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2.3.1.26: sterol O-acyltransferase

This is an abbreviated version!
For detailed information about sterol O-acyltransferase, go to the full flat file.

Word Map on EC 2.3.1.26

Reaction

a long-chain acyl-CoA
+
a sterol
=
CoA
 +
a long-chain 3-hydroxysterol ester

Synonyms

A2, ACAT, ACAT-1, ACAT-2, ACAT1, ACAT2, acyl coenzyme A-cholesterol-O-acyltransferase, acyl coenzyme A: cholesteryl acyltransferase, acyl-CoA cholesterol acyltransferase, acyl-CoA cholesterol O-acyltransferase, acyl-CoA: cholesterol acyltransferase, acyl-CoA:cholesterol acyltransferase, acyl-CoA:cholesterol acyltransferase 1, acyl-CoA:cholesterol acyltransferase 2, acyl-coA:cholesterol o-acyl transferase 2, acyl-coenzyme A: cholesterol acyltransferase, acyl-coenzyme A:cholesterol acyltransferase, acyl-coenzyme A:cholesterol acyltransferase 1, acyl-coenzyme A:cholesterol acyltransferase 2, acyl-coenzyme A:cholesterol acyltransferase-1, acyl-coenzyme A:cholesterol O-acyltransferase, acyl-coenzymeA cholesterol acyltransferase, acyl-coenzymeA:cholesterol acyl-transferase, acylcoenzyme A:cholesterol O-acyltransferase, acyltransferase, cholesterol, AsAT, cholesterol acyltransferase, cholesterol acyltransferase 2, cholesterol ester synthase, cholesterol ester synthetase, cholesteryl ester synthetase, hACAT, hACAT-1, hACAT-2, hACAT1, SOAT, SOAT!, Soat1, Soat2, sterol O-acyltransferase 2, sterol-ester synthase, sterol-ester synthetase, steroyl O-acyltransferase 1, steroyl O-acyltransferase 2

ECTree

     2 Transferases
         2.3 Acyltransferases
             2.3.1 Transferring groups other than aminoacyl groups
                2.3.1.26 sterol O-acyltransferase

