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Literature summary for 3.4.22.38 extracted from
- Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools (2009), Biol. Chem., 390, 941-948.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | cathepsin K is a target for the pharmacological treatment of osteoporosis | Mus musculus |
| medicine | cathepsin K is a target for the pharmacological treatment of osteoporosis | Homo sapiens |
| medicine | cathepsin K is a target for the pharmacological treatment of osteoporosis | Rattus norvegicus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| balicatib | high degree of potency and selectivity for purified human Cat K | Homo sapiens |  |
| balicatib | - |
Mus musculus | |
| balicatib | - |
Rattus norvegicus | |
| benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate | shows any degree of Cat K selectivity (10fold vs. Cat L and F) | Homo sapiens | |
| benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate | - |
Mus musculus | |
| benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate | - |
Rattus norvegicus | |
| BML-244 | has moderate selectivity (more than 30fold), but is a relatively weak inhibitor of human Cat K | Homo sapiens | |
| BML-244 | - |
Mus musculus | |
| BML-244 | - |
Rattus norvegicus | |
| Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z | - |
Homo sapiens | |
| Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z | - |
Mus musculus | |
| Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z | - |
Rattus norvegicus | |
| dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate | - |
Homo sapiens | |
| dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate | - |
Mus musculus | |
| dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate | - |
Rattus norvegicus | |
| K4b | potent, reversible, Cat K-selective inhibitor | Homo sapiens | |
| K4b | potent, reversible, Cat K-selective inhibitor | Mus musculus | |
| K4b | potent, reversible, Cat K-selective inhibitor | Rattus norvegicus | |
| L-873724 | high degree of potency and selectivity (more than 100fold) for purified human Cat K | Homo sapiens | |
| L-873724 | - |
Mus musculus | |
| L-873724 | - |
Rattus norvegicus | |
| additional information | not inhibited by pyrimidine nitrile | Homo sapiens | |
| additional information | not inhibited by pyrimidine nitrile | Mus musculus | |
| additional information | not inhibited by pyrimidine nitrile | Rattus norvegicus | |
| Mu-Leu-Hph-fluoromethylketone | highly potent versus Cat K, but is essentially non-selective versus all human cathepsins | Homo sapiens | |
| Mu-Leu-Hph-fluoromethylketone | - |
Mus musculus | |
| Mu-Leu-Hph-fluoromethylketone | - |
Rattus norvegicus | |
| NC-2300 | - |
Homo sapiens | |
| NC-2300 | - |
Mus musculus | |
| NC-2300 | - |
Rattus norvegicus | |
| odanacatib | high degree of potency and selectivity for purified human Cat K | Homo sapiens | |
| odanacatib | - |
Mus musculus | |
| odanacatib | - |
Rattus norvegicus | |
| relacatib | highly potent versus human Cat K, but lacks selectivity versus Cat L, S, and F | Homo sapiens | |
| relacatib | - |
Mus musculus | |
| relacatib | - |
Rattus norvegicus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Type I collagen + H2O | Mus musculus | - |
? | - |
? | |
| Type I collagen + H2O | Homo sapiens | - |
? | - |
? | |
| Type I collagen + H2O | Rattus norvegicus | - |
? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
| Oryctolagus cuniculus | - |
- |
- |
| Rattus norvegicus | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
- |
Mus musculus |
- |
Homo sapiens |
- |
Rattus norvegicus |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| dermal fibroblast | - |
Homo sapiens | - |
| HIG-82 cell | - |
Oryctolagus cuniculus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Type I collagen + H2O | - |
Mus musculus | ? | - |
? | |
| Type I collagen + H2O | - |
Homo sapiens | ? | - |
? | |
| Type I collagen + H2O | - |
Rattus norvegicus | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Cat K | - |
Mus musculus |
| Cat K | - |
Homo sapiens |
| Cat K | - |
Rattus norvegicus |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000002 | - |
pH and temperature not specified in the publication | Homo sapiens | odanacatib | |
| 0.0000002 | - |
pH and temperature not specified in the publication | Homo sapiens | L-873724 | |
| 0.0000006 | - |
pH and temperature not specified in the publication | Homo sapiens | benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate | |
| 0.0000007 | - |
pH and temperature not specified in the publication | Homo sapiens | relacatib | |
| 0.0000014 | - |
pH and temperature not specified in the publication | Homo sapiens | balicatib | |
| 0.0000023 | - |
pH and temperature not specified in the publication | Homo sapiens | Mu-Leu-Hph-fluoromethylketone | |
| 0.0000076 | - |
pH and temperature not specified in the publication | Rattus norvegicus | Mu-Leu-Hph-fluoromethylketone | |
| 0.000013 | - |
pH and temperature not specified in the publication | Homo sapiens | Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z | |
| 0.000018 | - |
pH and temperature not specified in the publication | Mus musculus | Mu-Leu-Hph-fluoromethylketone | |
| 0.00002 | - |
pH and temperature not specified in the publication | Rattus norvegicus | L-873724 | |
| 0.000035 | - |
pH and temperature not specified in the publication | Rattus norvegicus | benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate | |
| 0.000043 | - |
pH and temperature not specified in the publication | Mus musculus | L-873724 | |
| 0.000044 | - |
pH and temperature not specified in the publication | Mus musculus | benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate | |
| 0.000046 | - |
pH and temperature not specified in the publication | Homo sapiens | NC-2300 | |
| 0.000051 | - |
pH and temperature not specified in the publication | Rattus norvegicus | relacatib | |
| 0.000053 | - |
pH and temperature not specified in the publication | Homo sapiens | K4b | |
| 0.000056 | - |
pH and temperature not specified in the publication | Rattus norvegicus | balicatib | |
| 0.000066 | - |
pH and temperature not specified in the publication | Mus musculus | relacatib | |
| 0.000102 | - |
pH and temperature not specified in the publication | Mus musculus | NC-2300 | |
| 0.000108 | - |
pH and temperature not specified in the publication | Mus musculus | odanacatib | |
| 0.000112 | - |
pH and temperature not specified in the publication | Rattus norvegicus | odanacatib | |
| 0.000145 | - |
pH and temperature not specified in the publication | Mus musculus | K4b | |
| 0.000163 | - |
pH and temperature not specified in the publication | Homo sapiens | BML-244 | |
| 0.000181 | - |
pH and temperature not specified in the publication | Homo sapiens | dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate | |
| 0.000239 | - |
pH and temperature not specified in the publication | Rattus norvegicus | K4b | |
| 0.000269 | - |
pH and temperature not specified in the publication | Rattus norvegicus | Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z | |
| 0.000296 | - |
pH and temperature not specified in the publication | Mus musculus | Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z | |
| 0.000319 | - |
pH and temperature not specified in the publication | Rattus norvegicus | NC-2300 | |
| 0.00048 | - |
pH and temperature not specified in the publication | Mus musculus | balicatib | |
| 0.000748 | - |
pH and temperature not specified in the publication | Mus musculus | BML-244 | |
| 0.002106 | - |
pH and temperature not specified in the publication | Rattus norvegicus | BML-244 | |
| 0.002588 | - |
pH and temperature not specified in the publication | Rattus norvegicus | dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate | |
| 0.00426 | - |
pH and temperature not specified in the publication | Mus musculus | dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate | |
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