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Literature summary for 3.4.24.B4 extracted from

  • Li, J.J.; Johnson, A.R.
    Selective MMP13 inhibitors (2011), Med. Res. Rev., 31, 863-894.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
additional information MMP13 knockout mice are viable, healthy, and grossly normal. The absence of MMP13, however, delays the endochondral ossification process of skeletal development, knockout phenotype, overview. The mutant mice show hypertrophic chondrocytes within the articular cartilage of trabecular bone that is due to impaired remodeling of the extracellular matrix, and they show reduced apoptosis of the hypertrophic chondrocytes. Tibial cartilage erosion does not progress with time in MMP13 knockout mice Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
(2R,3R)-4-[[4-(2-chloro-4-fluorophenoxy)phenyl]sulfonyl]-N,2-dihydroxy-2-methylmorpholine-3-carboxamide
-
Homo sapiens
(2S,3R)-1-acetyl-N-hydroxy-2-methyl-4-[[4-(2-methylbenzyl)phenyl]sulfonyl]piperidine-3-carboxamide
-
Homo sapiens
(4R)-1-[4-(4-fluorophenoxy)benzyl]-N-hydroxy-2-oxoimidazolidine-4-carboxamide
-
Homo sapiens
(4S)-4-[4-(4-fluorophenoxy)phenyl]-N-hydroxy-5-oxo-D-prolinamide
-
Homo sapiens
1,5-anhydro-2,3-dideoxy-3-[[4-(2,4-dichlorophenoxy)phenyl]sulfonyl]-4-C-(hydroxycarbamoyl)-D-threo-pentitol
-
Homo sapiens
1-(4-amino-2-methylquinolin-6-yl)-3-(4-methoxyphenyl)urea
-
Homo sapiens
1-(4-phenoxyphenyl)-1,7,9-triazaspiro[4.5]decane-2,6,8,10-tetrone
-
Homo sapiens
1-(6-[4-[4-(4-fluorophenyl)-1,3-oxazol-2-yl]phenoxy]pyridin-3-yl)-1,7,9-triazaspiro[4.5]decane-6,8,10-trione
-
Homo sapiens
2-(ethyl[[4-(prop-1-yn-1-yloxy)phenyl]sulfonyl]amino)-5-phenylpentane(thioperox)ic O-acid
-
Homo sapiens
2-fluoro-N-hydroxy-6-([4-[4-(trifluoromethoxy)phenoxy]piperidin-1-yl]sulfonyl)benzamide
-
Homo sapiens
2-[(4-chlorobenzyl)sulfanyl]-6-methylpyrimidin-4-ol competitive Homo sapiens
2-[benzyl[(4-methoxyphenyl)sulfonyl]amino]-N-hydroxy-3,5-dimethylbenzamide WAY- 152177 Homo sapiens
2-[[(4'-chlorobiphenyl-4-yl)oxy]methyl]-N-hydroxy-4-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)butanamide
-
Homo sapiens
2-[[(4'-cyanobiphenyl-4-yl)oxy]methyl]-N-hydroxy-4-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)butanamide
-
Homo sapiens
2-[[(4'-[[(5-bromo-4-methoxy-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]methyl]-3-methylbutanoic acid
-
Homo sapiens
2-[[[4-(4-chlorophenoxy)phenyl]sulfonyl](methyl)amino]-N-hydroxy-3-[(4-methylpiperazin-1-yl)methyl]benzamide
-
Homo sapiens
3-[(4-methoxyphenyl)sulfonyl]propane-1-thiol
-
Homo sapiens
3-[(4-phenoxyphenyl)sulfonyl]cyclohexanethiol
-
Homo sapiens
3-[[4-(phenylsulfanyl)phenyl]sulfonyl]cyclohexanethiol
-
Homo sapiens
4'-aminobiphenyl-4-sulfonamide competitive Homo sapiens
4-(3-[3-[3-(3,4-difluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]prop-2-yn-1-yl]phenyl)butanoic acid
-
Homo sapiens
4-([6-[(4-methoxybenzyl)carbamoyl]-4-oxopyrido[3,4-d]pyrimidin-3(4H)-yl]methyl)benzoic acid a less potent MMP13 inhibitor Homo sapiens
4-([[4-(4-fluorophenoxy)phenyl]sulfonyl]amino)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
Homo sapiens
4-methoxy-N,N'-bis(pyridin-3-ylmethyl)benzene-1,3-dicarboxamide competitive Homo sapiens
4-[2-[4-(4-[[5-(2-ethoxyethyl)-2,4,6-trioxohexahydropyrimidin-5-yl]oxy]phenoxy)phenyl]-1,3-oxazol-4-yl]benzonitrile
