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Literature summary extracted from

  • Ohshiro, T.; Rudel, L.L.; Omura, S.; Tomoda, H.
    Selectivity of microbial acyl-CoA: cholesterol acyltransferase inhibitors toward isozymes (2007), J. Antibiot., 60, 43-51.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.26 beauvericin IC50: 0.00035 mM, ACAT1; IC50: 0.00035 mM, ACAT2 Chlorocebus aethiops
2.3.1.26 beauvericin
-
 Cricetulus griseus
2.3.1.26 beauvericin
-
 Rattus norvegicus
2.3.1.26 beauveriolide I IC50: 0.0019 mM, ACAT2; IC50: 0.0022 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 beauveriolide I
-
 Cricetulus griseus
2.3.1.26 beauveriolide I
-
 Mus musculus
2.3.1.26 beauveriolide III IC50: 0.003 mM, ACAT1; IC50: 0.003 mM, ACAT2 Chlorocebus aethiops
2.3.1.26 beauveriolide III
-
 Cricetulus griseus
2.3.1.26 beauveriolide III
-
 Mus musculus
2.3.1.26 CL-283,546 IC50: 0.00006 mM, ACAT2; IC50: 0.00012 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 CL-283,546
-
 Cricetulus griseus
2.3.1.26 glisoprenin A IC50: 0.0004 mM, ACAT1; IC50: 0.0013 mM, ACAT2 Chlorocebus aethiops
2.3.1.26 glisoprenin A
-
 Cricetulus griseus
2.3.1.26 glisoprenin A
-
 Rattus norvegicus
2.3.1.26 K97-0239A IC50: 0.038 mM, ACAT2; IC50: 0.04 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 K97-0239A
-
 Cricetulus griseus
2.3.1.26 K97-0239A
-
 Mus musculus
2.3.1.26 K97-0239B IC50: above 0.07 mM, ACAT1; IC50: above 0.7 mM, ACAT2 Chlorocebus aethiops
2.3.1.26 K97-0239B
-
 Cricetulus griseus
2.3.1.26 K97-0239B
-
 Mus musculus
2.3.1.26 phenochalasin A IC50: above 0.1 mM, ACAT1; IC50: above 0.1 mM, ACAT2 Chlorocebus aethiops
2.3.1.26 phenochalasin A
-
 Cricetulus griseus
2.3.1.26 phenochalasin A
-
 Mus musculus
2.3.1.26 purpactin A IC50: 0.0009 mM, ACAT1; IC50: 0.0018 mM, ACAT2 Chlorocebus aethiops
2.3.1.26 purpactin A
-
 Cricetulus griseus
2.3.1.26 purpactin A
-
 Rattus norvegicus
2.3.1.26 purpactin B IC50: 0.012 mM, ACAT2; IC50: 0.022 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 purpactin B
-
 Cricetulus griseus
2.3.1.26 purpactin B
-
 Rattus norvegicus
2.3.1.26 purpactin C IC50: 0.028 mM, ACAT1; IC50: 0.03 mM, ACAT2 Chlorocebus aethiops
2.3.1.26 purpactin C
-
 Cricetulus griseus
2.3.1.26 purpactin C
-
 Rattus norvegicus
2.3.1.26 pyripyropene A IC50: 0.00006 mM, ACAT2; IC50: above 0.03 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 pyripyropene A
-
 Cricetulus griseus
2.3.1.26 pyripyropene A
-
 Rattus norvegicus
2.3.1.26 pyripyropene B IC50: 0.0008 mM, ACAT2; IC50: 0.03 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 pyripyropene B
-
 Cricetulus griseus
2.3.1.26 pyripyropene B
-
 Rattus norvegicus
