Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(-)-epigallocatechin-3-gallate
-
i.e. EGCG, inhibits the proteasomal chymotrypsin-like activity
(2E)-3-(4-tert-butylphenyl)-1-[4-(4-nitrophenyl)piperazin-1-yl]prop-2-en-1-one
-
-
(2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,4,5-triethoxybenzoate)
-
inhibits 48% of MDA-MB-231 cell proliferation at 0.05 mM
(2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,4,5-trihydroxybenzoate)
-
-
(2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,5-diethoxybenzoate)
-
70-79% inhibition in MDA-MB-231 cells at 0.025-0.050 mM
(2R,3S)-1,2,3,4-tetrahydronaphthalene-2,3-diyl bis(3,5-dihydroxybenzoate)
-
-
(acetato-kappaO)[2,4-diiodo-6-({[(pyridin-2-yl-kappaN)methyl]amino-kappaN}methyl)phenolato-kappaO]copper
-
a copper complex, causes selective 20S proteasomal inhibition and apoptosis induction in several lines of cancer cells
1-[1-(1-[(2,4-dioxoimidazolidin-1-ylimino)-methyl]-2-phenyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol)
2-(2-bromo-4-tert-butylphenoxy)-1-[4-(4-nitrophenyl)piperazin-1-yl]ethanone
-
-
2-(2-chlorophenyl)-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]quinoline-4-carboxamide
-
-
2-(4-tert-butylphenoxy)-1-[4-(4-methoxy-2-nitrophenyl)piperazin-1-yl]ethanone
-
-
2-methyl-5-[4-(phenylamino)phthalazin-1-yl]-N-(tetrahydrofuran-2-ylmethyl)benzenesulfonamide
-
-
4-(4-methoxyphenyl)-N-(4-nitrophenyl)piperazine-1-carbothioamide
-
-
4-hydroxy-2-nonenal
-
specific subunits of the 20S proteasome are targeted for modification by 4-hydroxy-2-nonenal (0.5 mM)
4-tert-butyl-N-[4-(diethylsulfamoyl)phenyl]benzamide
-
-
4-tert-butyl-N-[4-(dipropylsulfamoyl)phenyl]benzamide
-
-
4-tert-butyl-N-[4-[di(prop-2-en-1-yl)sulfamoyl]phenyl]benzamide
-
-
acetyl-Ala-Pro-norleucine-Leu-Asp-aldehyde
acetyl-Leu-Leu-Arg
-
IC50: 0.85 mM for chymotrypsin-like activity, 0.0056 mM for trypsin-like activity
acetyl-Leu-Leu-norleucinal
-
competitive
adamantaneacetyl-(6-aminohexanoyl)3-(leucyl)3-vinylmethyl sulfone
-
-
AEBSF
-
25% inhibition of hydrolysis of acetyl-norleucine-Leu-Pro-norleucine-Leu-Asp-7-amino-4-methylcoumarin, 22% inhibition of hydrolysis of acetyl-norleucine-GPLD-7-amido-4-methylcoumarin, 19% inhibition of hydrolysis of acetyl-GPLL-7-amido-4-methylcoumarin, 21% inhibition of hydrolysis of acetyl-Ala-Pro-norleucine-Leu-Leu-7-amido-4-methylcoumarin, 26% inhibition of hydrolysis of succinyl-LLVY-7-amido-4-methylcoumarin, 98% inhibition of hydrolysis of tert-butyloxycarbonyl-LRR-7-amino-4-methylcoumarin
Aprotinin
-
0.0133 mg/ml, 53.62% inhibition
ATP
-
inhibits trypsin-like, peptidylglutamyl peptide hydrolase, and branched-chain amino acid preferring activities
belactosin A
-
isolated from a Streptomyces sp. strain
Belactosin C
-
isolated from a Streptomyces sp. strain
benzyloxycarbonyl-Ala-Ala-Phe-CH2Cl
-
-
benzyloxycarbonyl-GPAF aldehyde
-
-
benzyloxycarbonyl-GPFL aldehyde
-
-
benzyloxycarbonyl-IE-(Ot-Bu)-AL aldehyde
-
0.002 mg/ml, 75% inhibition of chymotrypsin-like activity, hydrolysis of benzyloxycarbonyl-GGL-4-nitroanilide. 0.002 mM, 8% inhibition of peptidyl-glutamyl-peptide-hydrolyzing activity, hydrolysis of benzyloxycarbonyl-LLE-2-naphthylamide
benzyloxycarbonyl-Leu-Gly-Arg
-
IC50: 0.11 mM for chymotrypsin-like activity, 0.0066 mM for trypsin-like activity
benzyloxycarbonyl-Leu-Leu
-
0.1 mM, 84% inhibition of hydrolysis of succinyl-Leu-leu-Val-Tyr-7-amido-4-methylcoumarin, 43% inhibition of hydrolysis of tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin, 20% inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Leu-7-amido-4-methylcoumarin, 86% inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin
Benzyloxycarbonyl-Leu-Leu-Arg
-
IC50: 0.056 mM for chymotrypsin-like activity, 0.0014 mM for trypsin-like activity
benzyloxycarbonyl-Leu-Leu-CH2Cl
-
-
benzyloxycarbonyl-Leu-Leu-Leu-CHO
-
