 subsite, overview
Ac-DQMD-CHO
-
-
Ac-DW3-KE
-
-
-
Ac-F-D-beta-hLeu-hLeu-D-KE
-
-
-
Ac-IEPD-CHO
-
a reversible aldehyde caspase-3 inhibitor, bound in extended conformation in the S1-S4 substrate binding sites of caspase-3, binding structure with hydrogen bond and ionic interactions, overview
Ac-WEHD-CHO
-
a reversible aldehyde caspase-3 inhibitor, bound in extended conformation in the S1-S4 substrate binding sites of caspase-3, binding structure with hydrogen bond and ionic interactions, overview
Ac-YVAD-CHO
-
a reversible aldehyde caspase-3 inhibitor, bound in extended conformation in the S1-S4 substrate binding sites of caspase-3, binding structure with hydrogen bond and ionic interactions, overview
acetyl-AEVD-aldehyde
-
-
acetyl-Ala-Pro-Nle-Asp-aldehyde
-
-
Acetyl-Asp-Glu-Val-Asp-aldehyde
-
-
acetyl-Asp-Met-Gln-Asp-aldehyde
-
-
acetyl-DEVD-aldehyde
acetyl-DEVD-CHO
-
-
acetyl-DEVD-fluoromethylketone
-
-
acetyl-IETD-aldehyde
-
-
acetyl-Val-Asp-Val-Ala-Asp-aldehyde
-
-
acetyl-WEHD-aldehyde
-
-
acetyl-YVAD-aldehyde
-
-
Asp-Glu-Val-Asp-aldehyde
Asp-Glu-Val-Asp-chloromethylketone
-
-
Asp-Glu-Val-Asp-fluoromethylketone
Asp-Phe-Leu-Asp-aldehyde
-
IC50 for membrane enzyme: 4.7 nM
baculovirus p35
-
IC50 for membrane enzyme: 0.074 nM
-
Bcl-2
-
an antiapoptotic protein that is localized to the intracellular membrane, nuclear membrane and endoplasmic reticulum, and blocks caspase activation by inhibiting the mitochondrial release of cytochrome c
-
Bcl2-Like12
-
is a nuclear and cytoplasmic oncoprotein that inhibits caspase-3 and apoptosis, mechanism, overview
-
benzyloxycarbonyl-Asp-Glu-Val-aza-aspartyl-(S,S) Glu-Pro-CO-N(CH2Ph)2
-
-
benzyloxycarbonyl-Asp-Glu-Val-aza-aspartyl-(S,S) Glu-Pro-CO-NHCH2Ph
-
-
benzyloxycarbonyl-Asp-Glu-Val-aza-aspartyl-(S,S) Glu-Pro-COO-CH2Ph
-
-
benzyloxycarbonyl-DEVD-fluoromethylketone
-
-
benzyloxycarbonyl-Glu-Val-aza-aspartyl-(S,S) Glu-Pro-CO-NH-CH2CH2Ph
-
-
benzyloxycarbonyl-Leu-Glu-Val-aza-aspartyl-(S,S) Glu-Pro-CO-Ala-NH-CH2Ph
-
-
benzyloxycarbonyl-Pro-Nle-Asp-aldehyde
-
-
-
benzyloxycarbonyl-VAD-fluoromethylketone
-
-
benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone
-
a specific caspase 3 inhibitor
benzyloxycarbonyl-Val-Ala-Asp-fluoromethylketone
benzyloxycarbonyl-Val-Ala-DL-Asp-fluoromethylketone
-
a general caspase inhibitor
benzyloxycarbonyl-WEHD-fluoromethylketone
-
-
-
BF4NO
-
0.1 mM, complete inhibition
Boc-D(OMe)-fluoromethyl ketone
-
a pan-caspase irreversible inhibitor
bradykinin
-
prevents caspase-3 activation in neurons
calbindin D28k
-
prevents osteoblast apoptosis by interaction and direct inhibition of caspase-3
-
carbobenzyloxy-DEVD-fluoromethyl ketone
-
a caspase-3 inhibitor
carbobenzyloxy-VAD
-
-
carbobenzyloxy-VAD-fluoromethyl ketone
-
a pan-caspase inhibitor
Cd2+
-
-
cIAP
-
-
-
cowpox serpin CrmA
-
-
-
DEVD-CHO
-
a potent caspase-3 inhibitor
DEVD-fluoromethyl ketone
DEVD-fluoromethylketone
-
-
ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
-
a BH3 mimetic compound, inhibits activation of procaspase-3
FAM-Ahx2-CV3-AOMK
-
-
-
FAM-DEVD-AOMK
-
-
FAM-DEVD-FMK
-
-
Fe3+
-
50% inhibition at 0.007 mM
FLICE-inhibitory proteins
-
some isoforms, including FLIPR inhibit Fas-mediated apoptosis by impeding caspase 3 activity as well as poly(ADP-ribose) polymerase cleavage
-
G-CSF
-
a caspase-3 inhibitor that also inhibits the steady increase in cytosolic free Ca2 during neutrophil aging, which is essential for apoptosis
-
glutathione disulfide
-