-
Homo sapiens
4-[[1-methyl-2,4-dioxo-6-(3-phenylprop-1-yn-1-yl)-1,4-dihydroquinazolin-3(2H)-yl]methyl]benzoic acid noncompetitive, extremely selective for inhibition of MMP13 over all other MMPs Homo sapiens
4-[[4-oxo-6-(3-phenylprop-1-yn-1-yl)quinazolin-3(4H)-yl]methyl]benzoic acid
-
Homo sapiens
4-[[6-(2-[3-[3-(hydroxyamino)-3-oxopropoxy]phenyl]-1,3-oxazol-5-yl)-4-oxoquinazolin-3(4H)-yl]methyl]benzoic acid
-
Homo sapiens
5-(2-ethoxyethyl)-5-[4-[4-(1,3,4-oxadiazol-2-yl)phenoxy]phenoxy]pyrimidine-2,4,6(1H,3H,5H)-trione
-
Homo sapiens
5-(3,4-difluorobenzyl)-7-methyl-4,6-dioxo-N-[[2-(3-sulfanylpropoxy)pyridin-4-yl]methyl]-3a,4,5,6-tetrahydrothieno[3,2-c]pyridine-2-carboxamide
-
Homo sapiens
5-(4-chlorophenoxy)-5-methylpyrimidine-2,4,6(1H,3H,5H)-trione
-
Homo sapiens
5-hexyl-5-(4-phenoxyphenoxy)pyrimidine-2,4,6(1H,3H,5H)-trione
-
Homo sapiens
5-methyl-5-(4-phenoxyphenoxy)pyrimidine-2,4,6(1H,3H,5H)-trione
-
Homo sapiens
5-[4-(1H-imidazol-1-yl)phenyl]-4-methyl-1,2-dihydro-3H-pyrazol-3-one
-
Homo sapiens
benzyl 6-benzyl-5,7-dioxo-6,7-dihydro-5H-[1,3]thiazolo[3,2-c]pyrimidine-2-carboxylate competitive, does not ligate the catalytic zinc, zinc binding is unnecessary to achieve nanomolar affinity, extremely selective for inhibition of MMP13 over all other MMPs Homo sapiens
marimastat a nonselective inhibitor Rattus norvegicus
methyl 3-[4-(1H-imidazol-1-yl)phenyl]propanoate
-
Homo sapiens
additional information structure-function relationships of different inhibitor types, overview. No inhibition by 27, i.e. CGS27023A Homo sapiens
N,N'-bis(3-methylbenzyl)pyrimidine-4,6-dicarboxamide extremely selective for inhibition of MMP13 over all other MMPs Homo sapiens
N,N'-bis(3-methylbenzyl)pyrimidine-4,6-dicarboxamide a MMP13-specific inhibitor Rattus norvegicus
N,N'-bis(pyridin-3-ylmethyl)pyrimidine-4,6-dicarboxamide
-
Homo sapiens
N-([4'-[(1-benzofuran-2-ylcarbonyl)amino]biphenyl-4-yl]sulfonyl)valine
-
Homo sapiens
N-([4'-[([4-[(2-carboxypropan-2-yl)oxy]-1-benzofuran-2-yl]carbonyl)amino]biphenyl-4-yl]sulfonyl)-L-valine
-
Homo sapiens
N-hydroxy-2,2-dimethyl-4-[[4-(pyridin-4-yloxy)phenyl]sulfonyl]thiomorpholine-3-carboxamide
-
Homo sapiens
N-hydroxy-2,6-dimethoxy-3-[[(4-methoxyphenyl)sulfonyl](pyridin-3-ylmethyl)amino]pyridine-4-carboxamide
-
Homo sapiens
N-hydroxy-2-[[(4-methoxyphenyl)sulfonyl](pyridin-3-ylmethyl)amino]-3-methylbenzamide
-
Homo sapiens
N-hydroxy-3-methyl-2-(methyl[[4-(pyridin-4-yloxy)phenyl]sulfonyl]amino)benzamide
-
Homo sapiens
N-hydroxy-4-([4-[(4-hydroxybut-2-yn-1-yl)oxy]phenyl]sulfonyl)-2,2-dimethylthiomorpholine-3-carboxamide
-
Homo sapiens
N-hydroxy-N2-methyl-3-[(4-phenoxyphenyl)sulfonyl]-L-alaninamide
-
Homo sapiens
N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-(pyridin-4-ylmethyl)valinamide
-
Homo sapiens
N-[2-(4-[benzyl[2-(hydroxycarbamoyl)-4,6-dimethylphenyl]sulfamoyl]phenoxy)ethyl]-1-benzofuran-2-carboxamide WAY-170523 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-2-carboxamide
-
Homo sapiens
N-[4-(morpholin-4-yl)butyl]-1-benzofuran-2-carboxamide i.e. CL-82198 Homo sapiens
N-[[(3-phenyl-1,2-oxazol-5-yl)methyl]carbamothioyl]benzamide competitive, is synergic with acetohydroxamic acid Homo sapiens
N-[[4-(4-fluorophenoxy)phenyl]sulfonyl]-N-[1-(hydroxycarbamoyl)cyclopentyl]-b-alanine
-
Homo sapiens
