Inhibitors | Comment | Organism | Structure |
---|---|---|---|
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 | Homo sapiens | |
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 | Rattus norvegicus | |
bortezomib | induces apoptosis in primary myeloma cells, but causes no induction of apoptosis in peripheral blood mononuclear cells from healthy humans | Homo sapiens | |
bortezomib | - |
Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
mononuclear cell | peripheral blood | Rattus norvegicus | - |
myeloma cell | primary, multiple | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
N-succinyl-LLVY-7-amido-4-methylcoumarin + H2O | chymotrypsin-like proteasome activity | Homo sapiens | N-succinyl-LLVY + 7-amino-4-methylcoumarin | - |
? | |
N-succinyl-LLVY-7-amido-4-methylcoumarin + H2O | chymotrypsin-like proteasome activity | Rattus norvegicus | N-succinyl-LLVY + 7-amino-4-methylcoumarin | - |
? | |
succinyl-LLVY-aminoluciferin + H2O | chymotrypsin-like proteasome activity | Homo sapiens | succinyl-LLVY + aminoluciferin | - |
? | |
succinyl-LLVY-aminoluciferin + H2O | chymotrypsin-like proteasome activity | Rattus norvegicus | succinyl-LLVY + aminoluciferin | - |
? |
Synonyms | Comment | Organism |
---|---|---|
20S proteasome | - |
Homo sapiens |
20S proteasome | - |
Rattus norvegicus |
proteasome | - |
Homo sapiens |
proteasome | - |
Rattus norvegicus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Homo sapiens |
37 | - |
assay at | Rattus norvegicus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
7.5 | - |
assay at | Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00022 | - |
pH 7.5, 30°C | Homo sapiens | 1-[1-(1-[(2,4-dioxoimidazolidin-1-ylimino)-methyl]-2-phenyl-ethylcarbamoyl)-2-(1H-indol-3-yl)-ethylcarbamoyl]-2-(1H-indol) |