Application | Comment | Organism |
---|---|---|
pharmacology | K-604, a potent and selective inhibitor of ACAT-1, suppresses the development of atherosclerosis in an animal model without affecting plasma cholesterol levels, providing direct evidence that pharmacological inhibition of ACAT-1 in the arterial walls leads to suppression of atherosclerosis | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
CHO cells stably overexpressing human ACAT-1 are used | Homo sapiens |
CHO cells stably overexpressing human ACAT-2 are used | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide | K-604 | Homo sapiens | |
CI-1011 | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00462 | - |
oleoyl-CoA | - |
Homo sapiens | |
0.00999 | - |
oleoyl-CoA | - |
Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
44000 | - |
determined by SDS-PAGE and Western Blot analysis | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
acyl-CoA + cholesterol | Homo sapiens | - |
CoA + cholesterol ester | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
microsomal fractions of CHO cells are prepared | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
macrophage | - |
Homo sapiens | - |
THP-1 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
acyl-CoA + cholesterol | - |
Homo sapiens | CoA + cholesterol ester | - |
? | |
oleoyl-CoA + cholesterol | activity assay | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
ACAT-1 | - |
Homo sapiens |
ACAT-2 | - |
Homo sapiens |
acyl-coenzyme A:cholesterol O-acyltransferase | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
ACAT activity assay | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.8 | - |
ACAT activity assay | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000378 | - |
2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide | inhibition is competitive with respect to oleoyl-coenzyme A | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000068 | - |
inhibition of cholesterol esterification in human monocyte-derived macrophages | Homo sapiens | 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide | |
0.00045 | - |
recombinant ACAT-1, K-604 is 229-fold more selective for ACAT-1 than for ACAT-2 | Homo sapiens | 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide | |
0.01872 | - |
recombinant ACAT-1 | Homo sapiens | CI-1011 | |
0.01911 | - |
recombinant ACAT-2 | Homo sapiens | CI-1011 | |
0.1028 | - |
recombinant ACAT-2 | Homo sapiens | 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide |