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Information on EC 3.4.24.86 - ADAM 17 endopeptidase and Organism(s) Homo sapiens and UniProt Accession P78536

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     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.24 Metalloendopeptidases
                3.4.24.86 ADAM 17 endopeptidase
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Homo sapiens
UNIPROT: P78536 not found.
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
adam17, adam-17, tnf-alpha converting enzyme, tace/adam17, tumor necrosis factor-alpha converting enzyme, tumor necrosis factor-alpha-converting enzyme, a disintegrin and metalloprotease 17, metalloproteinase adam17, tumor necrosis factor alpha-converting enzyme, tumor necrosis factor alpha converting enzyme, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
(TACE/ADAM17/CD156q)
247
-
(TACE:ADAM17)
247
-
a disintegrin and metalloprotease 17
ADAM-17
ADAM17 proteinase
-
-
-
-
ADAM17/tumor necrosis factor-alpha (TNF-A)converting enzyme
247
-
ADAMTS-2
247
-
CD156
247
-
H-TACE
247
-
human TACE B
247
-
metalloprotease TACE
-
-
-
-
metalloprotease-disintegrin tumour necrosis factor alpha convertase
247
-
metalloproteinase ADAM17
-
-
-
-
pro tumor necrosis factor cleavage enzyme
-
-
-
-
pro-tumor necrosis factor-alpha-processing enzyme
-
-
-
-
proteinase, pro-tumor necrosis factor (9CI)
-
-
-
-
sheddase
247
-
TACE proteinase
-
-
-
-
TACE/ADAM17
247
-
TNF-alpha convertase
-
-
-
-
TNF-alpha converting enzyme
TNF-alpha processing protease
-
-
-
-
tumor necrosis factor alpha convertase
-
-
-
-
tumor necrosis factor alpha converting enzyme
247
-
tumor necrosis factor alpha-converting enzyme
tumor necrosis factor-alpha converting enzyme
tumor necrosis factor-alpha-converting enzyme
247
-
tumour necrosis factor alpha-converting enzyme
247
-
CAS REGISTRY NUMBER
COMMENTARY hide
151769-16-3
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
(EDANS)-ELAQAVRSSSRK-(DABCYL) + H2O
?
show the reaction diagram
-
TNF-alpha derived substrate
-
-
?
(EDANS)-EPLAQAVRSSSK-(DABCYL) + H2O
?
show the reaction diagram
-
TNF-alpha derived substrate
-
-
?
amphiregulin + H2O
?
show the reaction diagram
-
ADAM17, but not related ADAM10, is required for amphiregulin, TGF-alpha, and TNFR1 shedding
-
-
?
CD16 + H2O
?
show the reaction diagram
-
substrates CD16a and CD16b are IgG Fc receptors expressed by human natural killer cells and neutrophils, respectively. Substrates contain three separate cleavage sites in close proximity at P1/P1' positions Ala195/Val196, Val196/Ser197, and Thr198/Ile199, revealing a membrane proximal cleavage region in CD16. Mutation S197P effectively blocks CD16a and CD16b cleavage in cell-based assays. Mutant CD16a/S197P is resistant to cleavage when expressed in cells. The S197P mutation does not disrupt IgG binding by the receptor or its activation of NK92 cells by antibody-treated tumor cells
-
-
?
CD16b + H2O
?
show the reaction diagram
-
human IgG Fc receptor CD16, i.e. FcgammaRIII. CD16b plasma levels are significantly decreased in patients administered a selective inhibitor targeting the metalloproteases ADAM10 and ADAM17. Inhibition of ADAM17 significantly blocks the cleavage of CD16b following neutrophil activation and apoptosis
-
-
?
cell surface VEGF receptor Flt + H2O
?
show the reaction diagram
-
-
release of an N-terminal extracellular fragment which can antagonize the effects of vascular endothelial growth factor, substrate can be cleaved to release an N-terminal extracellular fragment. Overexpression of ADAM10, EC 3.4.24.81, and ADAM17 increase cleavage while knockdown of ADAM10 and ADAM17 reduce N-terminal cleavage
-
?
CSF-1 receptor + H2O
?
show the reaction diagram
-
TACE cleaves the receptor between residues Gln503 and Ser504. Replacement of fourteen residues at the end of the CSF-1 extracellular domain blocks TACE cleavage
-
-
?
Glu(EDANS)-Pro-Leu-Ala-Gln-Ala-Val-Arg-Ser-Ser(4O-(beta-D-Gal-(1->3)-alpha-D-GalNAc))-Ser-Lys(DABCYL) + H2O
Glu(EDANS)-Pro-Leu-Ala-Gln-Ala + Val-Arg-Ser-Ser(4O-(beta-D-Gal-(1->3)-alpha-D-GalNAc))-Ser-Lys(DABCYL)
show the reaction diagram
-
-
-
-
?
Glu(EDANS)-Pro-Leu-Ala-Gln-Ala-Val-Arg-Ser-Ser-Ser-Lys(DABCYL) + H2O
Glu(EDANS)-Pro-Leu-Ala-Gln-Ala + Val-Arg-Ser-Ser-Ser-Lys(DABCYL)
show the reaction diagram
-
-
-
-
?
interleukin-6 receptor + H2O
?
show the reaction diagram
-
the cleavage site by ADAM17 is LPVQ357-/-DSSV, N-linked glycosylation sites are: Asn55, Asn93, Asn221, Asn350
-
-
?
PLAAAVFSS + H2O
PLAAA + VFSS
show the reaction diagram
-
mutant peptide derived from TNF-alpha, very poor substrate
-
-
?
PLAMAVMSS + H2O
PLAMA + VMSS
show the reaction diagram
-
mutant peptide derived from TNF-alpha, very poor substrate
-
-
?
PLAQAVRSS + H2O
PLAQA + VRSS
show the reaction diagram
-
peptide derived from TNF-alpha
-
-
?
