Application | Comment | Organism |
---|---|---|
medicine | because of its central role in the ceramide metabolism, the enzyme may offer a novel molecular target in disorders with dysfunctional ceramide-mediated signaling | Homo sapiens |
medicine | because of its central role in the ceramide metabolism, the enzyme may offer a novel molecular target in disorders with dysfunctional ceramide-mediated signaling | Mus musculus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide | - |
Homo sapiens | |
2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide | - |
Mus musculus | |
6-(4-fluorophenyl)-2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide | - |
Homo sapiens | |
6-(4-fluorophenyl)-2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide} | in vivo plasma pharmacokinetic profile in mice, overview | Mus musculus | |
6-bromo-2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide | - |
Homo sapiens | |
6-bromo-2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide | - |
Mus musculus | |
additional information | a class of benzoxazolone carboxamides act as the first potent and systemically active inhibitors of the acid ceramidase. Prototype members of this class inhibit the enzyme with low nanomolar potency by covalent binding to the catalytic cysteine. No inhibition by N-methyl-2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide, 4-phenylbutyl 2-oxo-1,3-benzoxazole-3(2H)-carboxylate, and 3-(6-phenylhexanoyl)-1,3-benzoxazol-2(3H)-one, while 2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carbothioamide is unstable | Homo sapiens | |
additional information | a class of benzoxazolone carboxamides act as the first potent and systemically active inhibitors of the acid ceramidase. Prototype members of this class inhibit the enzyme with low nanomolar potency by covalent binding to the catalytic cysteine. No inhibition by N-methyl-2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide, 4-phenylbutyl 2-oxo-1,3-benzoxazole-3(2H)-carboxylate, and 3-(6-phenylhexanoyl)-1,3-benzoxazol-2(3H)-one, while 2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carbothioamide is unstable | Mus musculus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
N-acylsphingosine + H2O | Homo sapiens | the carboxylate is a fatty acid | carboxylate + sphingosine | - |
? | |
N-acylsphingosine + H2O | Mus musculus | the carboxylate is a fatty acid | carboxylate + sphingosine | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q13510 | - |
- |
Mus musculus | Q9WV54 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
brain | - |
Mus musculus | - |
colon | - |
Mus musculus | - |
colon adenocarcinoma cell | - |
Homo sapiens | - |
heart | - |
Mus musculus | - |
hippocampus | - |
Mus musculus | - |
kidney | - |
Mus musculus | - |
liver | - |
Mus musculus | - |
lung | - |
Mus musculus | - |
pancreas | - |
Mus musculus | - |
RAW-264.7 cell | - |
Mus musculus | - |
SW-403 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
N-acylsphingosine + H2O | the carboxylate is a fatty acid | Homo sapiens | carboxylate + sphingosine | - |
? | |
N-acylsphingosine + H2O | the carboxylate is a fatty acid | Mus musculus | carboxylate + sphingosine | - |
? |
Synonyms | Comment | Organism |
---|---|---|
acid ceramidase | - |
Homo sapiens |
acid ceramidase | - |
Mus musculus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
37 | - |
assay at | Mus musculus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
7.4 | - |
assay at | Mus musculus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000031 | - |
pH 7.4, 37°C | Homo sapiens | 6-bromo-2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide | |
0.000064 | - |
pH 7.4, 37°C | Homo sapiens | 2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide | |
0.000079 | - |
pH 7.4, 37°C | Homo sapiens | 6-(4-fluorophenyl)-2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3(2H)-carboxamide |
General Information | Comment | Organism |
---|---|---|
physiological function | ceramide hydrolysis by acid ceramidase stops the biological activity of ceramides and influences survival and function of normal and neoplastic cells | Homo sapiens |
physiological function | ceramide hydrolysis by acid ceramidase stops the biological activity of ceramides and influences survival and function of normal and neoplastic cells | Mus musculus |