glutathionylation of caspase can occur at physiologically relevant concentrations of glutathione disulfide and results in the inhibition of caspase activation and activity
HBx
-
hepatitis virus Hbx protein, potent
-
Hg2+
-
-
human poly(ADP-ribose) polymerase autoantibodies
-
-
-
IDN6556
-
-
inhibitor of apoptosis protein
-
IAP, the family members block effector caspase-3 further downstream, which potentially inhibits apoptosis
-
iodoacetamide
-
-
isoquinoline-1,3,4(2H)-trione
-
50% inhibition at 149 nM
lipoic acid
-
80% inhibition
m-(Ac-L-Asp-L-Val-NH)-N-nitroso-N-phenylglycine
-
-
m-(acetyl-L-Asp-L-Val-NH)-N-nitroso-N-phenylglycine
-
-
methyl (8-bromo-4-methyl-1,3-dioxo-1,3-dihydro-2H-pyrrolo[3,4-c]quinolin-2-yl)acetate
-
50% inhibition at 0.00046 mM
methyl 3-nitro-5-[[(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-5-yl)amino]carbonyl]benzoate
-
50% inhibition at 104 nM
methyl 3-nitro-5-[[(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)amino]carbonyl]benzoate
-
50% inhibition at 66 nM
methyl N-acetyl-3-(pyridin-3-yl)-D-alanyl-N-[[(3S)-1-[(2R)-1-[(3S)-1-methoxy-5-[[(5-methylthiophen-2-yl)carbonyl]oxy]-1,4-dioxopentan-3-yl]amino-1-oxo-3-phenylpropan-2-yl]amino]-5-methyl-1-oxohexan-3-yl]-L-alpha-asparaginate
-
low nanomolar potency against caspase-3 with more than 120fold selectivity over caspase-7
-
methyl N-[[4-methyl-1,3-dioxo-2-(1,3,5-trimethyl-1H-pyrazol-4-yl)-2,3-dihydro-1H-pyrrolo[3,4-c]quinolin-8-yl]sulfonyl]-D-phenylalaninate
-
50% inhibition at 0.000023 mM
methyl [4-methyl-8-(morpholin-4-ylsulfonyl)-1,3-dioxo-1,3-dihydro-2H-pyrrolo[3,4-c]quinolin-2-yl]acetate
-
50% inhibition at 0.000016 mM
methyl [4-methyl-8-(morpholin-4-ylsulfonyl)-1,3-dioxo-1,3-dihydro-2H-pyrrolo[3,4-c]quinolin-2-yl]propionate
-
50% inhibition at 0.000037 mM
MX-1013
-
-
-
myricetin
-
myricetin directly interacts with the active site of caspase-3 via three hydrogen bonds, via two hydroxyl groups on the B ring of myricetin interacting with Glu123 and the ether oxygen on the C ring interacting with Arg207, and myricetin directly inhibits caspase-3 activity, thereby inhibiting glutamate-induced cell death, but myricetin inhibits glutamate-induced neuronal toxicity by multiple biochemical pathways, e.g. inhibition of NMDA receptor 1 Ser-890 phosphorylation, overview. Molecular docking analysis by Monte Carlo and molecular dynamics simulations
N-(2-bromophenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(2-fluorobenzyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(2-fluorophenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(2-hydroxyethyl)-4-methyl-1,3-dioxo-2-(1,3,5-trimethyl-1H-pyrazol-4-yl)-2,3-dihydro-1H-pyrrolo[3,4-c]quinoline-8-sulfonamide
-
50% inhibition at 0.000020 mM
N-(2-methoxybenzyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(2-methoxyethyl)-4-methyl-1,3-dioxo-2-(1,3,5-trimethyl-1H-pyrazol-4-yl)-2,3-dihydro-1H-pyrrolo[3,4-c]quinoline-8-sulfonamide
-
50% inhibition at 0.000021 mM
N-(2-methoxyphenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(2-methoxyphenyl)-N'-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)succinamide
-
50% inhibition at 113 nM, comparison with inhibitory effect on caspase-2, caspase-6, caspase-7, caspase-8, papain, proteasome, trypsin and thrombin
N-(2-nitrophenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(3-bromophenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(3-ethoxyphenyl)-N'-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)succinamide
-
50% inhibition at 55 nM