Pro-BTC + H2O
?
show the reaction diagram
-
the cleavage site by ADAM17 is CVVA31-/-DGNS, N-linked glycosylation site is Asn34
-
-
?
pro-EPR + H2O
?
show the reaction diagram
-
the cleavage site by ADAM17 is DNPR59-/-VAQV, N-linked glycosylation site is Asn47
-
-
?
pro-HB-EGF + H2O
?
show the reaction diagram
-
the cleavage site by ADAM17 is RKVR62-/-DLQE, O-linked glycosylation sites are Thr75 and Thr85
-
-
?
pro-TGFalpha + H2O
?
show the reaction diagram
-
the cleavage site by ADAM17 is VAAA39-/-VVSH, N-linked glycosylation site is Asn25
-
-
?
pro-tumor necrosis factor alpha + H2O
?
show the reaction diagram
-
with and without a glycan moiety attached, glycosylation increases the enzyme activity. The cleavage site of TNFalpha by ADAM17 is only four residues away from a glycosylated residues, whereas glycosylation occurs 14 residues away from the TGFalpha cleavage site. Cleavage site for ADAM-17 is LAQA76-/-VRSS, O-linked glycosylation site is Ser80
-
-
?
proheparin-binding EGF-like growth factor + H2O
?
show the reaction diagram
-
-
cleavage occurs between residues RKVR62-DLQE. Substrate shows O-linked glycosylation 13 residues apart from scissile bond
-
?
proTNF-alpha + H2O
soluble TNF-alpha + H2O
show the reaction diagram
-
-
cleavage occurs between residues LAQA76-VRSS. Substrate shows O-linked glycosylation 4 residues apart from scissile bond
-
?
protransforming growth factor alpha + H2O
?
show the reaction diagram
-
-
cleavage occurs between residues AAA39-VVSH. Substrate shows N-linked glycosylation 14 residues apart from scissile bond
-
?
S80-glycosylated (EDANS)-ELAQAVRSSSRK-(DABCYL) + H2O
?
show the reaction diagram
-
TNF-alpha derived substrate
-
-
?
S80-glycosylated (EDANS)-EPLAQAVRSSSK-(DABCYL) + H2O
?
show the reaction diagram
-
TNF-alpha derived substrate
-
-
?
syndecan-1 + H2O
?
show the reaction diagram
-
both ADAM10 and ADAM17 contribute to SDC1 shedding
-
-
?
TGF-alpha + H2O
?
show the reaction diagram
-
ADAM17, but not related ADAM10, is required for amphiregulin, TGF-alpha, and TNFR1 shedding
-
-
?
TNF-alpha + H2O
?
show the reaction diagram
-
-
-
-
?
transferrin receptor protein 1 + H2O
?
show the reaction diagram
-
-
cleavage occurs between residues ECER100-LAGT. Substrate shows O-linked glycosylation 4 residues apart from scissile bond
-
?
TRP1 + H2O
?
show the reaction diagram
-
the cleavage site by ADAM17 is ECER100-/-LAGT, O-linked glycosylation sites are: Thr104, Asn251, Asn317, Asn727
-
-
?
tumor necrosis factor receptor 1 + H2O
?
show the reaction diagram
-
ADAM17, but not related ADAM10, is required for amphiregulin, TGF-alpha, and TNFR1 shedding
-
-
?
(7-methoxycoumarin-4-yl)-acetyl-KSPLAQA-VRSSSRK(2,4-dinitrophenyl)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
(7-methoxycoumarin-4-yl)-acetyl-Pro-Leu-Ala-Gln-Ala-Val-[N-3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl]-Arg-Ser-Ser-Ser-Arg-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
(7-methoxycoumarin-4-yl)-acetyl-SPLAQAVRSSSRK-(2,4-dinitrophenyl)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
(7-methoxycoumarin-4-yl)acetyl-Ser-Pro-Leu-Ala-Gln-Ala-Val-Arg-Ser-Ser-Ser-Arg-Lys(Dnp)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
26 kDa proTNF-alpha + H2O
17 kDa soluble TNF-alpha + ?
show the reaction diagram
-
-
-
-
?
4',5'-dimethoxyfluoresceinyl-SPLAQAVRSSSR-cys(4-(3-succinimid-1-yl)fluorescein)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-(yl)acetyl-Pro-Leu-Ala-Gln-Ala-Val-Arg-Ser-Ser-Ser-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl-Arg-NH2 + H2O
?
show the reaction diagram
-
an internally quenched peptide substrate is used
-
-
?
7-methoxycoumarin-4-yl-acetyl-Lys-Pro-Leu-Gly-Pro-Leu-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl-Ala-Arg + H2O
?
show the reaction diagram
-
-
-
-
?
75kDaTNFR2 + H2O
?
show the reaction diagram
-
-
-
-
?
acetyl-SPLAQAVRSSSR-COOH + H2O
acetyl-SPLAQA + VRSSSR-COOH
show the reaction diagram
-
-
-
-
?
Alzheimer's disease amyloid precursor protein + H2O
?
show the reaction diagram
amphiregulin + H2O
?
show the reaction diagram
-
-
-
-
?
amyloid-protein precursor + H2O
?
show the reaction diagram
-
-
-
-
?
beta-amyloid precursor protein + H2O
?
show the reaction diagram
c-KLR + H2O
?
show the reaction diagram
-
-
-
-
?
CD30 + H2O
?
show the reaction diagram
cellular prion protein PrPc + H2O
?
show the reaction diagram
-
-
-
-
?
Dpa-SPLAQAVRSSSR-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
endothelial protein C receptor + H2O
?
show the reaction diagram
-
-
-
-
?
FcalphaR + H2O
?
show the reaction diagram
-
i.e. Fc receptor for immunoglobulin A
-
-
?
fractalkine + H2O
?
show the reaction diagram
GHR + H2O
?
show the reaction diagram
-
-
-
-
?
glycoprotein Ibalpha + H2O
?
show the reaction diagram
glycoprotein V + H2O
?
show the reaction diagram
-
-
-
-
?
heparin-binding EGF-like growth factor + H2O
?
show the reaction diagram
-
ADAM17 may be involved in heparin-binding EGF-like growth factor cleavage in response to injury
-
-
?
heparin-binding epidermal growth factor-like growth factor + H2O
?
show the reaction diagram
-
-
-
-
?
