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Literature summary extracted from

  • Ohshiro, T.; Matsuda, D.; Nagai, K.; Doi, T.; Sunazuka, T.; Takahashi, T.; Rudel, L.L.; Omura, S.; Tomoda, H.
    The selectivity of beauveriolide derivatives in inhibition toward the two isozymes of acyl-CoA: cholesterol acyltransferase (2009), Chem. Pharm. Bull., 57, 377-381.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.26 expression of isoforms ACT1 and ACAT2 in CHO cell Chlorocebus aethiops

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.26 (6R,9S,13S)-3-benzyl-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone inhibition of both isoforms ACAT1 and ACAT2; inhibition of both isoforms ACAT1 and ACAT2 Chlorocebus aethiops
2.3.1.26 (6S,9S,13R)-9-(2-chlorobenzyl)-6-methyl-3-[(1S)-1-methylpropyl]-13-pentyl-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone selective inhibition of isoform ACAT1 Chlorocebus aethiops
2.3.1.26 (6S,9S,13S)-6-methyl-13-[(1S)-1-methylnonyl]-3-[(1S)-1-methylpropyl]-9-(naphthalen-2-ylmethyl)-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone selective inhibition of isoform ACAT2 Chlorocebus aethiops
2.3.1.26 (6S,9S,13S)-6-methyl-9-(4-methylbenzyl)-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone selective inhibition of isoform ACAT1 Chlorocebus aethiops
2.3.1.26 (6S,9S,13S)-9-(3-chlorobenzyl)-6-methyl-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone selective inhibition of isoform ACAT1 Chlorocebus aethiops
2.3.1.26 (6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1R)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone selective inhibition of isoform ACAT2 Chlorocebus aethiops
2.3.1.26 (6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone selective inhibition of isoform ACAT2 Chlorocebus aethiops

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.26 Chlorocebus aethiops O77759 isoform ACAT2
-
2.3.1.26 Chlorocebus aethiops O77760 isoform ACAT1
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.1.26 0.00006
-
 (6R,9S,13S)-3-benzyl-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT2, 37°C Chlorocebus aethiops
2.3.1.26 0.00009
-
 (6R,9S,13S)-3-benzyl-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT1, 37°C Chlorocebus aethiops
2.3.1.26 0.0001
-
 (6S,9S,13S)-6-methyl-9-(4-methylbenzyl)-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT1, 37°C Chlorocebus aethiops
2.3.1.26 0.0001
-
 (6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1R)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT2, 37°C Chlorocebus aethiops
2.3.1.26 0.00015
-
 (6S,9S,13S)-9-(3-chlorobenzyl)-6-methyl-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT1, 37°C Chlorocebus aethiops
2.3.1.26 0.00025
-
 (6S,9S,13S)-6-methyl-13-[(1S)-1-methylnonyl]-3-[(1S)-1-methylpropyl]-9-(naphthalen-2-ylmethyl)-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT2, 37°C Chlorocebus aethiops
2.3.1.26 0.00027
-
 (6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT2, 37°C Chlorocebus aethiops
2.3.1.26 0.001
-
 (6S,9S,13R)-9-(2-chlorobenzyl)-6-methyl-3-[(1S)-1-methylpropyl]-13-pentyl-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT1, 37°C Chlorocebus aethiops
2.3.1.26 0.004
-
 (6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1R)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT1, 37°C Chlorocebus aethiops
2.3.1.26 0.004
-
 (6S,9S,13S)-6-methyl-9-(4-methylbenzyl)-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT2, 37°C Chlorocebus aethiops
2.3.1.26 0.0065
-
 (6S,9S,13S)-9-(3-chlorobenzyl)-6-methyl-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT2, 37°C Chlorocebus aethiops
2.3.1.26 0.01
-
 (6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT1, 37°C Chlorocebus aethiops
2.3.1.26 0.02
-
 (6S,9S,13S)-6-methyl-13-[(1S)-1-methylnonyl]-3-[(1S)-1-methylpropyl]-9-(naphthalen-2-ylmethyl)-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT1, 37°C Chlorocebus aethiops
2.3.1.26 0.04
-
 (6S,9S,13R)-9-(2-chlorobenzyl)-6-methyl-3-[(1S)-1-methylpropyl]-13-pentyl-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone isoform ACAT2, 37°C Chlorocebus aethiops