N-(3-fluorobenzyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(3-fluorophenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(3-methoxybenzyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(3-methoxyphenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(3-propyloxyphenyl)-N'-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)succinamide
-
50% inhibition at 71 nM
N-(4-benzoylphenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(4-bromophenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(4-fluorobenzyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(4-fluorophenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(4-iodophenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(4-methoxybenzyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(4-methoxyphenyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(5-methylpyridin-2-yl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-(furan-2-ylmethyl)-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-acetyl-3-(pyridin-3-yl)-L-alanyl-N-[(3S)-1-[[(2S)-1-([(2S)-1-carboxy-4-[(2,6-dimethylbenzoyl)oxy]-3-oxobutan-2-yl]amino)-5-methyl-1-oxohexan-2-yl]amino]-5-methyl-1-oxohexan-3-yl]-L-alpha-asparagine
-
low nanomolar potency against caspase-3 with more than 30fold selectivity over caspase-7
N-acetyl-Asp-Glu-Val-Asp-aldehyde
-
a caspase-3 inhibitor, i.e. DEVD-CHO, partially inhibits the DNA fragmentation and growth-inhibition induced by inotodiol
N-acetyl-Asp-Glu-Val-Asp-CHO
-
-
N-acetyl-DEVD-CHO
-
-
N-acetyl-L-alpha-aspartyl-L-alanyl-N-[(1S)-1-(carboxymethyl)-2-oxo-5-phenylpentyl]-L-valinamide
-
50% inhibition at 2 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer
N-acetyl-L-alpha-aspartyl-L-alanyl-N-[(1S)-3-(benzylsulfanyl)-1-(carboxymethyl)-2-oxopropyl]-L-valinamide
-
50% inhibition at 0.5 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-N-[(1S)-1-(carboxymethyl)-2-oxo-3-phenylpropyl]-L-valinamide
-
comparison with inhibition of caspase-7
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-N-[(1S)-1-(carboxymethyl)-2-oxo-4-phenylbutyl]-L-valinamide
-
comparison with inhibition of caspase-7
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-N-[(1S)-1-(carboxymethyl)-2-oxoheptyl]-L-valinamide
-
comparison with inhibition of caspase-7
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-N-[(1S)-1-(carboxymethyl)-2-oxooctyl]-L-valinamide
-
comparison with inhibition of caspase-7
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-N-[(1S)-1-(carboxymethyl)-4-(2,5-dimethylphenyl)-2-oxobutyl]-L-valinamide
-
comparison with inhibition of caspase-7
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-N-[(1S)-1-(carboxymethyl)-4-(3-methylphenyl)-2-oxobutyl]-L-valinamide
-
-
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-N-[(1S)-2-carboxy-1-formylethyl]-L-valinamide
-
50% inhibition at 27 nM. Comparison of inhibition with caspase 1, caspase 7, caspase 6 and with induction of apoptosis. Increase in stability of otherwise rapidly degraded enzyme heterotetramer
N-acetyl-L-alpha-aspartyl-L-valyl-N-[(1S)-2-carboxy-1-[[(4-methylphenyl)(nitroso)amino]methyl]ethyl]-L-alaninamide
-
-
N-acetyl-L-aspartyl-L-valyl-N-[(1S)-2-carboxy-1-[[(4-methylphenyl)(nitroso)amino]methyl]ethyl]-L-alaninamide
-
-
N-allyl-N'-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)succinamide
-
50% inhibition at 44 nM
N-alpha-tosyl-L-lysinyl-chloromethylketone
-
TLCK, a serine protease inhibitor and potent but nonspecific inhibitor of mature caspases, TLCK has no or only slight effect on caspase-3 processing, but TLCK substantially inhibits caspase-3 enzymatic DEVDase activity, but does not prevent cells from death
