Inhibitors | Comment | Organism | Structure |
---|---|---|---|
ethyl-2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate | i.e. HA14-1, a reversible small molecule Bcl-2 inhibitor that also inhibits GlcT-1 enzyme activity. HA14-1 is a competitive and mixed-type inhibitor with respect to C6-NBD-ceramide and UDP-glucose, respectively. HA-14 does not possess structural homology with the substrates UDP-glucose and ceramide. Possible binding of GlcT-1 to Bcl-2 | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q16739 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
B-16 cell | - |
Homo sapiens | - |
melanoma cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
UDP-glucose + 6-(((N-7-nitrobenz-2-oxa-1,3-diazol-4yl)amino)caproyl)sphingosine | - |
Homo sapiens | UDP + ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
GlcT-1 | - |
Homo sapiens |
UDP-glucose: ceramide glucosyltransferase | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0045 | - |
ethyl-2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate | pH 7.5, 30°C | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
additional information | the use of ethyl-2-amino-6-bromo-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate, i.e. HA14-1, as a Bcl-2 inhibitor in studies of apoptosis might produce misleading results, because HA14-1 can also affect a ceramide-mediated cell death pathway by inhibiting GlcT-1. Bcl-2 is a protein factor known to suppress apoptosis by binding and inactivating pro-apoptotic proteins such as Bax and BH3-only family proteins | Homo sapiens |