2.3.1.26 pyripyropene C IC50: 0.00035 mM, ACAT2; IC50: 0.015 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 pyripyropene C
-
 Cricetulus griseus
2.3.1.26 pyripyropene C
-
 Rattus norvegicus
2.3.1.26 pyripyropene D IC50: 0.0012 mM, ACAT2; IC50: 0.015 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 pyripyropene D
-
 Cricetulus griseus
2.3.1.26 pyripyropene D
-
 Rattus norvegicus
2.3.1.26 sespendole IC50: 0.012 mM, ACAT2; IC50: 0.02 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 sespendole
-
 Cricetulus griseus
2.3.1.26 sespendole
-
 Mus musculus
2.3.1.26 spylidone IC50: 0.003 mM, ACAT2; IC50: 0.007 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 spylidone
-
 Cricetulus griseus
2.3.1.26 spylidone
-
 Mus musculus
2.3.1.26 terpendole C IC50: 0.0005 mM, ACAT2; IC50: 0.008 mM, ACAT1 Chlorocebus aethiops
2.3.1.26 terpendole C
-
 Cricetulus griseus
2.3.1.26 terpendole C
-
 Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.3.1.26 endoplasmic reticulum
-
 Cricetulus griseus 5783
-
2.3.1.26 endoplasmic reticulum
-
 Mus musculus 5783
-
2.3.1.26 endoplasmic reticulum
-
 Rattus norvegicus 5783
-
2.3.1.26 membrane
-
 Cricetulus griseus 16020
-
2.3.1.26 membrane
-
 Mus musculus 16020
-
2.3.1.26 membrane
-
 Rattus norvegicus 16020
-
2.3.1.26 microsome
-
 Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.26 acyl-CoA + cholesterol Cricetulus griseus
-
 CoA + cholesterol ester
-
 ?
2.3.1.26 acyl-CoA + cholesterol Mus musculus
-
 CoA + cholesterol ester
-
 ?
2.3.1.26 acyl-CoA + cholesterol Rattus norvegicus
-
 CoA + cholesterol ester
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.26 Chlorocebus aethiops
-
 ACAT1 expressed by CHO cells
-
2.3.1.26 Chlorocebus aethiops
-
 ACAT2 expressed by CHO cells
-
2.3.1.26 Cricetulus griseus
-
-
-
2.3.1.26 Mus musculus
-
-
-
2.3.1.26 Rattus norvegicus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.1.26 microsomes are prepared Cricetulus griseus
2.3.1.26 microsomes are prepared Rattus norvegicus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.1.26 CHO cell
-
 Cricetulus griseus
-
2.3.1.26 liver
-
 Rattus norvegicus
-
2.3.1.26 peritoneal macrophage
-
 Mus musculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.26 acyl-CoA + cholesterol
-
 Cricetulus griseus CoA + cholesterol ester
-
 ?
2.3.1.26 acyl-CoA + cholesterol
-
 Mus musculus CoA + cholesterol ester
-
 ?
2.3.1.26 acyl-CoA + cholesterol
-
 Rattus norvegicus CoA + cholesterol ester
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.26 ACAT
-
 Cricetulus griseus
2.3.1.26 ACAT
-
 Mus musculus
2.3.1.26 ACAT
-
 Rattus norvegicus
2.3.1.26 ACAT-1
-
 Cricetulus griseus
2.3.1.26 ACAT-2
-
 Cricetulus griseus
2.3.1.26 ACAT1
-
 Chlorocebus aethiops
2.3.1.26 ACAT2
-
 Rattus norvegicus
2.3.1.26 ACAT2
-