reversible inhibitor, modulation by sodium ion
benzyloxycarbonyl-Leu-Ser-Arg
-
IC50: 0.017 mM for chymotrypsin-like activity, 0.0017 mM for trypsin-like activity
benzyloxycarbonyl-Leu-Thr-Arg
-
IC50: 0.065 mM for chymotrypsin-like activity, 0.0021 mM for trypsin-like activity
benzyloxycarbonyl-LLF aldehyde
-
-
benzyloxycarbonyl-LLL aldehyde
-
0.001 mg/ml, 69% inhibition of chymotrypsin-like activity, hydrolysis of benzyloxycarbonyl-GGL-4-nitroanilide
benzyloxycarbonyl-Phe-Ser-Arg
-
IC50: 0.0089 mM for chymotrypsin-like activity, 0.002 mM for trypsin-like activity
benzyloxycarbonyl-Pro-norleucine-Leu-Asp-aldehyde
calpeptin
-
inhibits calpain-like activity
carbobenzoxy-L-leucyl-L-leucyl-leucinal
-
MG-132
cetyltrimethylammonium bromide
-
-
chloro[2,4-diiodo-6-({[(pyridin-2-yl-kappaN)methyl]amino-kappaN}methyl)phenolato-kappaO]copper
-
a copper complex, causes selective 20S proteasomal inhibition and apoptosis induction in several lines of cancer cells
Cl-
-
inhibits peptidylglutamyl peptide hydrolase activity
clasto-lactacystin beta-lactone
-
complete inhibition of the chymotrypsin-like activity at 0.01 mM, complete inhibition of the trypsin-like activity at 0.02 mM, and complete inhibition of caspase-activity of the 26S proteasome at 0.02 mM
clastolactacystin-beta-lactone
-
-
cystatin
-
0.0133 mg/mL 46.38% inhibition
-
c[Ala-Leu-Leu-Glu(Leu-vinyl ester)]
-
-
c[Gly-Leu-Leu-Glu(Leu-vinyl ester)]
-
-
c[Ser-Leu-Leu-Glu(Leu-vinyl ester)]
-
-
c[Val-Leu-Leu-Glu(Leu-vinyl ester)]
-
-
delanzomib
-
slow-binding inhibitor, kinetic analysis
dibromo[(dimethylamino)methanedithiolato(2-)-kappa2S1,S1]aurate(3-)
-
proteasome inhibition and apoptosis induction are completely blocked by addition of dithiothreitol or N-acetyl-L-cysteine, showing that process of oxidation is required for proteasome inhibition
diisopropylfluorophosphate
-
-
E-64
-
0.0133 mg/ml, 71.15% inhibition
E-64-d
-
0.1 mM, 30% inhibition of hydrolysis of succinyl-Leu-leu-Val-Tyr-7-amido-4-methylcoumarin, no inhibition of hydrolysis of tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin, benzyloxycarbonyl-Leu-Leu-Leu-7-amido-4-methylcoumarin, benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin
ethanol
-
ethanol-induced proteasome inhibition in liver cells
glial fibrillary acidic protein
-
human recombinant GFP-tagged, accumulation of the intermediate filament protein, glial fibrillary acidic protein, GFAP, in astrocytes of Alexander disease impairs proteasome function in astrocytes, also oligomers of R239C mutant GFAP inhibit the proteasome system in Alexander disease astrocytes to an even higher extent compared to the wild-type GFAP. The small heat shock protein chaperone alphaB-crystallin reverses the inhibition by shifting the size of the mutant protein from larger oligomers to smaller oligomers and monomers. The proteasome cannot efficiently degrade unassembled R239C GFAP, and the interaction of R239C GFAP with proteasomes actually inhibits proteasomal protease activity in a non-competitive manner, detailed overview
-
H-Ala-Leu-Leu-Glu(Leu-vinyl ester)-NH2
-
-
H-Gly-Leu-Leu-Glu(Leu-vinyl ester)-NH2
-
-
H-Ser-Leu-Leu-Glu(Leu-vinyl ester)-NH2
-
-
H-Val-Leu-Leu-Glu(Leu-vinyl ester)-NH2
-
-
hepatitis B virus X protein
-
-
-
histone H3
-
activity with benzyloxycarbonyl-LAF-4-aminobenzoate, 87%, benzyloxycarbonyl-dALR-4-aminobenzoate, 43%, or benzyloxycarbonyl-LLE-2-naphthylamide, 81% as substrates
-
iodoacetic acid
-
1.0 mM, 54.04 mM inhibition
ixazomib
-
slow-binding inhibitor, kinetic analysis
Mn2+
-
inhibits peptidylglutamyl peptide hydrolase activity
mutant huntingtin
-
mutant huntingtin filamentous aggregates can inhibit 26S proteasome activity, but only when not recruited inclusion bodies
-
N,N'-bis(4-methoxyphenyl)tricyclo[3.3.1.13,7]decane-1,3-dicarboxamide
-
-