Inhibitors

Inhibitors on EC 2.3.1.26 - sterol O-acyltransferase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl (9Z,12E)-octadeca-9,12-dienoate
-
-
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl 3-methylbutanoate
-
-
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl benzoate
-
-
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl butanoate
-
-
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl pent-4-enoate
-
-
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl pentanoate
-
-
(1R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl propanoate
-
-
(1R,3R,7R)-1-[(1S)-1-hydroxypropyl]-3,7-diphenyl-6-[(1S)-1-phenylethyl]-2-oxa-6-azaspiro[3.3]heptan-5-one
-
45% inhibition, reference standard lovastatin, literature data reference IC50 = 0.012 mM, 0.0168 mM when concurrently tested
(1R,3R,7S)-1-[(1S)-1-hydroxypropyl]-3,7-diphenyl-6-[(1S)-1-phenylethyl]-2-oxa-6-azaspiro[3.3]heptan-5-one
(1S)-1-[(1R,3R,5R)-3,5-diphenyl-6-[(1S)-1-phenylethyl]-2-oxa-6-azaspiro[3.3]hept-1-yl]propan-1-ol
-
0.01 mM, 45% inhibition
(24R)-ethylcholest-5-ene-3,7-diol
-
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-2-(2-methoxyphenyl)-4a,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-cyanobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 2-chlorobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 2-cyanobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 2-fluorobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 2-methoxybenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 3-bromobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 3-chlorobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 3-cyanobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 3-fluorobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 3-methoxybenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-bromobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-chlorobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-cyanobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-fluorobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-formylbenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-methoxybenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-2-phenyl-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-nitrobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-2-(2-methylphenyl)-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-cyanobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-2-(2-methylphenyl)-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-fluorobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-2-(3-methylphenyl)-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-cyanobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-2-(3-methylphenyl)-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-fluorobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-2-(4-methylphenyl)-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-cyanobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-2-(4-methylphenyl)-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-fluorobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-12-hydroxy-4a,6a,12b-trimethyl-2-(naphthalen-2-yl)-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-cyanobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-2-(2,4-dimethylphenyl)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-cyanobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-2-(2,6-dimethylphenyl)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-cyanobenzoate
-
(2R,4bR,6S,6aS,12R,12aS,12bS,14aS)-2-(2-fluorophenyl)-12-hydroxy-4a,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-2H,11H-pyrano[3'',4'':5',6']pyrano[3',2':5,6]naphtho[2,1-d][1,3]dioxin-6-yl 4-cyanobenzoate
-
(2S)-2-[(5aR,6R,8R,9aR,10R)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]propane-1,2-diyl diacetate
compound exhibits potent activity against isoform ACAT2 and greater selectivity for ACAT2 than for ACAT1, ratio of IC50 value for ACTA1/ACAT2 is above 1000
(3R,5R,7R,8S)-7-ethyl-8-hydroxy-3,5-diphenyl-2-[(1S)-1-phenylethyl]-6-oxa-2-azaspiro[3.4]octan-1-one
-
0.01 mM, 23% inhibition
(3R,5S,7S,8R)-7-ethyl-8-hydroxy-3,5-diphenyl-2-[(1R)-1-phenylethyl]-6-oxa-2-azaspiro[3.4]octan-1-one
-
27% inhibition, reference standard lovastatin, literature data reference IC50 = 0.012 mM, 0.0168 mM when concurrently tested
(3S,4aR,6S,6aS,12R,12aS,12bS)-12-hydroxy-4,6a,12b-trimethyl-11-oxo-3-(propanoyloxy)-4-[(propanoyloxy)methyl]-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-12-hydroxy-4,6a,12b-trimethyl-3-[(2-methylpropanoyl)oxy]-4-[[(2-methylpropanoyl)oxy]methyl]-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-12-hydroxy-4,6a,12b-trimethyl-11-oxo-4-(propylcarbamoyl)-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-12-hydroxy-4,6a,12b-trimethyl-11-oxo-4-[(propanoyloxy)methyl]-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-12-hydroxy-4,6a,12b-trimethyl-11-oxo-4-[[(3-phenylpropanoyl)oxy]methyl]-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-12-hydroxy-4,6a,12b-trimethyl-4-[[(2-methylpropanoyl)oxy]methyl]-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-12-hydroxy-4-[(2-methoxy-2-oxoethyl)carbamoyl]-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(2-ethoxy-2-oxoethyl)carbamoyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 2,3,4-trifluorobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 2-chlorobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 2-cyanobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 2-fluorobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 2-iodobenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 2-methoxybenzoate