 Chlorocebus aethiops
2.3.1.26 acyl-CoA: cholesterol acyltransferase
-
 Cricetulus griseus
2.3.1.26 acyl-CoA: cholesterol acyltransferase
-
 Mus musculus
2.3.1.26 acyl-CoA: cholesterol acyltransferase
-
 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.26 37
-
 activity assay Cricetulus griseus
2.3.1.26 37
-
 activity assay Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.26 0.00006
-
 IC50: 0.00006 mM, ACAT2 Chlorocebus aethiops pyripyropene A
2.3.1.26 0.00006
-
 IC50: 0.00006 mM, ACAT2 Chlorocebus aethiops CL-283,546
2.3.1.26 0.00006
-
 enzyme assay Cricetulus griseus pyripyropene A
2.3.1.26 0.00006
-
 enzyme assay Cricetulus griseus CL-283,546
2.3.1.26 0.00007
-
 cell-based assay Cricetulus griseus pyripyropene A
2.3.1.26 0.00009
-
 cell-based assay Cricetulus griseus CL-283,546
2.3.1.26 0.0001
-
 cell-based assay Cricetulus griseus CL-283,546
2.3.1.26 0.00012
-
 IC50: 0.00012 mM, ACAT1 Chlorocebus aethiops CL-283,546
2.3.1.26 0.00012
-
 enzyme assay Cricetulus griseus CL-283,546
2.3.1.26 0.00013
-
-
 Rattus norvegicus beauvericin
2.3.1.26 0.00035
-
 IC50: 0.00035 mM, ACAT1 Chlorocebus aethiops beauvericin
2.3.1.26 0.00035
-
 IC50: 0.00035 mM, ACAT2 Chlorocebus aethiops pyripyropene C
2.3.1.26 0.00035
-
 IC50: 0.00035 mM, ACAT2 Chlorocebus aethiops beauvericin
2.3.1.26 0.00035
-
 enzyme assay Cricetulus griseus pyripyropene C
2.3.1.26 0.00035
-
 enzyme assay Cricetulus griseus beauvericin
2.3.1.26 0.00036
-
 cell-based assay Cricetulus griseus pyripyropene C
2.3.1.26 0.0004
-
 IC50: 0.0004 mM, ACAT1 Chlorocebus aethiops glisoprenin A
2.3.1.26 0.0004
-
 enzyme assay Cricetulus griseus glisoprenin A
2.3.1.26 0.00041
-
-
 Mus musculus beauveriolide III
2.3.1.26 0.0005
-
 IC50: 0.0005 mM, ACAT2 Chlorocebus aethiops terpendole C
2.3.1.26 0.0005
-
 enzyme assay Cricetulus griseus terpendole C
2.3.1.26 0.0006
-
-
 Mus musculus phenochalasin A
2.3.1.26 0.0006
-
 cell-based assay Cricetulus griseus beauveriolide I
2.3.1.26 0.0007
-
 cell-based assay Cricetulus griseus beauvericin
2.3.1.26 0.00078
-
-
 Mus musculus beauveriolide I
2.3.1.26 0.0008
-
 IC50: 0.0008 mM, ACAT2 Chlorocebus aethiops pyripyropene B
2.3.1.26 0.0008
-
 enzyme assay Cricetulus griseus pyripyropene B
2.3.1.26 0.0009
-
 IC50: 0.0009 mM, ACAT1 Chlorocebus aethiops purpactin A
2.3.1.26 0.0009
-
 cell-based assay Cricetulus griseus beauveriolide III
2.3.1.26 0.0009
-
 enzyme assay Cricetulus griseus purpactin A
2.3.1.26 0.0012
-
 IC50: 0.0012 mM, ACAT2 Chlorocebus aethiops pyripyropene D
2.3.1.26 0.0012
-
 enzyme assay Cricetulus griseus pyripyropene D
2.3.1.26 0.0013
-
 IC50: 0.0013 mM, ACAT2 Chlorocebus aethiops glisoprenin A
2.3.1.26 0.0013
-
 enzyme assay Cricetulus griseus glisoprenin A