N-(1-hydroxy-2-methylpropan-2-yl)-5-[4-[(3-hydroxyphenyl)amino]phthalazin-1-yl]-2-methylbenzenesulfonamide
-
-
N-(2-methyl-1,3-thiazole-5-carbonyl)-5-phenyl-L-norvalyl-N-[(1E,3S)-1-(methanesulfonyl)-5-methylhex-1-en-3-yl]-L-homoserinamide
-
compound has low nanomolar activity at killing parasite in the 72 h treatment with exceptionally low toxicity against human foreskin fibroblast resulting in greatly enhanced selectivity ratio. Compound has no toxicity to HepG2 cells even after 72 h treatment with doses as high as 10 microM
N-(3-hydroxy-2-oxopropyl)-5-[4-[(3-hydroxyphenyl)amino]phthalazin-1-yl]-2-methylbenzenesulfonamide
-
-
N-(4-methoxyphenyl)-3-(4-methylphenyl)tricyclo[3.3.1.13,7]decane-1-carboxamide
-
-
N-(tert-butoxycarbonyl)-L-alanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
-
-
N-(tert-butoxycarbonyl)-L-alanyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide
-
-
N-(tert-butoxycarbonyl)-L-isoleucyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
-
-
N-(tert-butoxycarbonyl)-L-phenylalanyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
60.06% inhibition at 0.01 mM
N-(tert-butoxycarbonyl)-L-phenylalanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
-
-
N-(tert-butoxycarbonyl)-O-methyl-L-tyrosyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
89.7% inhibition at 0.01 mM
N-(tert-butoxycarbonyl)-O-methyl-L-tyrosyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
69.7% inhibition at 0.01 mM
N-(tert-butoxycarbonyl)glycyl-N1-benzyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-L-glutamamide
-
shows significant inhibition of 20S proteasome chymotrypsin-like, b5 activity
N-(tert-butoxycarbonyl)glycyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
-
shows significant inhibition of 20S proteasome chymotrypsin-like, b5 activity
N-(tert-butoxycarbonyl)glycyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide
-
-
N-acetyl-Leu-Leu-norleucinal
-
-
N-acetyl-leucyl-leucyl-norleucinal
-
MG132, 0.03 mM
N-carbobenzoxy-L-leucyl-L-norvalinal
-
-
N-Cbz-Leu-Leu-leucinal
-
MG132
N-methoxysuccinyl-Glu-Val-Lys-Phe-H
-
modified
N-tert-butyl-5-[4-[(3-hydroxyphenyl)amino]phthalazin-1-yl]-2-methylbenzenesulfonamide
-
-
N-tosylphenylalanylchloromethylketone
-
-
N-[(1S)-1-benzyl-2-[[(1S)-1-(furan-2-ylcarbonyl)-3-methylbutyl]amino]-2-oxoethyl]-Na-(tert-butoxycarbonyl)-L-phenylalaninamide
-
inhibits chymotrypsin-like activity of the 26S proteasome
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
58.5% inhibition at 0.01 mM
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
73.4% inhibition at 0.01 mM
N-[(benzyloxy)carbonyl]-L-phenylalanyl-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
82.2% inhibition at 0.01 mM
N-[4-(acetylsulfamoyl)phenyl]-2-(4-ethoxyphenyl)quinoline-4-carboxamide
-
-
N-[4-(acetylsulfamoyl)phenyl]-2-(4-ethylphenyl)quinoline-4-carboxamide
-
-
N-[4-(azepan-1-ylsulfonyl)phenyl]-4-tert-butylbenzamide
-
-
N-[4-(benzylsulfamoyl)phenyl]-2-methylbenzamide
-
-
N-[4-(benzylsulfamoyl)phenyl]-2-[4-(thiophen-2-yl)phenyl]quinoline-4-carboxamide
-
-
N2-(decylcarbamoyl)-N-[(3E,5S,8S,9E)-2,7-dioxo-5-(propan-2-yl)-1,6-diazacyclododeca-3,9-dien-8-yl]-L-valinamide
-
rational design and synthesis of a syringolin A-based lipophilic derivative, which proves to be a very potent syrbactin-based proteasome inhibitor
N2-(tert-butoxycarbonyl)-N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-3-[(naphthalen-2-ylmethyl)amino]-3-oxo-D-alaninamide
-
-
N2-(tert-butoxycarbonyl)-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide
-
-
N2-(tert-butoxycarbonyl)-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide
-
-
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
7.7% inhibition at 0.01 mM
Nalpha-(tert-butoxycarbonyl)-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
16.5% inhibition at 0.01 mM
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
-
