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(3R)-3-(3-[[acetyl(methyl)amino]methyl]-1,2,4-oxadiazol-5-yl)-6-cyclohexyl-N-hydroxyhexanamide
-
-
(3R)-3-[3-(6-aminopyridin-3-yl)-1,2,4-oxadiazol-5-yl]-6-cyclohexyl-N-hydroxyhexanamide
-
-
(3R)-3-[3-(aminomethyl)-1,2,4-oxadiazol-5-yl]-6-cyclohexyl-N-hydroxyhexanamide
-
-
(3R)-3-[3-([[(aminooxy)sulfinyl]amino]methyl)-1,2,4-oxadiazol-5-yl]-6-cyclohexyl-N-hydroxyhexanamide
-
-
(3R)-3-[3-[(acetylamino)methyl]-1,2,4-oxadiazol-5-yl]-6-cyclohexyl-N-hydroxyhexanamide
-
-
(3R)-3-[3-[(carbamoylamino)methyl]-1,2,4-oxadiazol-5-yl]-6-cyclohexyl-N-hydroxyhexanamide
-
-
(3R)-3-[3-[(cyclobutylamino)methyl]-1,2,4-oxadiazol-5-yl]-6-cyclohexyl-N-hydroxyhexanamide
-
-
(3R)-3-[3-[(tert-butylamino)methyl]-1,2,4-oxadiazol-5-yl]-6-cyclohexyl-N-hydroxyhexanamide
-
-
(3R)-6-cyclohexyl-3-(3-[[(cyclopropylsulfonyl)amino]methyl]-1,2,4-oxadiazol-5-yl)-N-hydroxyhexanamide
-
-
(3R)-6-cyclohexyl-3-[3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-1,2,4-oxadiazol-5-yl]-N-hydroxyhexanamide
-
-
(3R)-6-cyclohexyl-3-[3-(2-furyl)-1,2,4-oxadiazol-5-yl]-N-hydroxyhexanamide
-
-
(3R)-6-cyclohexyl-3-[3-[(cyclopropylamino)methyl]-1,2,4-oxadiazol-5-yl]-N-hydroxyhexanamide
-
-
(3R)-6-cyclohexyl-3-[3-[(dimethylamino)methyl]-1,2,4-oxadiazol-5-yl]-N-hydroxyhexanamide
-
-
(3R)-6-cyclohexyl-3-[3-[(ethylamino)methyl]-1,2,4-oxadiazol-5-yl]-N-hydroxyhexanamide
-
-
(3R)-6-cyclohexyl-3-[3-[6-(dimethylamino)pyridin-3-yl]-1,2,4-oxadiazol-5-yl]-N-hydroxyhexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-(3-phenyl-1,2,4-oxadiazol-5-yl)hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-(3-pyrazin-2-yl-1,2,4-oxadiazol-5-yl)hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-(3-pyridin-3-yl-1,2,4-oxadiazol-5-yl)hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-(3-pyridin-4-yl-1,2,4-oxadiazol-5-yl)hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-(3-pyrimidin-2-yl-1,2,4-oxadiazol-5-yl)hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-(3-pyrimidin-5-yl-1,2,4-oxadiazol-5-yl)hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-(3-[2-[(methylsulfinyl)amino]ethyl]-1,2,4-oxadiazol-5-yl)hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-(3-[[(1-methylethyl)amino]methyl]-1,2,4-oxadiazol-5-yl)hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-(3-[[(2-hydroxy-1,1-dimethylethyl)amino]methyl]-1,2,4-oxadiazol-5-yl)hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-(1-methyl-1H-imidazol-2-yl)-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-(1H-pyrazol-4-yl)-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-(4H-pyrazol-3-yl)-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-(6-methylpyridazin-3-yl)-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-(morpholin-4-ylmethyl)-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-(pyridin-2-ylmethyl)-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-(pyridin-3-ylmethyl)-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-(pyridin-4-ylmethyl)-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-(pyrrolidin-1-ylmethyl)-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-[(4-hydroxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-[(methylamino)methyl]-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1,2,4-oxadiazol-5-yl]hexanamide
-
-
(3R)-6-cyclohexyl-N-hydroxy-3-[3-[6-(methylamino)pyridin-3-yl]-1,2,4-oxadiazol-5-yl]hexanamide
-
-
1,4-dithio-L-threitol
-
-
1-acetyl-L-prolyl-L-tyrosyl-L-tyrosyl-N-hydroxyglycinamide
-
-
1H-pyrazol-4-yl [(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)methyl]amidosulfite
-
-
2-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)-N,N-dimethylpyridine-4-carboxamide
-
-
2-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)-N-methylpyridine-4-carboxamide
-
-
2-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)pyridine-4-carboxamide
-
-
2-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)pyridine-4-carboxylic acid
-
-
2-(N-((3s,5s,7s)-adamantan-1-yl)-4-methoxyphenylsulfonamido)-N-hydroxyacetamide
-
9-21% inhibition at 0.010 mM
2-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-5-methyl-1,3-oxazole-4-carboxamide
-
-
2-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-N,N-dimethyl-5-methyl-1,3-oxazole-4-carboxamide
-
-
2-[[3-(hydroxyamino)-3-oxopropyl][2-(4-methoxyphenyl)ethyl]sulfamoyl]benzoic acid
-
32% inhibition at 0.010 mM
3-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)benzoic acid
-
-
4-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)benzoic acid
-
-
4-[benzyl[(4-methoxyphenyl)sulfonyl]amino]-N-hydroxybutanamide
-
-
4-[[3-(hydroxyamino)-3-oxopropyl](2-phenylethyl)sulfamoyl]benzoic acid
-
-
4-[[3-(hydroxyamino)-3-oxopropyl][2-(4-methoxyphenyl)ethyl]sulfamoyl]-N-phenylbenzamide
-
-
5-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)pyridine-2-carboxylic acid
-
-
5-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)pyridine-3-carboxylic acid
-
-
5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-N-(phenylsulfonyl)-1,2,4-oxadiazole-3-carboxamide
-
-
5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-N-[(3,4-dimethoxyphenyl)sulfonyl]-1,2,4-oxadiazole-3-carboxamide
-
-
5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-N-[(4-fluorophenyl)sulfonyl]-1,2,4-oxadiazole-3-carboxamide
-
-
5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-N-[(4-methoxyphenyl)sulfonyl]-1,2,4-oxadiazole-3-carboxamide
-
-
5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-N-[(4-methylphenyl)sulfonyl]-1,2,4-oxadiazole-3-carboxamide
-
-
5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-1,2,4-oxadiazole-3-carboxamide
-
i.e. UK-383,367. Good selectivity over matrix metalloproteinases involved in wound healing, effective in a cell-based model of collagen deposition and in penetrating human skin in vitro
5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-N,N-dimethyl-1,2,4-oxadiazole-3-carboxamide
-
good selectivity over matrix metalloproteinases involved in wound healing
5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-N-isopropyl-1,2,4-oxadiazole-3-carboxamide
-
-
Ac-Met-Val-Gly-Asp-Asp-Pro-Tyr-Asn-NH2
-
weak inhibitor
acidic dipeptide hydroxamate derivates
-
mimic the location of aspartic acid residues in the P1' and P2' positions of the PCP cleavage site in procollagen
-
alpha2-Macroglobulin
-
-
-
Arg
-
inhibits at 5-10 mM
Asp-Pro-Ile-Val-Cys-Pro-Pro-Leu-Asn-Cys-Ser-Gln-Pro-Val-His-Leu-Pro-Asp-Gln
peptide derived from amino acids 727-745 of chordin
Bovine alpha2-macroglobulin
-
-
-
butyl [[2-(hydroxyamino)-2-oxoethyl][(4-methoxyphenyl)sulfonyl]amino]acetate
-
-
Chicken alpha2-macroglobulin
-
-
-