N2-[(2S)-2-[[(4-benzylbenzyl)(hydroxy)phosphoryl]methyl]-4-phenylbutanoyl]-N,3-dimethyl-L-valinamide
-
Homo sapiens
N2-[(2S)-2-[[(4-benzylbenzyl)(hydroxy)phosphoryl]methyl]-6-phenoxyhexanoyl]-N,3-dimethyl-L-valinamide
-
Homo sapiens
N2-[(4'-bromobiphenyl-4-yl)sulfonyl]-N-hydroxy-D-valinamide
-
Homo sapiens
N2-[(4'-bromobiphenyl-4-yl)sulfonyl]-N-hydroxy-D-valinamide a nonselective inhibitor Rattus norvegicus
RS 102,481 a small molecule preferential inhibitor of MMP13, the compound is able to potently inhibit the release of type II collagen degradation peptides from human osteoarthritis articular cartilage explants Homo sapiens
RS 102,481 a small molecule preferential inhibitor of MMP13 Mus musculus
RS 102,481 a small molecule preferential inhibitor of MMP13 Rattus norvegicus

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ dependent on Mus musculus
Ca2+ dependent on Homo sapiens
Ca2+ dependent on Rattus norvegicus
Zn2+ dependent on Mus musculus
Zn2+ dependent on Homo sapiens
Zn2+ dependent on Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Gelatin + H2O Mus musculus
-
?
-
?
Gelatin + H2O Homo sapiens
-
?
-
?
Gelatin + H2O Rattus norvegicus high activity ?
-
?
additional information Rattus norvegicus rat MMP13 is a better gelatinase than a collagenase. Injection of catalytically active recombinant MMP13 enzyme into a rat knee joint to induce cartilage damage ?
-
?
Type I collagen + H2O Mus musculus fibrillar type ?
-
?
Type I collagen + H2O Homo sapiens fibrillar type ?
-
?
Type I collagen + H2O Rattus norvegicus fibrillar type ?
-
?
type II collagen + H2O Mus musculus fibrillar type ?
-
?
type II collagen + H2O Homo sapiens fibrillar type ?
-
?
type II collagen + H2O Rattus norvegicus fibrillar type ?
-
?
type III collagen + H2O Mus musculus fibrillar type ?
-
?
type III collagen + H2O Homo sapiens fibrillar type ?
-
?
type III collagen + H2O Rattus norvegicus fibrillar type ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
bone
-
Mus musculus
-
bone mRNA encoding MMP13 is present in multiple cell types involved in human fetal bone development Homo sapiens
-
breast cancer cell
-
Homo sapiens
-
cartilage
-
Mus musculus
-
cartilage articular, from osteoarthritis and rheumatoid arthritis patients Homo sapiens
-
chondrocyte
-
Mus musculus
-
chondrocyte
-
Homo sapiens
-
head and neck squamous cell carcinoma cell line
-
Homo sapiens
-
kidney
-
Homo sapiens
-
salivary gland cancer cell
-
Homo sapiens
-
skin cancer cell high levels of MMP13 mRNA only in malignant squamous epithelium of the skin, while premalignant and benign tumors are mostly negative for MMP13 Homo sapiens
-
synovial membrane expression of MMP13 in the synovial membrane of patients with rheumatoid and osteoarthritis Homo sapiens
-
synovial tissue high expression of MMP13 in rheumatoid arthritis synovial tissue Homo sapiens
-
uterus
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-PLG(S)LLG-OEt thioester + H2O
-
Homo sapiens ?
-
?
Gelatin + H2O
-
Mus musculus ?
-
?
Gelatin + H2O
-
Homo sapiens ?
-
?
Gelatin + H2O
-
Rattus norvegicus ?
-
?
Gelatin + H2O high activity Rattus norvegicus ?
-
?
additional information rat MMP13 is a better gelatinase than a collagenase. Injection of catalytically active recombinant MMP13 enzyme into a rat knee joint to induce cartilage damage Rattus norvegicus ?
-
?
Type I collagen + H2O fibrillar type Mus musculus ?
-
?
Type I collagen + H2O fibrillar type Homo sapiens ?
-
?
Type I collagen + H2O fibrillar type Rattus norvegicus ?
-
?
type II collagen + H2O fibrillar type Mus musculus ?
-
?
type II collagen + H2O fibrillar type Homo sapiens ?
-
?
type II collagen + H2O fibrillar type Rattus norvegicus ?
-
?
type III collagen + H2O fibrillar type Mus musculus ?
-
?
type III collagen + H2O fibrillar type Homo sapiens ?
-
?
type III collagen + H2O fibrillar type Rattus norvegicus ?
-
?

Synonyms

Synonyms Comment Organism
collagenase-3
-
Homo sapiens
collagenase-3
-
Rattus norvegicus
MMP13
-
Mus musculus
MMP13
-
Homo sapiens
MMP13
-
Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information steady-state inhibition kinetics studies Homo sapiens
0.00000003
-
N-hydroxy-2,2-dimethyl-4-[[4-(pyridin-4-yloxy)phenyl]sulfonyl]thiomorpholine-3-carboxamide pH not specified in the publication, temperature not specified in the publication Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000000016
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[[(4'-chlorobiphenyl-4-yl)oxy]methyl]-N-hydroxy-4-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)butanamide
0.00000008
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[[[4-(4-chlorophenoxy)phenyl]sulfonyl](methyl)amino]-N-hydroxy-3-[(4-methylpiperazin-1-yl)methyl]benzamide
0.0000002
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[[(4'-cyanobiphenyl-4-yl)oxy]methyl]-N-hydroxy-4-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)butanamide
0.00000033
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-(4-phenoxyphenyl)-1,7,9-triazaspiro[4.5]decane-2,6,8,10-tetrone
0.00000036
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-(6-[4-[4-(4-fluorophenyl)-1,3-oxazol-2-yl]phenoxy]pyridin-3-yl)-1,7,9-triazaspiro[4.5]decane-6,8,10-trione
0.00000036
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-[2-[4-(4-[[5-(2-ethoxyethyl)-2,4,6-trioxohexahydropyrimidin-5-yl]oxy]phenoxy)phenyl]-1,3-oxazol-4-yl]benzonitrile
0.0000004
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-hydroxy-N2-methyl-3-[(4-phenoxyphenyl)sulfonyl]-L-alaninamide
0.0000005
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-([[4-(4-fluorophenoxy)phenyl]sulfonyl]amino)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
0.00000067
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-[[1-methyl-2,4-dioxo-6-(3-phenylprop-1-yn-1-yl)-1,4-dihydroquinazolin-3(2H)-yl]methyl]benzoic acid
0.00000075
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-([[4-(4-fluorophenoxy)phenyl]sulfonyl]amino)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
0.0000009
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 1,5-anhydro-2,3-dideoxy-3-[[4-(2,4-dichlorophenoxy)phenyl]sulfonyl]-4-C-(hydroxycarbamoyl)-D-threo-pentitol
0.0000009
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[[4-(4-fluorophenoxy)phenyl]sulfonyl]-N-[1-(hydroxycarbamoyl)cyclopentyl]-b-alanine
0.00000095
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (2R,3R)-4-[[4-(2-chloro-4-fluorophenoxy)phenyl]sulfonyl]-N,2-dihydroxy-2-methylmorpholine-3-carboxamide
0.0000013
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-([4'-[(1-benzofuran-2-ylcarbonyl)amino]biphenyl-4-yl]sulfonyl)valine
0.00000154
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-[[4-oxo-6-(3-phenylprop-1-yn-1-yl)quinazolin-3(4H)-yl]methyl]benzoic acid
0.0000018
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[[(4'-[[(5-bromo-4-methoxy-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]methyl]-3-methylbutanoic acid
0.000003
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (2S,3R)-1-acetyl-N-hydroxy-2-methyl-4-[[4-(2-methylbenzyl)phenyl]sulfonyl]piperidine-3-carboxamide
0.000003
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (4R)-1-[4-(4-fluorophenoxy)benzyl]-N-hydroxy-2-oxoimidazolidine-4-carboxamide
0.000004
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-hydroxy-3-methyl-2-(methyl[[4-(pyridin-4-yloxy)phenyl]sulfonyl]amino)benzamide
0.0000045
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(ethyl[[4-(prop-1-yn-1-yloxy)phenyl]sulfonyl]amino)-5-phenylpentane(thioperox)ic O-acid
0.0000066
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N,N'-bis(pyridin-3-ylmethyl)pyrimidine-4,6-dicarboxamide
0.00000672
