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3.4.24.B10: ADAM12 endopeptidase

This is an abbreviated version!
For detailed information about ADAM12 endopeptidase, go to the full flat file.

Word Map on EC 3.4.24.B10

Reaction

proteolysis of proteins =

Synonyms

a disintegrin and metalloprotease 12, a disintegrin and metalloprotease with thrombospondin motifs 12, a disintegrin and metalloprotease-12, a disintegrin and metalloproteinase 12, a disintegrin and metalloproteinase domain 12, a disintegrin and metalloproteinase domain-containing protein 12, a disintegrin and metalloproteinase12, ADAM 12, ADAM 12-S, ADAM-12, ADAM-12m, ADAM-PCD, ADAM12, ADAM12-L, ADAM12-PC, ADAM12-S, ADAM12/meltrin alpha, ADAM12L, ADAM12S, ADAMTS-12, ADMA12L, basigin sheddase, disintegrin and metalloprotease 12, full-length ADAM 12-S, M12.212, meltrin alpha, meltrin-alpha, metalloprotease-disintegrin ADAM 12, metalloprotease-disintegrin ADAM12

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.24 Metalloendopeptidases
                3.4.24.B10 ADAM12 endopeptidase

Inhibitors

Inhibitors on EC 3.4.24.B10 - ADAM12 endopeptidase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2R)-N4-hydroxy-N1-[(1S)-1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl]-2-(2-methylpropyl)butanediamide
-
IC50: 5930 nM
(4-(N-hydroxyamino)-2R-isobutyl-3S-methylsuccinyl)-L-phenylglycine-N-methylamide
-
KB-R7785, 0.001mmol/l
1,10-phenanthroline
4-[[[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4,6,7-hexahydroquinolin-3-yl](pyridin-2-ylsulfonyl)amino]methyl]-N,N-dimethylpiperidine-1-carboxamide
-
Aprotinin
-
0.1 mg/ml
batimastat
BB94
-
0.01 mM
Co2+
-
0.01 mM Co2+ inhibits the activity by 80%, while increasing concentrations rescue the lost activity
endogenous matrix metalloprotease inhibitor
-
500 nM, TIMP-3
-
Hg2+
-
-
hydroxamate inhibitor BB-94
slight inhibition
KB-R7785
-
0.001 mM
marimastat
MMP inhibitor III
-
MMP inhibitor V
-
MMP-3 inhibitor VIII
-
Mn2+
-
-
N-TIMP-1
N-terminal domain of TIMP-1, tissue inhibitor of metalloproteinase
-
N-TIMP-1TACE
mutant (V4S/V69L/T98L/TIMP-3-ABloop) of N-TIMP-1, tissue inhibitor of metalloproteinase
-
N-TIMP-1[T98L]
mutant of N-TIMP-1, tissue inhibitor of metalloproteinase
-
N-TIMP-1[TIMP-2-ABloop]
mutant of N-TIMP-1, tissue inhibitor of metalloproteinase
-
N-TIMP-1[TIMP-3-ABloop]
mutant of N-TIMP-1, tissue inhibitor of metalloproteinase
-
N-TIMP-1[V4A]
mutant of N-TIMP-1, tissue inhibitor of metalloproteinase
-
N-TIMP-1[V4S]
mutant of N-TIMP-1, tissue inhibitor of metalloproteinase
-
N-TIMP-2
N-terminal domain of TIMP-2, tissue inhibitor of metalloproteinase
-
N-TIMP-2-deltaABloop
mutant of N-TIMP-2, tissue inhibitor of metalloproteinase
-
N-TIMP-2TACE
mutant (S2T/A70S/V71L/TIMP-3-ABloop) of N-TIMP-2, tissue inhibitor of metalloproteinase
-
N-TIMP-2TACE[F34G]
mutant of N-TIMP-2TACE, tissue inhibitor of metalloproteinase
-
N-TIMP-2TACE[L100E]
mutant of N-TIMP-2TACE, tissue inhibitor of metalloproteinase
-
N-TIMP-3
-
N-[(2E)-3-(2-fluorophenyl)-2-[(phenylcarbonyl)amino]prop-2-enoyl]valine
-
IC50: 40.5 nM
N-[(2E)-3-(3-bromophenyl)-2-[(furan-2-ylcarbonyl)amino]prop-2-enoyl]glycine
-
IC50: 16.7 nM
N-[(2E)-3-(4-bromofuran-2-yl)-2-[[(5-bromofuran-2-yl)carbonyl]amino]prop-2-enoyl]alanine
-
IC50: 24.8 nM
N-[(2E)-3-furan-2-yl-2-[(furan-2-ylcarbonyl)amino]prop-2-enoyl]alanine
-
IC50: 42.3 nM
NaCl
-
-
Ni2+
-
low concentrations of Ni2+ inhibit ADAM12-S drastically
small interfering RNA
-
inhibits expression of the enzyme in C2C12 cells
-
TIMP-1
-
TIMP-2
-
TIMP-3
tissue inhibitor of metalloproteinase
-
tissue inhibitor of metalloproteinase-3
i.e. TIMP-3, possible physiological inhibitor of the enzyme
-
additional information
-