cyclopropyl [(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)methyl]amidosulfite
-
-
decanoyl-Arg-Val-Lys-Arg-chloromethylketone
di-/tripeptidic hydroxamic acid derivates
-
-
-
diisopropylphosphofluoridate
ethyl 3-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)benzoate
-
-
ethyl 4-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)benzoate
-
-
ethyl [(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)methyl]amidosulfite
-
-
Fetal bovine serum
-
weak
-
Gln-Lys-Arg-Thr-Val-Ile-Cys-Asp-Pro-Ile-Val-Cys-Pro-Pro-Leu-Asn
Lys
-
inhibits at 5-10 mM
methyl 4-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)piperidine-1-sulfinate
-
-
methyl [(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)methyl]amidosulfite
-
-
methyl [(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)methyl]methylamidosulfite
-
-
methyl [4-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)phenyl]amidosulfite
-
-
methyl [5-(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)pyridin-2-yl]amidosulfite
-
-
N-ethylmaleimide
-
inhibits at 20 mM
N-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-phenylethyl)amino]butanamide
-
-
N-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](phenyl)amino]butanamide
-
-
N-hydroxy-N2-(4-methoxybenzyl)-N2-[(4-methoxyphenyl)sulfonyl]glycinamide
-
-
N-hydroxy-N2-(4-methoxyphenyl)-N2-[(4-methoxyphenyl)sulfonyl]glycinamide
-
-
N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-L-alpha-asparagine
-
-
N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-(2-phenylethyl)glycinamide
-
-
N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-phenylglycinamide
-
-
N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-[4-(trifluoromethyl)benzyl]glycinamide
-
-
N-hydroxy-N2-[2-(4-methoxyphenyl)ethyl]-N2-[(4-methoxyphenyl)sulfonyl]glycinamide
-
-
N-hydroxy-N3-(2-phenylethyl)-N3-(phenylsulfonyl)-beta-alaninamide
-
-
N-hydroxy-N3-(4-methoxyphenyl)-N3-[(4-methoxyphenyl)sulfonyl]-beta-alaninamide
-
-
N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-beta-alaninamide
-
-
N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-N3-(2-phenylethyl)-beta-alaninamide
-
-
N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-N3-phenyl-b-alaninamide
-
-
N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-N3-[2-(4-nitrophenyl)ethyl]-beta-alaninamide
-
-
N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-N3-[2-(4-sulfamoylphenyl)ethyl]-beta-alaninamide
-
-
N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-N3-[2-(morpholin-4-yl)ethyl]-beta-alaninamide
-
-
N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-N3-[2-(pyridin-2-yl)ethyl]-beta-alaninamide
-
-
N-hydroxy-N3-[(4-[[(4-methoxyphenyl)carbamoyl]amino]phenyl)sulfonyl]-N3-[2-(4-methoxyphenyl)ethyl]-beta-alaninamide
-
-
N-hydroxy-N3-[2-(2-methoxyphenyl)ethyl]-N3-[(4-methoxyphenyl)sulfonyl]-beta-alaninamide
-
45% inhibition at 0.010 mM
N-hydroxy-N3-[2-(3-methoxyphenyl)ethyl]-N3-[(4-methoxyphenyl)sulfonyl]-beta-alaninamide
-
-
N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-N3-([4-[(methylcarbamoyl)amino]phenyl]sulfonyl)-beta-alaninamide
-
-
N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-N3-([4-[(phenoxycarbamoyl)amino]phenyl]sulfonyl)-beta-alaninamide
-
-
N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-N3-([4-[(phenylcarbamoyl)amino]phenyl]sulfonyl)-beta-alaninamide
-
-