2.3.1.26 0.0015
-
-
 Mus musculus K97-0239A
2.3.1.26 0.0015
-
 cell-based assay Cricetulus griseus pyripyropene D
2.3.1.26 0.0015
-
 cell-based assay Cricetulus griseus purpactin A
2.3.1.26 0.0017
-
-
 Mus musculus K97-0239B
2.3.1.26 0.0018
-
 IC50: 0.0018 mM, ACAT2 Chlorocebus aethiops purpactin A
2.3.1.26 0.0018
-
 enzyme assay Cricetulus griseus purpactin A
2.3.1.26 0.0019
-
 IC50: 0.0019 mM, ACAT2 Chlorocebus aethiops beauveriolide I
2.3.1.26 0.0019
-
 enzyme assay Cricetulus griseus beauveriolide I
2.3.1.26 0.002
-
 cell-based assay Cricetulus griseus pyripyropene B
2.3.1.26 0.002
-
 cell-based assay Cricetulus griseus beauvericin
2.3.1.26 0.0022
-
 IC50: 0.0022 mM, ACAT1 Chlorocebus aethiops beauveriolide I
2.3.1.26 0.0022
-
 enzyme assay Cricetulus griseus purpactin B
2.3.1.26 0.0022
-
 enzyme assay Cricetulus griseus beauveriolide I
2.3.1.26 0.0025
-
-
 Rattus norvegicus terpendole C
2.3.1.26 0.0025
-
 cell-based assay Cricetulus griseus purpactin A
2.3.1.26 0.0028
-
 enzyme assay Cricetulus griseus purpactin C
2.3.1.26 0.003
-
 IC50: 0.003 mM, ACAT1 Chlorocebus aethiops beauveriolide III
2.3.1.26 0.003
-
 IC50: 0.003 mM, ACAT2 Chlorocebus aethiops spylidone
2.3.1.26 0.003
-
 IC50: 0.003 mM, ACAT2 Chlorocebus aethiops beauveriolide III
2.3.1.26 0.003
-
 enzyme assay Cricetulus griseus spylidone
2.3.1.26 0.003
-
 enzyme assay Cricetulus griseus beauveriolide III
2.3.1.26 0.004
-
-
 Mus musculus sespendole
2.3.1.26 0.0043
-
 cell-based assay Cricetulus griseus glisoprenin A
2.3.1.26 0.0045
-
-
 Rattus norvegicus purpactin A
2.3.1.26 0.005
-
 cell-based assay Cricetulus griseus spylidone
2.3.1.26 0.0057
-
 cell-based assay Cricetulus griseus purpactin B
2.3.1.26 0.0065
-
 cell-based assay Cricetulus griseus sespendole
2.3.1.26 0.007
-
 IC50: 0.007 mM, ACAT1 Chlorocebus aethiops spylidone
2.3.1.26 0.007
-
 enzyme assay Cricetulus griseus spylidone
2.3.1.26 0.008
-
 IC50: 0.008 mM, ACAT1 Chlorocebus aethiops terpendole C
2.3.1.26 0.008
-
 enzyme assay Cricetulus griseus terpendole C
2.3.1.26 0.009
-
 cell-based assay Cricetulus griseus K97-0239A
2.3.1.26 0.01
-
 cell-based assay Cricetulus griseus purpactin B
2.3.1.26 0.01
-
 cell-based assay Cricetulus griseus glisoprenin A
2.3.1.26 0.01
-
 cell-based assay Cricetulus griseus purpactin C
2.3.1.26 0.01
-
 cell-based assay Cricetulus griseus terpendole C
2.3.1.26 0.012
-
-
 Rattus norvegicus glisoprenin A
2.3.1.26 0.012
-
 IC50: 0.012 mM, ACAT2 Chlorocebus aethiops purpactin B
2.3.1.26 0.012
-
 IC50: 0.012 mM, ACAT2 Chlorocebus aethiops sespendole
2.3.1.26 0.012
-
 cell-based assay Cricetulus griseus sespendole
2.3.1.26 0.012
-
 enzyme assay Cricetulus griseus purpactin B
2.3.1.26 0.012
-