HER-4 Jma + H2O
?
show the reaction diagram
-
-
-
-
?
intercellular cell adhesion molecule-1 + H2O
?
show the reaction diagram
-
-
-
-
?
interleukin (IL)-1R-II + H2O
?
show the reaction diagram
interleukin-6-receptor + H2O
?
show the reaction diagram
-
-
-
-
?
KL-1 + H2O
?
show the reaction diagram
-
-
-
-
?
L-selectin + H2O
?
show the reaction diagram
LAQAVRSSSR + H2O
?
show the reaction diagram
-
fluorimetric assay for TACE, fluorogenic substrate, a 10-amino-acid peptide capped with an o-aminobenzoyl group on the N-terminal end and with a 3-(2,4-dinitrophenyl)-L-2,3-diaminopropionic amide group on the C-terminal end, enzymatic conversion of the substrate results in a fluorescence enhancement of 11fold
-
-
?
macrophage colony-stimulating factor receptor M-CSFR + H2O
?
show the reaction diagram
-
-
-
-
?
Mca-PLAQAV-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide-RSSSR-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
MHC class I-related chain + H2O
?
show the reaction diagram
-
i.e. transmembrane protein expressed in pathological conditions, ligands for the activating receptor NKG2D found on cytotoxic lymphocytes. The recruitment of both enzyme and substrate to detergent-resistant membrane microdomains is crucial for efficient proteolysis
-
-
?
NH2-LAQAVRSSSR-OH + H2O
?
show the reaction diagram
-
uncapped counterpart of the fluorogenic substrate
-
-
?
Notch 1 + H2O
?
show the reaction diagram
-
ADAM17 is required for Notch1 receptor proteolysis in NSCLC cells in vitro and in vivo
-
-
?
notch 1 receptor + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl-LAQAFRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
o-aminobenzoyl-LAQA + FRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide
show the reaction diagram
-
enzymatic cleavage 22%
-
-
?
o-aminobenzoyl-LAQAIRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
o-aminobenzoyl-LAQA + IRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide
show the reaction diagram
-
enzymatic cleavage 66%
-
-
?
o-aminobenzoyl-LAQALRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
o-aminobenzoyl-LAQA + LRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide
show the reaction diagram
-
enzymatic cleavage 92%
-
-
?
o-aminobenzoyl-LAQAVRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
o-aminobenzoyl-LAQA + VRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide
show the reaction diagram
-
enzymatic cleavage 90%
-
-
?
o-aminobenzoyl-LAQFVRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
o-aminobenzoyl-LAQF + RSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide
show the reaction diagram
-
enzymatic cleavage 39%
-
-
?
o-aminobenzoyl-LAQGVRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
o-aminobenzoyl-LAQG + VRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide
show the reaction diagram
-
enzymatic cleavage 11%
-
-
?
o-aminobenzoyl-LAQLVRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
o-aminobenzoyl-LAQL + VRSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide
show the reaction diagram
-
enzymatic cleavage 34%
-
-
?
o-aminobenzoyl-LAQVARSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide + H2O
o-aminobenzoyl-LAQVA + RSSSR-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl amide
show the reaction diagram
-
enzymatic cleavage 19%
-
-
?
p55 TNFR1 + H2O
?
show the reaction diagram
p75 tumour necrosis factor receptor + H2O
?
show the reaction diagram
pN-collagen I substrate + H2O
?
show the reaction diagram
-
-
-
-
?
preadipocyte factor 1 + H2O
?
show the reaction diagram
pro amphiregulin + H2O
?
show the reaction diagram
-
TACE is capable of cleaving both N- and C-terminal sites in the pro-amphiregulin ectodomain
-
-
?
pro heparin-binding epidermal growth factor + H2O
?
show the reaction diagram
-
purified soluble TACE cleaves a single site in the juxtamembrane stalk of pro heparin-binding epidermal growth factor
-
-
?
protein C receptor + H2O
?
show the reaction diagram
-
-
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
proTNF-alpha + H2O
soluble TNF-alpha + 9000 Da membrane-bound fragment of TNF-alpha
show the reaction diagram
-
-
-
-
?
RANKL + ?
?
show the reaction diagram
-
-
-
-
?
receptor tyrosine kinase c-Kit + H2O
?
show the reaction diagram
soluble TNF + H2O
?
show the reaction diagram
-
-
-
-
?
soluble TNF receptor 1 + H2O
?
show the reaction diagram
-
-
-
-
?
soluble TNF receptor 2 + H2O
?
show the reaction diagram
-
-
-
-
?
soluble TNF-alpha receptor type 1 + H2O
?
show the reaction diagram
-
-
-
-
?
TNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
TRANCE + H2O
?
show the reaction diagram
-
-
-
-
?
transforming growth factor alpha + H2O
?
show the reaction diagram
transforming growth factor-alpha + H2O
?
show the reaction diagram
-
-
-
-
?
tumour necrosis factor receptor-1 + H2O
?
show the reaction diagram
-
-
-
-
?
tumour necrosis factor receptor-2 + H2O
?
show the reaction diagram
-
-
-
-
?
vascular cellular adhesion molecule-1 + H2O
?
show the reaction diagram
-
-
-
-
?
vasorin + H2O
soluble vasorin + ?
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
Alzheimer's disease amyloid precursor protein + H2O
?
show the reaction diagram
-
TACE is involved in shedding of Alzheimer's disease amyloid precursor protein
-
-
?
glycoprotein Ibalpha + H2O
?
show the reaction diagram
-
ADAM17 is the key enzyme mediating shedding of glycoprotein Ibalpha
-
-
?
Notch 1 + H2O
?
show the reaction diagram
-
ADAM17 is required for Notch1 receptor proteolysis in NSCLC cells in vitro and in vivo
-
-
?
preadipocyte factor 1 + H2O
?
show the reaction diagram
-
TACE is the major protease responsible for conversion of membrane-bound Pref-1 to the biologically active diffusible form
-
-
?
proTNF-alpha + H2O
soluble TNF-alpha + 9000 Da membrane-bound fragment of TNF-alpha
show the reaction diagram
-
-
-
-
?
receptor tyrosine kinase c-Kit + H2O
?
show the reaction diagram
-
ADAM-17 controls mast cell survival by regulating shedding and surface expression of c-Kit
-
-
?
TNF-alpha + H2O
soluble TNF-alpha
show the reaction diagram
vasorin + H2O
soluble vasorin + ?
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Zn2+
-
active site zinc, metalloprotease
Zinc
-
pronounced diversity in electronic and chemical properties between the catalytic zinc sites of tumor necrosis factor-alpha-converting enzyme and matrix metalloproteinases despite their high structural similarity
additional information
-
metalloprotease
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(5S)-4-(cyclopentylmethyl)-5-(4-hydroxybenzyl)-1-[(2S)-1-(2-[[(6S)-6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione
-
90% inhibition at 0.04 mM
(5S)-5-(4-hydroxybenzyl)-1-[(2S)-1-(2-[[(6S)-6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]-4-[2-(tricyclo[3.3.1.13,7]dec-1-yl)ethyl]piperazine-2,3-dione
-
95% inhibition at 0.04 mM
1-[1-[2-[(2,3-dioxo-6-propylpiperazin-1-yl)methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-(4-hydroxybenzyl)-4-[3-adamantylpropyl]piperazine-2,3-dione
-
-
1-[1-[2-[(2,3-dioxo-6-propylpiperazin-1-yl)methyl]pyrrolidin-1-yl]-3-(naphthalen-2-yl)propan-2-yl]-5-(4-hydroxybenzyl)-4-[3-adamantylpropyl]piperazine-2,3-dione
-
-
4-(2-butylbenzyl)-1-[1-[2-[(2,3-dioxo-6-propylpiperazin-1-yl)methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-(4-hydroxybenzyl)piperazine-2,3-dione
-
-
4-(2-butylbenzyl)-1-[1-[2-[(2,3-dioxo-6-propylpiperazin-1-yl)methyl]pyrrolidin-1-yl]-3-(naphthalen-2-yl)propan-2-yl]-5-(4-hydroxybenzyl)piperazine-2,3-dione
-
-
4-(2-butylbenzyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(4-hydroxyphenyl)propan-2-yl]piperazine-2,3-dione
-
-
4-(2-butylbenzyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione
4-(cyclopentylmethyl)-1-[1-[2-[(2,3-dioxo-6-propylpiperazin-1-yl)methyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)propan-2-yl]-5-(4-hydroxybenzyl)piperazine-2,3-dione
-
-
4-(cyclopentylmethyl)-1-[1-[2-[(2,3-dioxo-6-propylpiperazin-1-yl)methyl]pyrrolidin-1-yl]-3-(naphthalen-2-yl)propan-2-yl]-5-(4-hydroxybenzyl)piperazine-2,3-dione
-
-
4-(cyclopentylmethyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(4-hydroxyphenyl)propan-2-yl]piperazine-2,3-dione
-
-
4-(cyclopentylmethyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione
5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(4-hydroxyphenyl)propan-2-yl]-4-[3-adamantylpropyl]piperazine-2,3-dione
-
-
5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(4-hydroxyphenyl)propan-2-yl]-4-[3-adamanylpropyl]piperazine-2,3-dione
-
-
5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]-4-[3-adamantylpropyl]piperazine-2,3-dione
-
-
methyl (6S,7S)-7-(hydroxycarbamoyl)-6-(4-phenylpiperazin-1-ylcarbonyl)-5-azaspiro[2.5]octane-5-carboxylate
-
i.e. INCB7839, selective inhibitor of endopeptidases ADAM-10 and ADAM-17
(1R,2R)-2-(3-phenoxylphenyl)-2-trans-carbomethoxylcyclopropane hydroxamic acid
-
-
(1R,2R)-2-trans-carboisopropoxyl-2-[3-(2-methylquinolin-4-yl)methoxylphenyl]cyclopropane hydroxyamic acid
-
-
(1R,2R)-2-trans-N-benzylaminocarbonyl-2-[3-(2-methylquinolin-4-yl)methoxylphenyl]cyclopropane hydroxyamic acid
-
-
(1R,2R)-2-[3-(3,4-dichlorobenzyloxy)phenyl]-2-trans-carbomethoxylcyclopropane hydroxamic acid
-
-
(1R,2R)-N-hydroxy-2-[(4-methylpiperazin-1-yl)carbonyl]-2-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropanecarboxamide
-
-
(1R,2R)-N1-benzyl-N2-hydroxy-N1-methyl-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2R)-N1-cyclohexyl-N2-hydroxy-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2R)-N2-hydroxy-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]-N1-phenylcyclopropane-1,2-dicarboxamide
-
-
(1R,2R)-N2-hydroxy-N1,N1-dimethyl-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2R)-N2-hydroxy-N1-methyl-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-(3-fluoro-4-[[2-(1-methyl-1H-pyrazol-5-yl)quinolin-4-yl]methoxy]benzyl)-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-(3-fluoro-4-[[2-(methylamino)quinolin-4-yl]methoxy]benzyl)-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[3-fluoro-4-[(2-morpholin-4-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[3-fluoro-4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N2-hydroxy-N1,N1-dimethylcyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[3-fluoro-4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[3-fluoro-4-[(2-pyridin-3-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[3-fluoro-4-[(2-pyrrolidin-1-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[4-(benzyloxy)benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[4-(but-2-yn-1-yloxy)benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-1-[4-[(2-ethylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N1-(piperidin-4-ylmethyl)cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-N1,N1-dimethyl-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-N1,N1-dimethyl-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
(1R,2S)-N2-hydroxy-N1-methyl-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
-
(1S,2R)-2-[[(3R)-3-(dimethylamino)pyrrolidin-1-yl]carbonyl]-N-hydroxy-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
(1S,2R)-2-[[(3S)-3-(dimethylamino)pyrrolidin-1-yl]carbonyl]-N-hydroxy-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
(1S,2R)-N-hydroxy-2-[[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]carbonyl]-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
(1S,2R)-N-hydroxy-2-[[(3S)-3-hydroxypyrrolidin-1-yl]carbonyl]-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
-