N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-N3-[(4-methoxyphenyl)sulfonyl]-beta-alaninamide
-
-
N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-N3-[(4-[[(2-phenylethyl)carbamoyl]amino]phenyl)sulfonyl]-beta-alaninamide
-
-
N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-N3-[[2-(methylsulfonyl)phenyl]sulfonyl]-beta-alaninamide
-
-
N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-N3-[[4-(methylsulfonyl)phenyl]sulfonyl]-beta-alaninamide
-
-
N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-N3-[[4-([[4-(trifluoromethyl)phenyl]carbamoyl]amino)phenyl]sulfonyl]-beta-alaninamide
-
-
N-hydroxy-N3-[[2-(N'-hydroxycarbamimidoyl)phenyl]sulfonyl]-N3-[2-(4-methoxyphenyl)ethyl]-beta-alaninamide
-
-
N-hydroxy-N3-[[3-(N'-hydroxycarbamimidoyl)phenyl]sulfonyl]-N3-[2-(4-methoxyphenyl)ethyl]-beta-alaninamide
-
-
N-hydroxy-N3-[[4-(N'-hydroxycarbamimidoyl)phenyl]sulfonyl]-N3-[2-(4-methoxyphenyl)ethyl]-beta-alaninamide
-
-
N-[(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)carbonyl]glycine
-
-
N-[(hydroxyamino)methyl]-L-alpha-aspartyl-N-methyl-L-alpha-glutamine
-
-
N-[2-(4-methoxyphenyl)ethyl]-4-(methylsulfonyl)-N-(2-sulfanylethyl)benzenesulfonamide
-
-
N-[2-(4-methoxyphenyl)ethyl]-4-(methylsulfonyl)-N-(3-sulfanylpropyl)benzenesulfonamide
-
-
N-[2-[carbamoyl(hydroxy)amino]ethyl]-N-[2-(4-methoxyphenyl)ethyl]-4-(methylsulfonyl)benzenesulfonamide
-
-
N2-(4-chlorobenzyl)-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide
-
-
N2-(4-fluorobenzyl)-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide
-
-
N2-(butylsulfonyl)-N-hydroxy-N2-[2-(4-methoxyphenyl)ethyl]glycinamide
-
-
N2-(diphenylmethyl)-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide
-
-
N2-benzyl-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-L-alpha-asparagine
-
-
N2-benzyl-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide
-
-
N2-butan-2-yl-N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]glycinamide
-
-
N2-[2-(4-methoxyphenyl)ethyl]-N2-[[4-(methylsulfonyl)phenyl]sulfonyl]-N-sulfanylglycinamide
-
-
N2-[2-(carboxymethyl)-4-(hydroxyamino)-4-oxobutanoyl]-N-methyl-L-alpha-glutamine
-
-
N2-[3-carboxy-2-(sulfanylmethyl)propanoyl]-N-methyl-L-alpha-glutamine
-
-
N3-(butylsulfonyl)-N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-beta-alaninamide
-
-
N3-(cyclohexylmethyl)-N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-beta-alaninamide
-
-
N3-([4-[(biphenyl-4-ylcarbamoyl)amino]phenyl]sulfonyl)-N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-beta-alaninamide
-
-
N3-([4-[(diphenoxycarbamoyl)amino]phenyl]sulfonyl)-N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-beta-alaninamide
-
-
N3-([4-[(diphenylcarbamoyl)amino]phenyl]sulfonyl)-N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-beta-alaninamide
-
-
N3-([4-[amino(phenylsulfonyl)methyl]phenyl]sulfonyl)-N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-beta-alaninamide
-
-
N3-benzyl-N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-beta-alaninamide
-
-
N3-butan-2-yl-N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-beta-alaninamide
-
-
N3-[(4-tert-butylphenyl)sulfonyl]-N-hydroxy-N3-(2-phenylethyl)-beta-alaninamide
-
-
N3-[(4-[[(4-chlorophenyl)carbamoyl]amino]phenyl)sulfonyl]-N-hydroxy-N3-[2-(4-methoxyphenyl)ethyl]-beta-alaninamide
-
-
N3-[2-(3,4-dimethoxyphenyl)ethyl]-N-hydroxy-N3-[(4-methoxyphenyl)sulfonyl]-beta-alaninamide
-
-
N3-[2-(4-methoxyphenyl)ethyl]-N3-[[4-(methylsulfonyl)phenyl]sulfonyl]-N-sulfanyl-beta-alaninamide
-
-
NaCl
-
inhibits at 200-500 mM
phenyl [(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)methyl]amidosulfite
-
-
pyridin-2-yl [(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)methyl]amidosulfite
-
-
pyridin-3-yl [(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)methyl]amidosulfite
-
-
small molecule ox(adi)azolyl-hydroxamic acid derivates
-
-
-
sulfonamide hydrxamate derivates of ornithine analogs
-
-
-
Synthetic peptides
-
with amino acid sequences similar to the amino acid sequence around the sites at which the C-propeptides are cleaved during the conversion of procollagen to collagen in vivo, e.g. Tyr-Tyr-Arg-Ala-Asp-Asp-Ala, 35-60% inhibition at 6-12 mM, shorter peptides containing the Ala-Asp bond cleaved by the enzyme are less effective
-
Tris-HCl buffer
-
inhibits at 200-500 mM
Tyr-Tyr-Arg-Ala-Asp-Asp-Ala
-
weak inhibitor
[[2-(hydroxyamino)-2-oxoethyl][(4-methoxyphenyl)sulfonyl]amino]acetic acid
-
-
1,10-phenanthroline
-
-
Cd2+
-
CdCl2
concanavalin A
-
-
-
CuCl2
-
-
CuCl2
-
inhibits at 0.01-0.1 mM
Cys-Asp-Pro-Ile-Val-Cys
minimal inhibitory peptide, derived from amino acids 726-731 of chordin. Peptide is not cleaved but instead undergoes cyclization by disulfide formation
Cys-Asp-Pro-Ile-Val-Cys
-
inhibits procollagen C-endopeptidase activity in vitro
decanoyl-Arg-Val-Lys-Arg-chloromethylketone
-
-
decanoyl-Arg-Val-Lys-Arg-chloromethylketone
-
-
decanoyl-Arg-Val-Lys-Arg-chloromethylketone
-
-
diisopropylphosphofluoridate
-
weak
diisopropylphosphofluoridate
-
weak
DTT
-
-
EDTA
a common inhibitor of several astacin metalloproteases
EDTA
a common inhibitor of several astacin metalloproteases
EDTA
a common inhibitor of several astacin metalloproteases
EGTA
-
-
Gln-Lys-Arg-Thr-Val-Ile-Cys-Asp-Pro-Ile-Val-Cys-Pro-Pro-Leu-Asn
peptide derived from amino acids 720-735 of chordin. Peptide is not cleaved but instead undergoes cyclization by disulfide formation
Gln-Lys-Arg-Thr-Val-Ile-Cys-Asp-Pro-Ile-Val-Cys-Pro-Pro-Leu-Asn
-
inhibits procollagen C-endopeptidase activity in vitro
L-arginine
-
weak
L-lysine
-
-
leupeptin
-
-
metal chelators
-
-
-
pepstatin
-
A
ZnCl2
-
-
additional information
-
not: cysteine proteinases; not: inhibitors of serine
-
additional information
-
not: cysteine proteinases; not: inhibitors of serine
-
additional information
-
not: cysteine proteinases; not: inhibitors of serine
-
additional information
-
procollagen C-proteinase enhancer-1 is not an inhibitor of BMP-1
-
additional information
-
the cyclic form AS1.11c (Gln-Lys-Arg-Thr-Val-Ile-Cys-Asp-Pro-Ile-Val-Cys-Pro-Pro-Leu-Asn) does not inhibit procollagen C-endopeptidase activity on procollagen type I
-
additional information
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design from substrate leads and synthesis of procollagen C-proteinase inhibitors, overview. The compounds are optimized for potency and selectivity, with N-substituted aryl sulfonamide hydroxamates having the best combination of these properties
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additional information
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not: inhibitors of serine
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