N-benxylozycarbonyl-tLeu-Asp
-
a peptide adehyde, competitively inhibits human caspase-3 activity in vitro. Z-tLeu-Asp-H impairs apoptosis in human DLD-1 colon adenocarcinoma cells without affecting caspase-8, in vivo effects, overview
N-benxylozycarbonyl-tLeu-Val-Asp
-
a peptide adehyde, competitively inhibits human caspase-3 activity in vitro
N-benxylozycarbonyl-Val-tLeu-Asp
-
a peptide adehyde, competitively inhibits human caspase-3 activity in vitro
N-benzyl-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-benzyloxycarbonyl-VAD-fluoromethyl ketone
-
a general caspase inhibitor
N-benzyloxycarbonyl-VAD-fluoromethylketone
-
a irreversible caspase inhibitor
N-benzyloxycarbonyl-Val-Ala-Asp-fluoromethylketone
-
-
N-benzyloxycarbonyl-valyl-alanyl-aspartic-acid fluoromethyl ketone
-
-
N-butyl-(S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
N-carbobenzyloxy-D(OMe)E(OMe)VD(OMe)-fluoromethyl ketone
-
a caspase-3 inhibitor
N-carbobenzyloxy-DEVD-fluoromethyl ketone
N-carbobenzyloxy-VAD(OMe)-fluoromethyl ketone
-
a Pan caspase inhibitor
N-carbobenzyloxy-VAD-fluoromethyl ketone
N-ethyl-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-propyl-(S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin
-
-
N-propyl-N'-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-yl)succinamide
-
50% inhibition at 59 nM
N-tosyl-L-phenylalaninyl-chloromethylketone
-
TPCK, a serine protease inhibitor and potent but nonspecific inhibitor of mature caspases, enhances caspase-3 processing although it substantially inhibits caspase-3 enzymatic DEVDase activity in HL-60 cells exposed to various cell death inducing stimuli, but does not prevent cells from death, overview
N-[2-(4-methylpiperazin-1-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[2-(morpholin-4-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[3-(4-methylpiperazin-1-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[3-(morpholin-4-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[4-(1,3-dioxolan-2-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[4-(4-methylpiperazin-1-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[4-(morpholin-4-yl)benzyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[4-(morpholin-4-yl)phenyl]-2-(3-oxo-1,2-benzothiazol-2(3H)-yl)acetamide
-
-
N-[4-(morpholin-4-yl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[4-(morpholin-4-ylsulfonyl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl]-3-oxo-1,2-benzothiazole-2(3H)-carboxamide
-
-
N-[6-[([3-carboxy-2-[6-(diethylamino)-3-(diethyliminio)-9a,10a-dihydro-3H-xanthen-9-yl]phenyl]carbamothioyl)amino]hexanoyl-]3-(pyridin-3-yl)-L-alanyl-N-[(3S)-1-[(2S)-1-[(2S)-1-carboxy-4-[(5-methylthiophen-2-yl)carbonyl]oxy]-3-oxobutan-2-yl]amino]-1-oxo
-
low nanomolar potency against caspase-3 with 140fold selectivity over caspase-7
-
peroxynitrite
-
0.01 mM, 50% inhibition
pralnacasan
-
-
Rho-DEVD-AOMK
-
-
-
RU36384/VRT-18858
-
-
-
S-nitrosoglutathione
-
0.1 mM, complete inhibition
sodium 4-methyl-1,3-dioxo-2-(1,3,5-trimethyl-1H-pyrazol-4-yl)-2,3-dihydro-1H-pyrrolo[3,4-c]quinoline-8-sulfonate
-
50% inhibition at 0.00014 mM
spermine-NO
-
1 mM, complete inhibition
survivin
-
taurocholate
-
at low concentrations of 0.00001-0.1 mM it increases caspase-3 activity, but at larger doses of 0.5-10 mM it reverses stimulation to inhibition. It inhibits the caspase-3 pathway and prevents ethanol-induced caspase-3 activation leading to inhibition of apoptosis, overview