(1S,2R)-N-hydroxy-2-{4-[(2-imino-1,2-dihydroquinolin-4-yl)methoxy]benzyl}-2-(methoxycarbonyl)cyclopropanecarboximidic acid
-
-
(1S,2S)-2-((S)-cyano(4-((2-phenylquinolin-4-yl)methoxy)phenyl)methyl)-N-hydroxycyclopropanecarboxamide
-
-
(2R)-5-nitroguanyl-2-([(2R,3S)-2-(cyclohexylmethyl)-3-cyclopropyl-3-[formyl(hydroxy)amino]propanoyl]-amino)-N-(1,3-thiazol-2-yl)pentanamide
-
-
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
-
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[(4-methylcyclohexyl)-methyl]hexanamide
-
-
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[(5-methyl-2-thienyl)methyl]hexanamide
-
-
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutyl-4-methylpentanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl-(hydroxy)amino]-2-isobutyl-4-methylpentanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl-(hydroxy)amino]-2-isobutylhexanamide
-
-
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-6,6,6-trifluoro-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-(cyclohexylmethyl)-3-[formyl(hydroxy)amino]hexanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-(cyclohexylmethyl)-6,6,6-trifluoro-3-[formyl(hydroxy)amino]hexanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-[(1S)-1-[formyl(hydroxy)amino]-2-phenylethyl]-4-methylpentanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[5-methyl-2-thienylmethyl]hexanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]hexanamide
-
-
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
-
(2R,3S)-N-[(1S,2R)-4-nitroguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
-
(2R,3S)-N-{(1R)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl}-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
-
(2S)-2-amino-5-({(E)-amino[(methylsulfonyl)imino]-methyl}amino)-N-(1,3-thiazol-2-yl)pentanamide hydrochloride
-
-
(2S)-2-[(tert-butoxycarbonyl)amino]-5-({(Z)-(methyl-sulfanyl)[(methylsulfonyl)imino]methyl}amino)pentanoic acid
-
-
(2S,3R)-2-[(tert-butoxycarbonyl)amino]-5-{[imino(2-oxido-2-oxohydrazino)methyl]amino}-3-methylpentanoic acid (3R) Nalpha-boc-Ngamma-nitro-3-methyl L-arginine
-
-
(2S,3R)-2-{[(benzyloxy)carbonyl]amino}-3-methyl-5-({(Z)-(methylsulfanyl)[(methylsulfonyl)imino]methyl}-amino)pentanoic acid
-
-
(2S,3R)-5-methanesulfonylguanyl-2-[((2R)-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-4-methylpentanoyl)amino]-3-methyl-N-(1,3-thiazol-2-yl)pentanamide
-
-
(2S,3R)-5-nitroguanyl-2-[((2R)-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-4-methylpentanoyl)amino]-3-methyl-N-(1,3-thiazol-2-yl)pentanamide
-
-
(3S)-4-[[4-(but-2-ynylamino)phenyl]sulfonyl]-N-hydroxy-2,2-dimethylthio-morpholine-3-carboxamide
-
-
(4-bromobut-2-enyloxymethyl)benzene
-
-
(4-methoxyphenyl)acetic acid 4-benzyloxybut-2-enyl ester
-
-
(5R)-5-(2',4'-difluorobiphenyl-4-yl)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5R)-5-(4'-chlorobiphenyl-4-yl)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[2'-(1-methyl-1H-tetrazol-5-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4'-(trifluoromethyl)biphenyl-4-yl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(6-oxo-1,6-dihydropyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(quinolin-6-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[3'-(2-methyl-1,3-thiazol-4-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4'-(1H-pyrazol-3-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1,3-thiazol-2-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-5-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-methyl-2H-indazol-6-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-methylpyridin-4-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(3-phenyl-1,2-oxazol-5-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(4-methyl-2,5-dioxoimidazolidin-4-yl)phenyl]imidazolidine-2,4-dione (non-preferred name)
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrazin-2-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-2-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-4-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrimidin-5-yl)phenyl]imidazolidine-2,4-dione
-
-
(5R)-5-[4-(2-aminopyridin-4-yl)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5R)-5-[4-(3,5-dimethyl-1,2-oxazol-4-yl)phenyl]-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5R)-5-[4-(5-chloro-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
(5S)-5-(4-fluorophenyl)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
1,10-phenanthroline
-
-
1-(1,3-benzoxazol-2-yl)-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
-
-
1-(1H-benzimidazol-2-yl)-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
-
-
1-(2,2-dimethylpropanoyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
1-(2,2-dimethylpropanoyl)-N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]piperidine-4-carboxamide
-
-
1-(2,2-dimethylpropyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
1-(butylsulfonyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
1-but-2-yn-1-yl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
1-ethylpropyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
1-methyl-2-morpholin-4-ylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
1-methylethyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropanecarboxylate
-
-
1-methylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
1-[(4-acetylpiperazin-1-yl)sulfonyl]-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
-
-
2(R)-benzyloxymethyl-N-(2,2-dimethyl-1(S)-methyl-carbamoylpropyl)-3-(S)-(4-methoxyphenyl)succinamic acid
-
-
2-(3-benzyloxyphenyl)-2-trans-carbomethoxylcyclopropane hydroxyamic acid
-
-
2-(6-methyl-2-oxo-2H-chromen-3-ylmethyl)-pent-4-enoic acid hydroxyamide
-
-
2-(N-benzoxycarbonyl)aminoethyl-N-(4-hydroxyamino-4-oxo-2-(isopropylthio)butanoyl)-L-3-(2'-naphthyl)-L-alanyl amide
-
peptidomimetic inhibitor, 54.5% inhibition in in vitro lipopolysaccharide cytotoxicity tests, inhibitory activity in vivo by measuring the expression of mTNFalpha
2-(N-benzoxycarbonyl)aminoethyl-N-(4-hydroxyamino-4-oxo-2-(isopropylthio)butanoyl)-L-3-phenylalanyl-L-alanyl amide
-
peptidomimetic inhibitor, 27.3% inhibition in in vitro lipopolysaccharide cytotoxicity tests, molecular docking studies