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-([6-[(4-methoxybenzyl)carbamoyl]-4-oxopyrido[3,4-d]pyrimidin-3(4H)-yl]methyl)benzoic acid
0.000007
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (4S)-4-[4-(4-fluorophenoxy)phenyl]-N-hydroxy-5-oxo-D-prolinamide
0.000008
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N,N'-bis(pyridin-3-ylmethyl)pyrimidine-4,6-dicarboxamide
0.000008
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-hydroxy-4-([4-[(4-hydroxybut-2-yn-1-yl)oxy]phenyl]sulfonyl)-2,2-dimethylthiomorpholine-3-carboxamide
0.000008
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-hydroxy-2-[[(4-methoxyphenyl)sulfonyl](pyridin-3-ylmethyl)amino]-3-methylbenzamide
0.00001
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-(2-ethoxyethyl)-5-[4-[4-(1,3,4-oxadiazol-2-yl)phenoxy]phenoxy]pyrimidine-2,4,6(1H,3H,5H)-trione
0.0000122
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-fluoro-N-hydroxy-6-([4-[4-(trifluoromethoxy)phenoxy]piperidin-1-yl]sulfonyl)benzamide
0.000014
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N2-[(2S)-2-[[(4-benzylbenzyl)(hydroxy)phosphoryl]methyl]-4-phenylbutanoyl]-N,3-dimethyl-L-valinamide
0.0000149
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-([4'-[([4-[(2-carboxypropan-2-yl)oxy]-1-benzofuran-2-yl]carbonyl)amino]biphenyl-4-yl]sulfonyl)-L-valine
0.000015
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[benzyl[(4-methoxyphenyl)sulfonyl]amino]-N-hydroxy-3,5-dimethylbenzamide
0.000017
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[2-(4-[benzyl[2-(hydroxycarbamoyl)-4,6-dimethylphenyl]sulfamoyl]phenoxy)ethyl]-1-benzofuran-2-carboxamide
0.000021
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N2-[(2S)-2-[[(4-benzylbenzyl)(hydroxy)phosphoryl]methyl]-6-phenoxyhexanoyl]-N,3-dimethyl-L-valinamide
0.00003
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens benzyl 6-benzyl-5,7-dioxo-6,7-dihydro-5H-[1,3]thiazolo[3,2-c]pyrimidine-2-carboxylate
0.000047
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-hydroxy-2,6-dimethoxy-3-[[(4-methoxyphenyl)sulfonyl](pyridin-3-ylmethyl)amino]pyridine-4-carboxamide
0.000065
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-methyl-5-(4-phenoxyphenoxy)pyrimidine-2,4,6(1H,3H,5H)-trione
0.000078
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-hexyl-5-(4-phenoxyphenoxy)pyrimidine-2,4,6(1H,3H,5H)-trione
0.00039
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-(4-chlorophenoxy)-5-methylpyrimidine-2,4,6(1H,3H,5H)-trione
0.01
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[4-(morpholin-4-yl)butyl]-1-benzofuran-2-carboxamide

Expression

Organism Comment Expression
Homo sapiens strong stimulus of a combination of interleukin-1alpha plus oncostatin M, inducing MMP13 expression up

General Information

General Information Comment Organism
additional information cartilage structural damage in osteoarthritis in mice is dependent on MMP13 activity Mus musculus
additional information high MMP13 expression is correlated with poor prognosis and reduced median overall survival in patients with head and neck cancer. High MMP13 levels in patients with salivary gland cancer are also associated with poor survival. And high levels of tumor-derived MMP13 correlate with poor prognosis in invasive breast cancer and reduced overall survival Homo sapiens
physiological function MMP13 plays a critical role in the redifferentiation phase of kidney development. Potential role of MMP13 in endochondral and intramembranous ossification, with a functional role in skeletal development. MMP13 plays a significant role in the cartilage collagen degradation that occurs in osteoarthritis, and a pathological role of the degradative MMP13 enzyme in rheumatoid arthritis. The catalytic activity of MMP13 may play a role in the high invasion capacity of these cancer cells. Degradation of basement membrane is thought to be an early and critical event influencing tumor invasion and metastasis. MMP13 plays a role in proteolytic activity in invasive malignant growth Homo sapiens
physiological function the MMP-13 knockout phenotype, which is due to an inability of chondrocytes to exit the growth plate, resolves completely by 12 weeks of age, suggesting that other (collagen degrading) proteases can at least partially functionally substitute for MMP13 in this developmental role Mus musculus