73% inhibition at 0.01 mM
Nalpha-[(2S)-2-[2-(tert-butoxycarbonyl)hydrazinyl]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
-
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-(4-methoxyphenyl)butanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
84.8% inhibition at 0.01 mM
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
47.5% inhibition at 0.01 mM
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
67.1% inhibition at 0.01 mM
Nalpha-[(2S)-2-[[(benzyloxy)carbonyl]amino]-4-phenylbutanoyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-O-methyl-L-tyrosinamide
-
14.9% inhibition at 0.01 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
5.7% inhibition at 0.01 mM
Nalpha-[(benzyloxy)carbonyl]-N-[(2S)-1-(furan-2-yl)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
13.6% inhibition at 0.01 mM
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
-
60.5% inhibition at 0.01 mM
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
-
36.4% inhibition at 0.01 mM
NH4Cl
-
lysosomal inhibitor
NLVS
-
irreversible inhibitor
NMDA
-
exposure causes the disassembly of 26S proteasomes and dissociation of E3, i.e. KCMF1, HUWE1, and UBE3A
NPLLLVS
O96780, O96787, O96788, Q9BMX8, Q9GU36, Q9GU37, Q9NDA1, Q9NDA2, Q9NDA3, Q9NHC5, Q9NHC6, Q9U793, Q9U794, Q9XZG5 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-methylcoumarin
NPLLNVS
O96780, O96787, O96788, Q9BMX8, Q9GU36, Q9GU37, Q9NDA1, Q9NDA2, Q9NDA3, Q9NHC5, Q9NHC6, Q9U793, Q9U794, Q9XZG5 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
ONX0912
-
a selective, irreversible inhibitor of the chymotrypsin-like activity of constitutive proteasome 20S and immunoproteasome 20S. ONX0912 exerts toxicity in Waldenstroem macroglobulinemia cells, by reducing bone marrow-derived interleukin-6 and insulin-like growth factor 1 secretion, thus inhibiting BM-induced p-Akt and phosphorylated extracellular signal-related kinase activation in Waldenstroem macroglobulinemia cells, overview. ONX0912 acts synergistically with bortezomib
p-chloromercuribenzoic acid
p65/relA
-
inhibits the degradation of IkappaBalpha by the proteasome
-
PA28
-
inhibition of the protease activities of the of the 20S- and 26S proteasome in all larvaeal stages, overview
-
pepstatin
-
0.0133 mg/ml 76.09% inhibition
phenylmethylsulfonyl fluoride
prion protein
-
recombinant mouse aggregated beta-PrP binds directly to human 20S and 26S proteasomes, i.e. its 20S core particle, overview. Conversion of cellular prion protein, PrPC, to toxic beta-sheet isoforms, PrPSc, which inhibit the ubiquitin-proteasome system and lead to accumulation of the system substrates, are associated with the prion diseases. PrP aggregates inhibit by stabilising the closed conformation of the substrate entry channel. The 20S proteasome is not inhibited when the gate in the alpha-ring is open due to a truncation mutation or by association with PA26/PA28. Modelling of location of aggregated beta-sheet rich PrP binding to the 20S proteasome and inhibition mechanism, detailed overview
-
pro-epigallocatechin-3-gallate
-
i.e. pro-EGCG, inhibitory efficacy is greatly improved from 42% inhibition to 89% inhibition when combined with 3,5-dinitrocatechol
PSI
-
0.1 mM, 93% inhibition of hydrolysis of succinyl-Leu-leu-Val-Tyr-7-amido-4-methylcoumarin, no inhibition of hydrolysis of tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin and benzyloxycarbonyl-Leu-Leu-Leu-7-amido-4-methylcoumarin, complete inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin
syringolin A methyl ester
-
-
-
syringolin B
-
SylB, synthesis and inhibitory potency, overview
TLCK
-
0.133 mg/ml, 79.57% inhibition
YLLLVS
O96780, O96787, O96788, Q9BMX8, Q9GU36, Q9GU37, Q9NDA1, Q9NDA2, Q9NDA3, Q9NHC5, Q9NHC6, Q9U793, Q9U794, Q9XZG5 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
Z-b-Ala-Val-Ser-Leu-vinyl ester