2-(N-benzoxycarbonyl)aminoethyl-N-(4-hydroxyamino-4-oxo-2-(phenylthio)butanoyl)-L-3-phenylalanyl-L-alanyl amide
-
peptidomimetic inhibitor, 54.5% inhibition in in vitro lipopolysaccharide cytotoxicity tests
2-benzyl-N-hydroxy-3-(6-methyl-2-oxo-2H-chromen-3-yl)-propionamide
-
-
2-morpholin-4-ylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
2-[3-(2-methylquinolin-4-yl)methoxylphenyl]-2-trans-carboxamidocyclopropane hydroxyamic acid
-
-
2-[3-(2-methylquinolin-4-yl)methoxyphenyl]-2-trans-carbomethoxylcyclopropane hydroxyamic acid
-
-
3(R)-benzyloxymethyl-2-(S)-(4-methoxyphenyl)pent-4-enoic acid
-
-
3(R)-benzyloxymethyl-2-(S)-(4-methoxyphenyl)pent-4-enoic acid (2,2-dimethyl-1-(S)-methylcarbamoylpropyl)amide
-
-
3-(6-bromo-2-oxo-2H-chromen-3-yl)-N-hydroxy-propanamide
-
-
3-(6-chloro-2-oxo-2H-chromen-3-yl)-N-hydroxy-propanamide
-
-
3-(6-tert-butyl-2-oxo-2H-chromen-3-yl)-N-hydroxypropanamide
-
-
3-([[4-(1,3-dihydrofuro[3,4-b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-([[4-(2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-([[4-(2,3-dihydrofuro[2,3-b]quinolin-4-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[([4-[(2,3-dimethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[([4-[(2-cyclopropylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[([4-[(2-ethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[([4-[(3-ethyl-2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
3-[4-[2-(hydroxyamino)-2-oxoethyl]-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidin-1-yl]propanoic acid
-
-
3-[[(4-[[2-(dimethylamino)quinolin-4-yl]methyl]phenyl)carbonyl]amino]-N-hydroxytetrahydro-2H-pyran-2-carboxamide
-
-
4'-[(4R)-4-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2,5-dioxoimidazolidin-4-yl]biphenyl-4-carboxamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(2-methyl-benzoyl)-piperidine-4-carboxylic acid hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(2-methyl-butyryl)-piperidine-4-carboxylic acid hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(propane-2-sulfonyl)-piperidine-4-carboxylic acid hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-isobutyryl-piperidine-4-carboxylic acid hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-pyridin-4-ylmethyl-piperidine-4-carboxylic acid hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-piperidine-1,4-dicarboxylic acid 1-diethylamide 4-hydroxyamide
-
-
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-piperidine-4-carboxylic acid hydroxyamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-(dimethylsulfamoyl)-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(2,5-dichlorothiophen-3-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(2,5-dimethyl-1,3-thiazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dichloropyridin-4-yl)carbonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dichloropyridin-4-yl)methyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dimethyl-1H-pyrazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dimethylisoxazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(5-chlorothiophen-2-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(morpholin-4-ylsulfonyl)piperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(piperidin-1-ylsulfonyl)piperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(pyrrolidin-1-ylsulfonyl)piperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-pyridin-2-ylpiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-pyridin-4-ylpiperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[(2-methyl-1H-imidazol-4-yl)sulfonyl]piperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]sulfonyl]piperidine-4-carboxamide
-
-
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]piperidine-4-carboxamide
-
-
4-[([4-[(1,1-dimethylbut-2-yn-1-yl)oxy]phenyl]sulfonyl)methyl]-N-hydroxy-1-(isopropylsulfonyl)piperidine-4-carboxamide
-
-
4-[2-(hydroxyamino)-2-oxoethyl]-N,N-dimethyl-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidine-1-carboxamide
-
-
4-[4-(4-hydroxy-but-2-ynylamino)-benzenesulfonylmethyl]-4-hydroxycarbamoyl-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)-thiomorpholinecarboxamide
-
IC50: 0.009 mM
5-[(5-methoxy-3-oxo-1,3-dihydro-2H-indazol-2-yl)methyl]-5-phenylimidazolidine-2,4-dione
-
-
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-(2-phenoxyphenyl)imidazolidine-2,4-dione
-
-
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-(3-phenoxyphenyl)imidazolidine-2,4-dione
-
-
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-oxopyrrolidin-1-yl)phenyl]imidazolidine-2,4-dione
-
-
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(morpholin-4-yl)phenyl]imidazolidine-2,4-dione
-
-
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-4-yloxy)phenyl]imidazolidine-2,4-dione
-
-
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrrolidin-1-ylcarbonyl)phenyl]imidazolidine-2,4-dione
-
-
5-[4-(cyclopentyloxy)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
5-[4-(isoquinolin-7-yloxy)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
-
APMA
-
inhibits TACE completely
BB 1101
-
-
BB 1433
-
-
BB 16
-
-
BB 2516
-
-
BB3103
-
-
-
benzyl (1S,2R)-4-({(E)-amino[(methylsulfonyl)imino]-methyl}amino)-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butylcarbamate
-
-
BMS-561392
-
-
CGS 27023
-
-
CT 572
-
-
-
cyclohexyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
cyclohexylmethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
cyclopentyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
cyclopropyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
dithiothreitol
-
-
EGTA
-
1 mM, treatment of cells dramatically inhibits shedding of shedding of FcalphaR, i.e. Fc receptor for immunoglobulin A
EndoH
-
full-length TACE is sensitive to EndoH, mature TACE is resistant
-
ethyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-[(2-methylquinolin-4-yl)methoxy]phenyl]cyclopropanecarboxylate
-
-