triptolide
-
a diterpenoid triepoxide derived from the herb Tripterygium wilfordii that is used as a natural medicine in China, activates caspase-3 4-119fold in KB cells, 4-70fold in SCC25 cells, and 7.5-90.5fold in OEC-M1 cells, all cancer cells, within 2 days, overview
Tyr-Val-Ala-Asp-chloromethylketone
-
-
Val-Ala-Asp-fluoromethylketone
-
-
Val-Glu-Ile-Asp-aldehyde
-
IC50 for membrane enzyme: 34 nM
VhhCasp31
-
reduces the enzyme activity by 39% at 0.0047 mM and by 85.5% at 0.0145 mM, which is a concentration three times that of caspase 3, the VHH proteins, expresed in SHSY-5Y cells and isolated from heavy chain antibody variable domain, i.e. VHH phage display library, are specific to caspase 3 and antagonist and agonist of apoptosis, effects of transiently-expressed VhhCasp31 and VhhCasp32 intrabodies on oxidative-stress-induced apoptosis in SHSY-5Y cells, overview
-
VX-765
-
-
X inhibitor of apoptosis protein
-
recombinant, a member of the inhibitor of apoptosis protein family, inhibits caspase-3
-
XIAP
-
inhibitor of apoptosis
-
XIAP inhibitors
-
peptide inhibitors
-
Z-Asp-2,6-dichlorobenzoyloxymethylketone
-
a caspase-3-specific inhibitor
-
Z-DEVD-fluoromethylketone
-
a caspase 3 specific inhibitor
Z-IETD-fluoromethylketone
-
a caspase 8 specific inhibitor, delays the activation of caspase 3 and caspase 9 significantly
Z-VAD-fluoromethylketone
Zn2+
-
-
[4-methyl-8-[(2-nitropyrrolidin-1-yl)sulfonyl]-1,3-dioxo-2,3-dihydro-1H-cyclopenta[c]quinolin-2-yl](oxo)acetyl chloride
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,2-benzenedithiol
-
4-5fold activation
1,3-benzenedithiol
-
6fold activation
2-mercaptoethanol
-
half-maximal activation at 1.4 mM
2-methoxyestradiol
-
increases the enzyme activity 2fold at 100 nM
3-[(dodecylthiocarbonyl)methyl]glutarimide
-
-
4,4-thiobisbenzenethiol
-
4-5fold activation
actinomycin D
-
significantly activates caspase-3
arachidonic acid
-
-
azinomycin epoxide
-
i.e. (2S,3S)-benzyl 3,4-epoxy-2-(3-methoxy-5-methyl-1-naphthoyloxy)-3-methylbutanamide, leads to activation and apoptosis in THP-1 cells in a p53-independent manner, while human apoptosis signal-regulating kinase 1, ASK1, is highly required for caspase-3 activation by (2S,3S)-benzyl 3,4-epoxy-2-(3-methoxy-5-methyl-1-naphthoyloxy)-3-methylbutanamide, transient expression of the dominant-negative human ASK1 with kinase-dead domain in THP-1 cells abolishes the caspase-3 activating effect of azinomycin epoxide, overview
-
C2-ketoCer
-
i.e. (2S,4E)-2-acetylamino-3-oxo-4-octadecen-1-ol, a ceramide analogue, activates caspase-3 and induces apoptosis
-
carboxyfluorescein-valyl-alanyl-aspartic-acid fluoromethyl ketone
-
the FAM-peptide irreversibly binds to active caspases
-
cisplatin
-
with or without pre-treatment with HA14-1 it increases the cleavage of caspase-3
cytochrome c
dithiothreitol
-
half-maximal activation at 1.1 mM
doxorubicin
-
augments caspase-3 activity
doxorubicin/2-methoxyestradiol
-
both in combination activate the enzyme 27fold
-
FADD
-
gamma-linolenic-acid
-
-
homocysteine
-
induces the enzyme activation 2.5fold and 4fold in endothelial progenitor cells at 0.1 mM and 0.2 mM, respectively. Vitamin B6, and B9 significantly impair homocysteine-mediated EPC caspase-3 activation in vitro, and inhibitor N-carbobenzyloxy-VAD-fluoromethyl ketone highly reduces the activating effect, overview
Lactic acid
-
induces the activation of caspase-3 in keratinocytes, the activation can be inhibited by N-carbobenzyloxy-VAD-fluoromethyl ketone, overview