-
-
Z-beta-Ala-Leu-Leu-Leu-vinyl ester
-
-
Z-Gly-Leu-Leu-Leu-vinyl ester
-
-
Z-Gly-Val-Ser-Leu-vinyl ester
-
-
Z-NH-(CH2)3-CO-Leu-Leu-Leu-vinyl ester
-
-
Z-NH-(CH2)3-CO-Val-Ser-Leu-vinyl ester
-
-
Z-NH-(CH2)4-CO-Leu-Leu-Leu-vinyl ester
-
-
Z-NH-(CH2)4-CO-Val-Ser-Leu-vinyl ester
-
-
Z-NH-(CH2)5-CO-Leu-Leu-Leu-vinyl ester
-
-
Z-NH-(CH2)5-CO-Val-Ser-Leu-vinyl ester
-
-
Z-NH-(CH2)6-CO-Leu-Leu-Leu-vinyl ester
-
-
Z-NH-(CH2)6-CO-Val-Ser-Leu-vinyl ester
-
-
Z-NH-(CH2)7-CO-Leu-Leu-Leu-vinyl ester
-
-
Z-NH-(CH2)7-CO-Val-Ser-Leu-vinyl ester
-
-
Zn2+
-
inhibits peptidylglutamyl peptide hydrolase activity
[Cu(HLI)(LI)]OAc
-
a copper complex, HLI is the ligand 2,4-diiodo-6-((pyridine-2-ylmethylamino)methyl)phenol, causes selective 20S proteasomal inhibition and apoptosis induction in several lines of cancer cells
-
1-[1-(1-[(2,4-dioxoimidazolidin-1-ylimino)-methyl]-2-phenyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol)
-
i.e. S-2209, potently inhibits chymotrypsin-like proteasome activity of the human 20S proteasome. S-2209 targets NFkappaB activity, overview. S-2209 inhibits cell growth and induces apoptosis in human multiple myeloma cells, mechanisms, overview
1-[1-(1-[(2,4-dioxoimidazolidin-1-ylimino)-methyl]-2-phenyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol)
-
i.e. S-2209, targets NFkappaB activity, overview
3,4-dichloroisocoumarin
-
-
3,4-dichloroisocoumarin
-
benzyloxycarbonyl-GGL-4-nitroanilide as substrate
3,4-dichloroisocoumarin
-
-
3,4-dichloroisocoumarin
-
-
3,4-dichloroisocoumarin
-
-
3,4-dichloroisocoumarin
-
-
acetyl-Ala-Pro-norleucine-Leu-Asp-aldehyde
-
99% inhibition of hydrolysis of acetyl-norleucine-Leu-Pro-norleucine-Leu-Asp-7-amido-4-methylcoumarin, complete inhibition of hydrolysis of acetyl-norleucine-GPLD-7-amido-4-methylcoumarin, 95% inhibition of hydrolysis of acetyl-GPLL-7-amido-4-methylcoumarin, 89% inhibition of hydrolysis of acetyl-Ala-Pro-norleucine-Leu-Leu-7-amido-4-methylcoumarin, 24% inhibition of hydrolysis of succinyl-LLVY-7-amido-4-methylcoumarin, no inhibition of hydrolysis of tert-butyloxycarbonyl-LRR-7-amino-4-methylcoumarin
acetyl-Ala-Pro-norleucine-Leu-Asp-aldehyde
-
-
antipain
-
0.0133 mg/ml, 74.04% inhibition
benzyloxycarbonyl-Pro-norleucine-Leu-Asp-aldehyde
-
99% inhibition of hydrolysis of acetyl-norleucine-Leu-Pro-norleucine-Leu-Asp-7-amino-4-methylcoumarin, complete inhibition of hydrolysis of acetyl-norleucine-GPLD-7-amido-4-methylcoumarin, 95% inhibition of hydrolysis of acetyl-GPLL-7-amido-4-methylcoumarin, 91% inhibition of hydrolysis of acetyl-Ala-Pro-norleucine-Leu-Leu-7-amido-4-methylcoumarin, 12% inhibition of hydrolysis of succinyl-LLVY-7-amido-4-methylcoumarin, no inhibition of hydrolysis of tert-butyloxycarbonyl-LRR-7-amido-4-methylcoumarin
benzyloxycarbonyl-Pro-norleucine-Leu-Asp-aldehyde
-
-
bortezomib
-
ONX0912 acts synergistically with bortezomib
bortezomib
-
induces apoptosis in primary myeloma cells, but causes no induction of apoptosis in peripheral blood mononuclear cells from healthy humans
bortezomib
-
the proteasome inhibitor bortezomib sensitizes previously resistant tumor cells, melanoma cells, for cytolytic T-cell attack
bortezomib
-
activates the mitochondrial pathway of apoptosis in activated CD4+ T cells by disrupting the equilibrium of pro-apoptotic and anti-apoptotic proteins at the outer mitochondrial membrane and by inducing the generation of reactive oxygen species
bortezomib
-
slow-binding inhibitor, kinetic analysis
bortezomib
-
proteasome inhibition with bortezomib led to an increased susceptibility to viral infection, e.g. with lymphocytic choriomeningitis virus, and proteasome inhibitors can alter Ag processing in vivo
bortezomib
-
i.e. [(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic acid, treatment of human respiratory syncytial virus-infected Balb/C mice with the proteasome inhibitor results in increased inflammation and mortality, in contrast to infected Vero cells, overview