ethyl (1R,2S)-1-[3-bromo-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-1-[3-chloro-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-1-[3-fluoro-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-1-[4-[(2-ethylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-phenoxybenzyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-[[2-(2-methylpropyl)quinolin-4-yl]methoxy]benzyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-[[2-(trifluoromethyl)quinolin-4-yl]methoxy]benzyl)cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-phenylpyridin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-pyridin-3-ylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
-
gelastatin hydroxamate
-
-
GI 129471
-
-
GM 6001
-
-
GM6001
GW 3333
GW1988
-
-
-
GW280264X
-
blocks ADAM10 and ADAM17 activity similarly
GW9471
IC-3
-
protects TACE from degradation by inhibiting either TACE itself or another metalloprotease
Immunex compound 3
-
-
JMV 390
-
-
KB-R7785
-
-
L-NG-(2-pyridylsulfonyl)arginine2-aminothiazole amide hydochloride
-
-
L-NG-nitroarginine 2-aminothiazole amide dihydrochloride
-
-
macrocyclic hydroxamic acid
-
-
-
methyl (1R,2R)-1-[3-(2-[3-[(1Z)-buta-1,3-dien-1-yl]phenyl]ethoxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-1-[3-(benzyloxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-1-[3-(but-2-yn-1-yloxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-1-[3-(cyclohexylmethoxy)phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-1-[3-[(4-chlorobenzyl)oxy]phenyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-(3-methoxyphenyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-(3-[[3-(trifluoromethyl)benzyl]oxy]phenyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-(3-[[4-(trifluoromethyl)benzyl]oxy]phenyl)cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(2-methylphenoxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(2-naphthalen-2-ylethoxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(2-phenylethoxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(4-methylphenoxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(naphthalen-2-ylmethoxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-(naphthalen-2-yloxy)phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2R)-2-(hydroxycarbamoyl)-1-[3-[(3-methoxybenzyl)oxy]phenyl]cyclopropanecarboxylate
-
-
methyl (1R,2S)-1-[4-(benzyloxy)benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2S)-1-[4-(but-2-yn-1-yloxy)benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2S)-1-[4-(cyclohexylmethoxy)benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2S)-1-[4-[(2-chlorobenzyl)oxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2S)-1-[4-[(3,4-dichlorobenzyl)oxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
-
methyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-(2-naphthalen-1-ylethoxy)benzyl]cyclopropanecarboxylate
-
-
methyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-(2-naphthalen-2-ylethoxy)benzyl]cyclopropanecarboxylate
-
-
methyl 3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
-
methyl 4'-[(4R)-4-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2,5-dioxoimidazolidin-4-yl]biphenyl-4-carboxylate
-
-
MMP-1
-
-
-
MMP-2
-
-
-
N(R)-[2-(hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-alanine amide
-
IC50: about 0.11 mM
N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
N-hydroxy-2-((6-methoxy-2H-chromen-3-yl)methyl)propanamide
-
-
N-hydroxy-2-(2-oxo-2H-chromen-3-yl)acetamide
-
-
N-hydroxy-2-methyl-3-(6-methyl-2-oxo-2H-chromen-3-yl)-propionamide
-
-
N-hydroxy-3-(2-oxo-2H-chromen-3-yl)propanamide
-
-
N-hydroxy-3-(6-methoxy-2-oxo-2H-chromen-3-yl)propanamide
-
-
N-hydroxy-3-(6-methyl-2-oxo-2H-chromen-3-yl)propanamide
-
-
N-hydroxy-3-[([4-[(2-morpholin-4-ylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-2-carboxamide
-
-
N-hydroxy-3-[([4-[(3-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-2-carboxamide
-
-
N-hydroxy-3-[[(4-[[2-(trifluoromethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-2-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-1-prop-2-yn-1-ylpyrrolidine-3-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydrofuran-3-carboxamide
-
-
N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
-
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]-1-(methylsulfonyl)piperidine-4-carboxamide
-
-
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]-1-propylpiperidine-4-carboxamide
-
-
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]piperidine-4-carboxamide
-
-
N-hydroxy-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]tetrahydro-2H-pyran-4-carboxamide
-
-
N-[(4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]methylcarbamoyl-5-hydroxy-2-methyloct-4-yl]-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]isophthalamide
-
-
N-[1-(1,1-dimethylprop-2-yn-1-yl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(2,2-dimethylpropanoyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(2,2-dimethylpropyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(2-fluoroethyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(3,3-dimethylbutanoyl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-(4,5-dihydro-1,3-thiazol-2-yl)-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-acetyl-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-ethyl-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-tert-butyl-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-[2-(ethylsulfonyl)ethyl]-4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[1-[2-(hydroxyamino)-2-oxoethyl]cyclohexyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-(2-methylpropanoyl)piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-(3-methylbutanoyl)piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-(methylsulfonyl)piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-methylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-phenylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-propanoylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-propylpiperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]-1-[2-(methylsulfonyl)ethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]tetrahydro-2H-pyran-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N-[4-[2-(hydroxyamino)-2-oxoethyl]tetrahydro-2H-pyran-4-yl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
-
-
N-[DL-[2-(hydroxyamino-carbonyl)methyl]-4-methylpentanoyl]-L-3-(tert-butyl)glycyl-L-alanine,2-aminoethylamide