 enzyme assay Cricetulus griseus sespendole
2.3.1.26 0.013
-
 cell-based assay Cricetulus griseus K97-0239A
2.3.1.26 0.013
-
 cell-based assay Cricetulus griseus K97-0239B
2.3.1.26 0.015
-
 IC50: 0.015 mM, ACAT1 Chlorocebus aethiops pyripyropene C
2.3.1.26 0.015
-
 IC50: 0.015 mM, ACAT1 Chlorocebus aethiops pyripyropene D
2.3.1.26 0.015
-
 enzyme assay Cricetulus griseus pyripyropene C
2.3.1.26 0.015
-
 enzyme assay Cricetulus griseus pyripyropene D
2.3.1.26 0.018
-
-
 Rattus norvegicus purpactin C
2.3.1.26 0.02
-
-
 Rattus norvegicus purpactin B
2.3.1.26 0.02
-
 IC50: 0.02 mM, ACAT1 Chlorocebus aethiops sespendole
2.3.1.26 0.02
-
 cell-based assay Cricetulus griseus beauveriolide I
2.3.1.26 0.02
-
 cell-based assay Cricetulus griseus beauveriolide III
2.3.1.26 0.02
-
 cell-based assay Cricetulus griseus phenochalasin A
2.3.1.26 0.02
-
 enzyme assay Cricetulus griseus sespendole
2.3.1.26 0.022
-
 IC50: 0.022 mM, ACAT1 Chlorocebus aethiops purpactin B
2.3.1.26 0.025
-
 cell-based assay Cricetulus griseus spylidone
2.3.1.26 0.028
-
 IC50: 0.028 mM, ACAT1 Chlorocebus aethiops purpactin C
2.3.1.26 0.03
-
 IC50: 0.03 mM, ACAT1 Chlorocebus aethiops pyripyropene B
2.3.1.26 0.03
-
 IC50: 0.03 mM, ACAT2 Chlorocebus aethiops purpactin C
2.3.1.26 0.03
-
 IC50: above 0.03 mM, ACAT1 Chlorocebus aethiops pyripyropene A
2.3.1.26 0.03
-
 enzyme assay Cricetulus griseus pyripyropene A
2.3.1.26 0.03
-
 enzyme assay Cricetulus griseus pyripyropene B
2.3.1.26 0.03
-
 enzyme assay Cricetulus griseus purpactin C
2.3.1.26 0.032
-
 cell-based assay Cricetulus griseus pyripyropene C
2.3.1.26 0.035
-
-
 Rattus norvegicus pyripyropene D
2.3.1.26 0.038
-
-
 Rattus norvegicus pyripyropene B
2.3.1.26 0.038
-
 IC50: 0.038 mM, ACAT2 Chlorocebus aethiops K97-0239A
2.3.1.26 0.038
-
 cell-based assay Cricetulus griseus pyripyropene D
2.3.1.26 0.038
-
 enzyme assay Cricetulus griseus K97-0239A
2.3.1.26 0.04
-
-
 Rattus norvegicus pyripyropene C
2.3.1.26 0.04
-
 IC50: 0.04 mM, ACAT1 Chlorocebus aethiops K97-0239A
2.3.1.26 0.04
-
 enzyme assay Cricetulus griseus K97-0239A
2.3.1.26 0.042
-
-
 Mus musculus spylidone
2.3.1.26 0.048
-
 cell-based assay Cricetulus griseus pyripyropene B
2.3.1.26 0.07
-
 IC50: above 0.07 mM, ACAT1 Chlorocebus aethiops K97-0239B
2.3.1.26 0.07
-
 enzyme assay Cricetulus griseus K97-0239B
2.3.1.26 0.08
-
-
 Rattus norvegicus pyripyropene A
2.3.1.26 0.08
-
 cell-based assay Cricetulus griseus pyripyropene A
2.3.1.26 0.1
-
 IC50: above 0.1 mM, ACAT1 Chlorocebus aethiops phenochalasin A
2.3.1.26 0.1
-
 IC50: above 0.1 mM, ACAT2 Chlorocebus aethiops phenochalasin A
2.3.1.26 0.1
-
 enzyme assay Cricetulus griseus phenochalasin A
2.3.1.26 0.7
-
 IC50: above 0.7 mM, ACAT2 Chlorocebus aethiops K97-0239B