bortezomib
-
an N-terminally blocked Phe-Leu dipeptide inhibitor containing a C-terminal boronic acid, inhibits chymotrypsin-likeand caspase-like actitivities of the proteasome, inhibitory pattern with the chymotrypsin-like activity of the intermediate-proteasome subtypes, overview
bortezomib
-
also termed VELCADE
Ca2+
-
-
Ca2+
-
inhibits peptidylglutamyl peptide hydrolase activity
Ca2+
-
significantly stimulates activity of the 20S proteasome at pH 7.5, completely inhibits at pH 5.5
carfilzomib
-
irreversible
carfilzomib
-
irreversible
CEP-18770
-
reversible
chymostatin
-
0.05 mg/ml, 98% inhibition of chymotrypsin-like activity, hydrolysis of benzyloxycarbonyl-GGL-4-nitroanilide. 0.05 mg/ml, 15% inhibition of trypsin-like activity, hydrolysis of benzyloxycarbonyl-GGR-2-naphthylamide
chymostatin
-
0.1 mM, 93% inhibition of hydrolysis of succinyl-Leu-leu-Val-Tyr-7-amido-4-methylcoumarin, 94% inhibition of hydrolysis of tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin, no inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Leu-7-amido-4-methylcoumarin, 93% inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin
chymostatin
-
partial inhibition
chymostatin
-
inhibits chymotrypsin-like activity
chymostatin
-
inhibits chymotrypsin-like activity
epoxomicin
-
-
epoxomicin
-
inhibition of the protease activities of the of the 20S- and 26S proteasome in all larvaeal stages, overview
epoxomicin
-
irreversible inhibitor
epoxomicin
-
inhibits the proteasome and causes cell cycle arrest at G2/M
epoxomicin
-
EPOX, a specific proteasome inhibitor, abolishes chymotrypsin-like activity in both wild-type 20S and a3DN 20S mutant proteasomes after pre-treatment with 50 mM epoxomicin
epoxomicin
-
inhibits trypsin-like activity
epoxomycin
-
effect on mRNA and protein abundance in HeLa cells, overview
epoxomycin
-
effect on mRNA and protein abundance in NIH-3T3 and N2A cells, overview
epoxomycin
-
effect on mRNA and protein abundance in PC-12 cells, overview
H2O2
A0A286S218; A0A286S1Z7; A0A286S200
stable until 0.04 mM
H2O2
-
30% inhibition at 0.003 mM
K+
-
-
K+
-
inhibits peptidylglutamyl peptide hydrolase activity
lactacystin
-
-
lactacystin
-
effect on mRNA and protein abundance in HeLa cells, overview
lactacystin
-
a specific proteasome inhibitor
lactacystin
-
specific inhibitor of the proteasome, partial inhibition of proteasome activity enhances remyelination after cuprizone-induced demyelination, overview
lactacystin
-
effect on mRNA and protein abundance in NIH-3T3 and N2A cells, overview
lactacystin
-
effect on mRNA and protein abundance in PC-12 cells, overview
leupeptin
-
0.0133 mg/ml, 53.19% inhibition
leupeptin
-
0.05 mg/ml, 25% inhibition of chymotrypsin-like activity, hydrolysis of benzyloxycarbonyl-GGL-4-nitroanilide. 0.05 mg/ml, 88% inhibition of trypsin-like activity, hydrolysis of benzyloxycarbonyl-GGR-2-naphthylamide
leupeptin
-
inhibits trypsin-like activity
leupeptin
-
inhibits trypsin-like activity
leupeptin
-
inhibits trypsin-like activity
leupeptin
-
inhibits trypsin-like activity
leupeptin
-
inhibits trypsin-like activity
leupeptin
O96780, O96787, O96788, Q9BMX8, Q9GU36, Q9GU37, Q9NDA1, Q9NDA2, Q9NDA3, Q9NHC5, Q9NHC6, Q9U793, Q9U794, Q9XZG5 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
MG-132
-
reversible inhibitor
MG115
-
-
MG115
-
0.1 mM, 99% inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin, 80% inhibition of hydrolysis of tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin, 61% inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Leu-7-amido-4-methylcoumarin, complete inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin
MG132
-
-
MG132
-
effect on mRNA and protein abundance in HeLa cells, overview
MG132
