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3.4.25.1: proteasome endopeptidase complex

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

Word Map on EC 3.4.25.1

Reaction

cleavage of peptide bonds with very broad specificity =

Synonyms

20 S proteasome, 206 proteasome, 20S CP, 20S protease core, 20S proteasome, 26 S proteasome, 26S protease, 26S proteasome, 26S proteasome complex, 27 kDa prosomal protein, 30 kDa prosomal protein, beta1-PF1404, c20S, Component Y8, constitutive proteasome 20S, EC 3.4.22.21, EC 3.4.24.5, EC 3.4.99.46, GPRO-28, HsBPROS26, HSN3, i20S, immunoproteasome 20S, ingensin, KIPase, large multicatalytic protease, macropain, multi-subunit protease complex, multicatalytic endopeptidase complex, Multicatalytic endopeptidase complex C7, multicatalytic protease, multicatalytic proteinase, p27K, PROS-27, PROS-30, PROS-Dm25, PROS-Dm28.1, PROS-Dm29, PROS-Dm35, Pros26.4, prosome, proteasome, proteasome 19S, proteasome 20S, Proteasome component C13, Proteasome component C2, Proteasome component C3, Proteasome component C5, Proteasome component C8, Proteasome component C9, Proteasome component DD4, Proteasome component DD5, Proteasome component pts1, proteasome subunit alpha-type 7-like, PSMA5, Psma8, RING12 protein, RN3, Scl1, SCL1 suppressor protein, SFRICE_003436, T20S, TAS-F22/FAFP98, TAS-G64, TCPR29, tricorn protease, tricorn proteinase, XC3

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.25 Threonine endopeptidases
                3.4.25.1 proteasome endopeptidase complex

IC50 Value

IC50 Value on EC 3.4.25.1 - proteasome endopeptidase complex

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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000086 - 0.000194
(-)-epigallocatechin-3-gallate
Homo sapiens
-
inhibition of the chymotrypsin-like activity of the proteasome in vitro, pH not specified in the publication, temperature not specified in the publication
0.019
(2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,4,5-trihydroxybenzoate)
Homo sapiens
-
for the chymotrypsin-like activity, pH 7.5, 37°C
0.029
(2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,5-dihydroxybenzoate)
Homo sapiens
-
for the chymotrypsin-like activity, pH 7.5, 37°C
0.00022
1-[1-(1-[(2,4-dioxoimidazolidin-1-ylimino)-methyl]-2-phenyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol)
Homo sapiens
-
pH 7.5, 30°C
0.85
acetyl-Leu-Leu-Arg
Patiria pectinifera
-
IC50: 0.85 mM for chymotrypsin-like activity, 0.0056 mM for trypsin-like activity
0.11
benzyloxycarbonyl-Leu-Gly-Arg
Patiria pectinifera
-
IC50: 0.11 mM for chymotrypsin-like activity, 0.0066 mM for trypsin-like activity
0.056
Benzyloxycarbonyl-Leu-Leu-Arg
Patiria pectinifera
-
IC50: 0.056 mM for chymotrypsin-like activity, 0.0014 mM for trypsin-like activity
0.017
benzyloxycarbonyl-Leu-Ser-Arg
Patiria pectinifera
-
IC50: 0.017 mM for chymotrypsin-like activity, 0.0017 mM for trypsin-like activity
0.065
benzyloxycarbonyl-Leu-Thr-Arg
Patiria pectinifera
-
IC50: 0.065 mM for chymotrypsin-like activity, 0.0021 mM for trypsin-like activity
0.0089
benzyloxycarbonyl-Phe-Ser-Arg
Patiria pectinifera
-
IC50: 0.0089 mM for chymotrypsin-like activity, 0.002 mM for trypsin-like activity
0.0074
dibromo[(dimethylamino)methanedithiolato(2-)-kappa2S1,S1]aurate(3-)
Oryctolagus cuniculus
-
inhibition of the chymotrypsin-like activity of the 20S proteasome
0.000049 - 0.002
glidobactin A
0.0347
KAuBr4
Oryctolagus cuniculus
-
-
0.1
leupeptin
Trypanosoma brucei
IC50: 0.0015 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin, most potent inhibitor for hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.1 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin
0.0000373
MG-132
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00084 - 0.01
N-(tert-butoxycarbonyl)-L-alanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
0.00428 - 0.01
N-(tert-butoxycarbonyl)-L-alanyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide
0.0015 - 0.01
N-(tert-butoxycarbonyl)-L-isoleucyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
0.00942
N-(tert-butoxycarbonyl)-L-phenylalanyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00147 - 0.01
N-(tert-butoxycarbonyl)-L-phenylalanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
0.00164
N-(tert-butoxycarbonyl)-O-methyl-L-tyrosyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00815
N-(tert-butoxycarbonyl)-O-methyl-L-tyrosyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00054 - 0.01
N-(tert-butoxycarbonyl)glycyl-N1-benzyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-L-glutamamide
0.00028 - 0.01
N-(tert-butoxycarbonyl)glycyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
0.00274 - 0.01
N-(tert-butoxycarbonyl)glycyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide
0.00785
N-[(1S)-1-benzyl-2-[[(1S)-1-(furan-2-ylcarbonyl)-3-methylbutyl]amino]-2-oxoethyl]-Na-(tert-butoxycarbonyl)-L-phenylalaninamide
Homo sapiens
-
-
0.00756
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00585
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00262
N-[(benzyloxy)carbonyl]-L-phenylalanyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00000865 - 0.0000796
N2-(decylcarbamoyl)-N-[(3E,5S,8S,9E)-2,7-dioxo-5-(propan-2-yl)-1,6-diazacyclododeca-3,9-dien-8-yl]-L-valinamide
0.00451 - 0.01
N2-(tert-butoxycarbonyl)-N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-3-[(naphthalen-2-ylmethyl)amino]-3-oxo-D-alaninamide
0.00723 - 0.01
N2-(tert-butoxycarbonyl)-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
0.00068 - 0.01
N2-(tert-butoxycarbonyl)-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide
0.01
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
Homo sapiens
-
IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C
0.01
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
Homo sapiens
-
IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C
0.00682
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-O-methyl-L-tyrosinamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00785
Nalpha-[(2S)-2-[2-(tert-butoxycarbonyl)hydrazinyl]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00327
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-(4-methoxyphenyl)butanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00839
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.00642
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.01
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
Homo sapiens
-
IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C
0.01
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
Homo sapiens
-
IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C
0.01
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
Homo sapiens
-
IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C
0.00601
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-O-methyl-L-tyrosinamide
Homo sapiens
-
in 10 mM HEPES (pH 7.6), at 37°C
0.01
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-[[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
Homo sapiens
-
IC50 above 0.01 mM, in 10 mM HEPES (pH 7.6), at 37°C
0.007
NPLLLVS
Trypanosoma brucei
IC50: 0.04 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.007 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin, most potent inhibitor for hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-meth
0.077
NPLLNVS
Trypanosoma brucei
IC50: 0.063 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-carbamoylcoumarin. IC50: 0.077 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin
0.00102 - 0.0103
syringolin A
0.000757 - 0.0187
syringolin A methyl ester
-
0.00778 - 0.1078
syringolin B
0.033
YLLLVS
Trypanosoma brucei
IC50: 0.048 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.033 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin
additional information
additional information
Homo sapiens
-
cell growth inhibition activities, overview
-