linoleic acid
-
-
Mch4
-
activation of CPP32
-
oleic acid
-
-
paclitaxel
-
pre-treatment of cells with HA14-1 followed by paclitaxel induces cleavage of pro-caspase-3 to active form
palmitic acid
-
-
pancreatic derived factor
-
islet specific cytokine, capable of inducing apoptosis, increases levels of cleaved CASP3 in beta-TC3 cells
-
staurosporine
-
in myotubes, staurosporine increases proteasome activity by 38% and stimulates cleavage of proteasome subunits, Rpt2, Rpt6, and Rpn2. Rpt5 and Rpn10 subunits are not cleaved in staurosporine-treated myotubes
stearic acid
-
-
TNF-alpha
-
induces caspase-3 activation
-
TNF-alpha/irradiation
-
leads to an increase of caspase-3, administration of TNF-alpha to non-irradiated hepatocytes does not lead to an increased activity of caspase-3, administration of TNF-alpha to non-irradiated hepatocytes does not lead to an increased activity of caspase-3. Irradiation induces TNF-alpha-mediated activation of caspase-3, and apoptosis in hepatocytes. Apoptosis induction is prevented by IkappaB antisense oligonucleotides mediated by suppression of caspases-3 activation, overview
-
trichothecin
-
trichothecin increases caspase-9, EC 3.4.22.62, expression and caspase-3 activity, and induces apoptosis of HepG2 cells via caspase-9 mediated activation of the mitochondrial death pathway
VhhCasp32
-
increases the enzyme activity by 38% at 0.0047 mM, the VHH proteins, expresed in SHSY-5Y cells and isolated from heavy chain antibody variable domain, i.e. VHH phage display library, are specific to caspase 3 and antagonist and agonist of apoptosis, effects of transiently-expressed VhhCasp31 and VhhCasp32 intrabodies on oxidative-stress-induced apoptosis in SHSY-5Y cells, overview
-
xanthorrhizol
-
a natural sesquiterpenoid compound isolated from the rhizome of Curcuma xanthorrhizza, modulates MDA-MB-231 cell apoptosis through the mitochondria-mediated pathway subsequent to the disruption of mitochondrial transmembrane potential, release of cytochrome c, activation of caspase-3 and caspase-9, and the modulation of PARP-1 protein, overview
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0016
5'-tetramethylrhodamine-5(6)-carboxamide-DEVD-cyanine 5
-
pH and temperature not specified in the publication
0.0337
Ac-DEVD-4-methylcoumarin 7-amide
-
pH 7.5, 25°C
0.011
acetyl-DEVD-4-nitroanilide
-
pH 7.5, 30°C
0.005 - 10.7
acetyl-DEVD-7-amido-4-methylcoumarin
0.044
acetyl-DQMD-4-nitroanilide
-
pH 7.5, 30°C
0.067
acetyl-L-Asp-L-Glu-L-Val-L-Asp-4-nitroanilide
-
pH 7.5, 22°C
0.0048 - 0.0335
acetyl-L-Asp-L-Glu-L-Val-L-Asp-7-amido-4-methylcoumarin
1.6
acetyl-L-Asp-L-Met-L-Gln-L-Asp-4-nitroanilide
-
pH 7.5, 22°C
0.222
acetyl-L-Asp-L-Val-L-Ala-L-Asp-4-nitroanilide
-
pH 7.5, 22°C
0.147
acetyl-L-Leu-L-Asp-L-Val-L-Ala-L-Asp-4-nitroanilide
-
pH 7.5, 22°C
0.164
acetyl-L-Val-L-Asp-L-Val-L-Ala-L-Asp-4-nitroanilide
-
pH 7.5, 22°C
0.2
acetyl-VDQMDGW-amide
-
pH 7.5, 30°C
0.067
acetyl-VDVAD-4-nitroanilide
-
pH 7.5, 30°C
0.25
acetyl-VEID-4-nitroanilide
-
pH 7.5, 30°C
0.51
acetyl-VQVD-4-nitroanilide
-
pH 7.5, 30°C
0.37
acetyl-YEVD-4-nitroanilide
-
pH 7.5, 30°C
29
acetyl-YVAD-4-nitroanilide
-
pH 7.5, 30°C
0.002 - 0.0255
benzoyl-L-Asp-L-Glu-L-Val-L-Asp-7-amido-4-methylcoumarin
0.0625
DEVD-4-nitroanilide
-
-
0.00073
DEVD-FQ
-
pH and temperature not specified in the publication
0.0023
DEVD-NucView488
-
-
0.00077
DW3-FQ
-
pH and temperature not specified in the publication
additional information
additional information
-
stopped-flow and steady-state kinetic kinetics
-