-
-
N-[[1-(hydroxycarbamoyl)cyclohexyl]methyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
-
N1-benzyloxy-2(R)-benzyloxymethyl-N4-(2,2-dimethyl-1(S)-methylcarbamoylpropyl)-3(S)-(4-methoxyphenyl)-succinamide
-
-
N4-(2,2-dimethyl-1(S)-methylcarbamoylpropyl)-N1-hydroxy-2(R)-hydroxymethyl-3(R)-(isobutyl)succinamide
-
-
N4-(2,2-dimethyl-1(S)-methylcarbamoylpropyl)-N1-hydroxy-2(R)-hydroxymethyl-3(S)-(4-methoxyphenyl)succinamide
-
-
N4-(2,2-dimethyl-1(S)-methylcarbamoylpropyl)-N1-hydroxy-2(R)-hydroxymethyl-3(S)-p-tolylsuccinamide
-
-
N4-(2,2-dimethyl-1(S)-methylcarbamoylpropyl)-N1-hydroxy-2(R)-hydroxymethyl-3(S)-phenylsuccinamide
-
-
NaCl
-
dramatic inhibitory effect on the activity of TACE
peptide hydroxamate
-
-
-
peptidomimetic hydroxamate
-
-
-
PKF242-484
-
-
pyridin-4-ylmethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
Ro 31-9790
-
-
Ro 32-7315
-
-
Ro32-7315
-
inhibitor specific for ADAM17, blocks shedding of CD30 antigen from cell membrane and a simultaneous release of soluble CD30
SC 903
-
-
-
SE 205
-
-
succinate
-
-
succinyl hydroxamate
-
-
sulfonamide hydroxamate
-
-
TACE-pro domain
-
pro domain is an inhibitor of the catalytic domain
-
TAPI-1
-
-
TAPI-2
tert-butyl (1S,2R)-4-{[imino(2-oxido-2-oxohydrazino)-methyl]amino}-2-methyl-1-[1,3-thiazol-2-ylaminocarbonyl]butylcarbamate
-
-
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-3-methyl-4-pentenoate
-
-
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-amino-3-methylpentanoate
-
-
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-azido-3-methylpentanoate
-
-
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-hydroxy-3-methylpentanoate
-
-
tert-butyl 3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
-
tert-butyl 3-[4-[2-(hydroxyamino)-2-oxoethyl]-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]piperidin-1-yl]propanoate
-
-
tert-butyl 4-(hydroxycarbamoyl)-4-[[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]methyl]piperidine-1-carboxylate
-
-
tert-butyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
-
tert-butyl 4-([[4-(but-2-ynylamino)phenyl]sulfonyl]methyl)-4-[(hydroxyamino)-carbonyl]piperidine-1-carboxylate
-
-
tert-butyl 4-[([4-[but-2-ynyl(methyl)amino]phenyl]sulfonyl)methyl]-4-[(hydroxyamino)carbonyl]piperidine-1-carboxylate
-
-
tert-butyl(1S)-4-({(Z)-(methylsulfanyl)[(methylsulfonyl)-imino]methyl}amino)-1-[(1,3-thiazol-2-ylamino)carbonyl]butylcarbamate
-
-
TIMP-3
-
TMI-1
-
-
TMI-2
-
complete inhibition at 50 nM
TNF-alpha proteinase inhibitor
-
0.00005 mM
-
tumor necrosis factor-alpha protease inhibitor
-
-
-
tumor necrosis factor-alpha-converting enzyme pro domain
-
inhibition of the tumor necrosis factor-alpha-converting enzyme by its isolated pro domain, IC50: 70 nM
-
[((3R,4S)-4-{[(benzyloxy)carbonyl]}-4-carboxy-3-methylbutyl)amino](imino)methanaminium nitrate (3R) 3-methyl L-arginine nitric acid salt
-
-
[N-hydroxy-1-(isopropylsulfonyl)-4-[(4-[(1-methylbut-2-yn-1-yl)oxy]phenyl]sulfonyl)-methyl]piperidine-4-carboxamide
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
12-HPETE
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i.e. 12-hydroperoxy-5Z,8Z,10E,14Z-eicosatetraenoic acid, a peroxide synthesized in the platelet lipoxygenase pathway, induces TACE-mediated receptor cleavage
anti-Ro/SSA autoantibody
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i.e. antinuclear autoantibodies in the blood directed against Ro/Sjögren's syndrome ribonucleoprotein A antigen. Adalimumab appears to be significantly more efficacious than Etanercept in preventing TACE activation caused by anti-Ro/SSA autoantibodies
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bortezomib
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stimulates ADAM17-catalyzed shedding of CD30, blocks bortezomib-stimulated sCD30 release from L540 cells with an IC50 of approximately 230 nM
glucose oxidase
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oxidative damage via glucose oxidase or hydrogen peroxide activates TACE and induces shedding of its targets, glycoprotein Ibalpha and glycoprotein V, in murine and human platelets. The TACE activation is independent of platelet activation. TACE activation induced by hydrogen peroxide is dependent on p38 mitogen-activated protein kinase signalling, whereas protein kinase C, phosphoinositide 3-kinase, and caspases are not involved. Inhibition of p38 cytoplasmic targets, phospholipase A2 and heat shock protein 27, does not prevent shedding, whereas blocking 12-lipoxygenase or Src kinase slightly inhibits TACE activation
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granulocyte-macrophage colony-stimulating factor
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granulocyte-macrophage colony-stimulating factor GM-CSF and interleukin-4 in combination potently up-regulate tumor necrosis factor-alpha coverting enzyme TACE and activity in monocytes, causing ectodomain shedding of M-CSF receptor
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heparan sulfate
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removal of cell surface heparan sulfate increases TACE activity and TACE-dependent formation of ErbB4 80 kDa intracellular domain
hydrogen peroxide
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interleukin-4
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granulocyte-macrophage colony-stimulating factor GM-CSF and interleukin-4 in combination potently up-regulate tumor necrosis factor-alpha coverting enzyme TACE and activity in monocytes, causing ectodomain shedding of M-CSF receptor
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lipopolysaccharide
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N-formyl-L-methionyl-phenylalanine
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ADAM17 substrates undergo efficient turnover during extended neutrophil activation by N-formyl-L-methionyl-phenylalanine
phorbol 12-myristate-13-acetate
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PMA
phorbol ester
phorbol-12-myristate 13-acetate
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additional information
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