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Literature summary for 2.3.1.26 extracted from

  • Ikenoya, M.; Yoshinaka, Y.; Kobayashi, H.; Kawamine, K.; Shibuya, K.; Sato, F.; Sawanobori, K.; Watanabe, T.; Miyazaki, A.
    A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels (2007), Atherosclerosis, 191, 290-297.
    View publication on PubMed
Search for more literature for 2.3.1.26

Application

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(Commentary)

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

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 [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00462
-
 oleoyl-CoA
-
 Homo sapiens
0.00999
-
 oleoyl-CoA
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
44000
-
 determined by SDS-PAGE and Western Blot analysis Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
acyl-CoA + cholesterol Homo sapiens
-
 CoA + cholesterol ester
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
microsomal fractions of CHO cells are prepared Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
macrophage
-
 Homo sapiens
-
THP-1 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
ACAT-1
-
 Homo sapiens
ACAT-2
-
 Homo sapiens
acyl-coenzyme A:cholesterol O-acyltransferase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 ACAT activity assay Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.8
-
 ACAT activity assay Homo sapiens

Ki Value [mM]

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 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