-
effect on mRNA and protein abundance in NIH-3T3 and N2A cells, overview
MG132
-
0.1 mM, 98% inhibition of hydrolysis of succinyl-Leu-leu-Val-Tyr-7-amido-4-methylcoumarin, 13% inhibition of hydrolysis of tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin, 82% inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Leu-7-amido-4-methylcoumarin, complete inhibition of hydrolysis of benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin
MG132
-
31% residual chymotrypsin-like activity at 0.04 mM, 24% residual trypsin-like activity at 0.04 mM, and complete inhibition of caspase-activity of the 26S proteasome at 0.02 mM
MG132
-
i.e. Z-Leu-Leu-Leu-aldehyde, inhibits the chymotrypsin-like proteasome activity, inhibitory pattern with the chymotrypsin-like activity of the intermediate-proteasome subtypes, overview. Does not affect the caspase-like activity of subtypes II-2, I,-3, and I-4 at all
MG132
-
effect on mRNA and protein abundance in PC-12 cells
Mg2+
-
inhibits trypsin like activity
Mg2+
-
inhibits peptidylglutamyl peptide hydrolase activity
Mg2+
-
significantly stimulates activity of the 20S proteasome at pH 7.5, completely inhibits at pH 5.5
MLN9708
-
an N-capped dipeptidyl leucine boronic acid, a potent inhibitor of the proteasome in tumor cells
MLN9708
-
an N-capped dipeptidyl leucine boronic acid, a potent inhibitor of the proteasome in tumor cells
N-ethylmaleimide
-
1.0 mM, 31.91% inhibition
N-ethylmaleimide
-
inhibits trypsin-like and chymotrypsin-like activities
NPI-0052
-
irreversible
p-chloromercuribenzoic acid
-
0.1 mM, 6.4% inhibition
p-chloromercuribenzoic acid
-
-
p-chloromercuribenzoic acid
-
-
phenylmethylsulfonyl fluoride
-
0.1 mM, 75.36% inhibition
phenylmethylsulfonyl fluoride
-
inhibits trypsin-like activity
phenylmethylsulfonyl fluoride
-
-
PS-341
-
use in cancer therapy
PS-341
-
reversible inhibitor
SDS
-
trypsin-like activity, hydrolysis of benzyloxycarbonyl-GGR-2-naphthylamide
SDS
-
inhibits trypsin-like and chymotrypsin-like activities
SDS
-
inhibits peptidylglutamyl peptide hydrolase activity
SDS
-
significantly stimulates activity of the 20S proteasome at pH 7.5, completely inhibits at pH 5.5
SDS
-
inhibits trypsin-like activity
syringolin A
-
SylA, synthesis and inhibitory potency, overview
syringolin A
-
a tripeptide derivative, from Pseudomonas putida pv. syringae B728a, consisting of an N-terminal valine followed by the two non-proteinogenic amino acids 3,4-dehydrolysine and 5-methyl-4-amino-2-hexenoic acid, the latter two forming a twelve-membered macrolactam ring, irreversibly inhibits the eukaryotic proteasome, mechanism, overview. The biosynthesis of the compound involves genes sylA-sylE, structure, overview
Yu101
-
-
Yu101
-
Nrf1-/- mouse embryonic fibroblasts are impaired in the recovery of proteasome activity after transient treatment with the covalent proteasome inhibitor YU101
[Au(ESDT)]2
-
i.e. AUL15, a gold(I)-dithiocarbamato species, inhibits the chymotrypsin-like activity of purified 20S proteasome and 26S proteasome in breast cancer cells
[Au(ESDT)]2
-
i.e. AUL15, a gold(I)-dithiocarbamato species, inhibits the chymotrypsin-like activity of purified 20S proteasome
[AuBr2(ESDT)]
-
i.e. AUL12, a gold(III)-dithiocarbamato species, inhibits the chymotrypsin-like activity of purified 20S proteasome and 26S proteasome in breast cancer cells
[AuBr2(ESDT)]
-
i.e. AUL12, a gold(III)-dithiocarbamato species, inhibits the chymotrypsin-like activity of purified 20S proteasome
additional information
-
proteasome inhibition by lipofuscin/ceroid during postmitotic aging of fibroblasts
-
additional information
-
inhibition of purified 20S proteasome and 26S proteasome activities by epigallocatechin-3-gallate and its analogues, overview
-
additional information
-
design and synthesis of boron peptide analogue proteasome inhibitors based on the structure of belactosin C, overview
-
additional information
-
study of potent and selective inhibition of the 20S proteasome beta1 catalytic subsite by a series of vinyl ester cyclopeptide analogues synthesized on the basis of a class of cyclopeptides derived from linear prototype inhibitors, in which the exocyclic pharmacophoric unit Leu-vinyl ester is linked to the c-carboxyl group of the glutamic acid residue at the C-terminus. The compounds inhibit the caspase-like activity of the proteasome at nanomolar concentrations, and demonstrate good resistance to proteolysis and a capacity to permeate the cell membrane
-
additional information
-
screening of compounds for in vitro capacity to inhibit the chymotryptic-, tryptic-like, and post-acidic activities of the proteasome, overview. Detection of N-terminal-prolonged vinyl ester-based peptides as selective proteasome beta1 subunit inhibitors. The inhibitors demonstrate resistance to plasmatic proteases and a good capacity to permeate the cell membrane, but low inhibitory potencies. Inhibitors of the post-acidic activity of proteasomes neither induce cell death nor greatly inhibit cell proliferation
-
additional information
-
MLN9708 has a shorter proteasome dissociation half-life and improved pharmacokinetics, pharmacodynamics, and antitumor activity compared with bortezomib in clinical trials
-
additional information
-
assignment of species [CuLI]+ as the minimal pharmacophore needed for proteasomal chymotryspin-like activity inhibition, copper complex synthesis and structures, overview. The proteasomal chymotrypsin-like activity is inhibited by 45%, 60%,70% and 80% after 2, 4, 8, and 18 h, respectively, by the copper complexes in C4-2B prostate cancer cells, overview
-
additional information
-
gold(I)- and gold(III)-compound-mediated proteasome inhibition and cell death induction are completely reversed by the addition of reducing agents, e.g. dithiothreitol or N-acetyl-L-cysteine
-
additional information
-
detection of drug-like proteasome inhibitrs by a multistep structure-based virtual ligand screening strategy, effects on trypsin-like, chymotrypsin-like, and post-acidic proteasome activities, overview
-
additional information
-
syrbactins, a family of natural products produced by strains of the plant pathogen Pseudomonas syringae pv. syringae, that belong either to the syringolin or glidobactin class, are highly potent proteasome inhibitors
-
additional information
-
no direct inhibition of the proteasome by LY294002, but treatment with phosphatidylinositol-3 kinase inhibitors LY294002 or wortmannin, leads to increased levels of PS1/gamma-secretase components through an inhibitory effect on their degradation. Phosphatidylinositol-3 kinase inhibition may trigger the multiple mono-ubiquitination of PS1, which precludes the degradation of PS1/gamma-secretase through the proteasomal pathway, overview
-
additional information
-
MLN9708 has a shorter proteasome dissociation half-life and improved pharmacokinetics, pharmacodynamics, and antitumor activity compared with bortezomib in clinical trials
-
additional information
-
although inhibitors of the caspase-like sites allosterically inhibit the chymotrypsin-like activity, inhibitors of the caspase-like sites allosterically inhibit the chymotrypsin-like activity. When caspase-like sites are occupied by the uncleaved propeptide or inhibitor, their substrates still inhibit the chymotrypsin like activity
-
additional information
-
gold(I)- and gold(III)-compound-mediated proteasome inhibition and cell death induction are completely reversed by the addition of reducing agents, e.g. dithiothreitol or N-acetyl-L-cysteine
-
additional information
-
design and screening method development for protease inhibitors, that do not induce the proteasome, overview
-