-
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 2-methylbenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-(methylsulfanyl)benzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-bromobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-chlorobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-cyanobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-ethenylbenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-fluoro-4-methoxybenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-fluoro-4-methylbenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-fluoro-4-nitrobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-fluorobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-iodobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-methoxybenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 3-methylbenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-(2lambda~5~-triaza-1,2-dien-2-yl)benzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-(methylsulfanyl)benzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-aminobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-bromo-2-fluorobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-bromo-3-fluorobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-bromobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-chloro-2-iodobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-chlorobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyano-3-fluorobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-ethenylbenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-ethylbenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-fluorobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-hydroxybenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-iodobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-methoxybenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-nitrobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[[(2,4-dimethoxyphenyl)methyl]carbamoyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-6-[(4-cyanobenzoyl)oxy]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-4-carboxylic acid
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(benzoyloxy)-4-[(benzoyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-3-(hexanoyloxy)-4-[(hexanoyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-3-(propanoyloxy)-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-3-[(phenylacetyl)oxy]-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-3-[(2-methylpropanoyl)oxy]-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-cyanobenzoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-6-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-3-yl 2-methylpropanoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-6-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-3-yl 3-phenylpropanoate
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(3S,4aR,6S,6aS,12R,12aS,12bS)-6-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-3-yl propanoate
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(3S,4R,4aS,6S,6aS,12R,12aR,12bR)-12,12b-dihydroxy-4,6a-dimethyl-4-[[(methylsulfonyl)oxy]methyl]-11-oxo-6-(pentanoyloxy)-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-3-yl benzoate
selective for isoform ACAT2
(3S,4R,4aS,6S,6aS,12R,12aR,12bR)-12,12b-dihydroxy-4,6a-dimethyl-4-[[(methylsulfonyl)oxy]methyl]-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromene-3,6-diyl dipentanoate
selective for isoform ACAT2
(3S,4R,4aS,6S,6aS,12R,12aR,12bR)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl 3-methylbutanoate
selective for isoform ACAT2
(3S,4R,4aS,6S,6aS,12R,12aR,12bR)-4-[(acetyloxy)methyl]-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromene-3,6-diyl diacetate
i.e. pyripyropene A,selective for isoform ACAT2
(3S,4R,4aS,6S,6aS,12R,12aR,12bR)-4-[(acetyloxy)methyl]-3-(butanoyloxy)-12,12b-dihydroxy-4,6a-dimethyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl hexanoate
selective for isoform ACAT2
(3S,4S)-3-[(1R,2R)-2-azido-1-hydroxybutyl]-3-bromo-4-phenyl-1-[(1S)-1-phenylethyl]azetidin-2-one
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65% inhibition, reference standard lovastatin, literature data reference IC50 = 0.012 mM, 0.0168 mM when concurrently tested
(3S,4S)-3-[(1S,2S)-2-azido-1-hydroxybutyl]-3-bromo-4-phenyl-1-[(1S)-1-phenylethyl]azetidin-2-one
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60% inhibition, reference standard lovastatin, literature data reference IC50 = 0.012 mM, 0.0168 mM when concurrently tested
(3S,4S,4aR,6S,6aS,12R,12aR,12bR)-3-(acetyloxy)-4-[(acetyloxy)methyl]-4,12,12b-trihydroxy-6a-methyl-11-oxo-9-pyridin-3-yl-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-benzo[f]pyrano[4,3-b]chromen-6-yl (2E)-pent-2-enoate
selective for isoform ACAT2
(3S,5R,7R,8S)-7-ethyl-8-hydroxy-3,5-diphenyl-2-[(1S)-1-phenylethyl]-6-oxa-2-azaspiro[3.4]octan-1-one
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0.01 mM, 27% inhibition
(3S,5S,7S,8R)-7-ethyl-8-hydroxy-3,5-diphenyl-2-[(1R)-1-phenylethyl]-6-oxa-2-azaspiro[3.4]octan-1-one
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23% inhibition, reference standard lovastatin, literature data reference IC50 = 0.012 mM, 0.0168 mM when concurrently tested
(4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(1-methylethyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate
selective for isoform ACAT2
(4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(2-methylphenyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate
selective for isoform ACAT2
(4aR,4bS,6S,6aS,12R,12aR,12bR,14aS)-12,12b-dihydroxy-4a,6a-dimethyl-2-(4-methylphenyl)-11-oxo-9-pyridin-3-yl-4,4a,4b,5,6,6a,12,12a,12b,13,14,14a-dodecahydro-11H-pyrano[4',3':2,3]chromeno[6,5-f][1,3]benzodioxin-6-yl pentanoate
selective for isoform ACAT2
(4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 2,2-difluoro-2H-1,3-benzodioxole-5-carboxylate
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(4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-(1-benzothiophen-2-yl)benzoate
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(4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 4-methylbenzoate
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(4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl 5,8-dihydronaphthalene-2-carboxylate
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(4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl benzoate
-
(4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl naphthalene-1-carboxylate
-
(4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-4-[(acetyloxy)methyl]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-6-yl [1,1'-biphenyl]-4-carboxylate
-
(4S)-3-[(1R,2S)-2-azido-1-hydroxybutyl]-3-[(R)-hydroxy(phenyl)methyl]-4-phenyl-1-[(1S)-1-phenylethyl]azetidin-2-one
-
0.01 mM, 87% inhibition
(4S)-3-[(1R,2S)-2-azido-1-hydroxybutyl]-3-[(S)-hydroxy(phenyl)methyl]-4-phenyl-1-[(1S)-1-phenylethyl]azetidin-2-one
-
87% inhibition, reference standard lovastatin, literature data reference IC50 = 0.012 mM, 0.0168 mM when concurrently tested
(4S)-3-[(1S,2R)-2-azido-1-hydroxybutyl]-3-[(R)-hydroxy(phenyl)methyl]-4-phenyl-1-[(1S)-1-phenylethyl]azetidin-2-one
-
79% inhibition, reference standard lovastatin, literature data reference IC50 = 0.012 mM, 0.0168 mM when concurrently tested
(4S)-3-[(1S,2R)-2-azido-1-hydroxybutyl]-3-[(S)-hydroxy(phenyl)methyl]-4-phenyl-1-[(1S)-1-phenylethyl]azetidin-2-one
-
0.01 mM, 79% inhibition
(4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenoic acid
-
-
(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
(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
(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
(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
(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
(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
(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
(S)-2',3',5'-trimethyl-4'-hydroxy-alpha-dodecylthio-alpha-phenylacetanilide
-
i.e. F12511, may have direct antiatherosclerotic effects on the cells of the vascular wall
(S)-7-dimethylamino-N-(4-hydroxy-2,3,5-trimethylphenyl)-2-isobutyryl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
shows about 16fold stronger anti-foam cell formation activity, 3fold stronger hepatic ACAT inhibitory activity, similar anti-low density lipoprotein (LDL) oxidative activity and 2fold more potent protective activity against macrophage cell death by oxidative stress in comparison with Pactimibe
(S)-N-(2,6-diisopropylphenyl)-2-octanoyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
ratio IC50 of pactimibe/IC50 of test compound: 2.2
(S)-N-(4-amino-2,6-diisopropylphenyl)-2-octanoyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide hydrochloride
-
ratio IC50 of pactimibe/IC50 of test compound: 0.96
(S)-N-(4-hydroxy-2,3,5-trimethylphenyl)-2-octanoyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
-
ratio IC50 of pactimibe/IC50 of test compound: 10
(Z)-17(20)-dehydrocholesterol
-
inhibits esterification of endogenous cholesterol
1-(2,6-diisopropyl-phenyl)-3-[4-(4'-nitrophenylthio)phenyl] urea
-
VULM 1457
1-(3,6-dimethylpyrazin-2-yl)-4-(5-phenylpyridazin-3-yl)-1,4-diazepane
-
0.1 mg/ml, 62% inhibition
1-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl]-3-{4-[(ethylamino)methyl]-2,6-bis(1-methylethyl)phenyl}urea
-
IC50: 680 nM
1-[2,4-bis(1-methylethyl)pyridin-3-yl]-3-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl]urea
-
IC50: 5.4 nM
1-[3-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-4-[3-(3-hydroxypropoxy)phenyl]-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea
-
IC50: 43 nM
1-[4-(aminomethyl)-2,6-bis(1-methylethyl)phenyl]-3-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl]urea
-
IC50: 382 nM
1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-(1-butyl-4-{3-[3-(ethylamino)propoxy]phenyl}-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl)urea
-
IC50: 452 nM
1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-2-oxo-4-[3-(3-piperidin-1-ylpropoxy)phenyl]-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea
-
IC50: 540 nM
1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-2-oxo-4-[3-(3-pyrrolidin-1-ylpropoxy)phenyl]-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea
-
IC50: 427 nM
1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-4-[3-(3-hydroxypropoxy)phenyl]-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea
-
i.e. SMP-797, possessing a potent ACAT inhibitory activity and significantly enhanced aqueous solubility under acidic conditions. The compound is a promising agent for oral treatment of hypercholesterolemia.IC50: 21 nM
1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-4-[3-(4-hydroxybutoxy)phenyl]-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea
-
IC50: 61 nM
1-[4-amino-2,6-di(propan-2-yl)phenyl]-3-({1-[2-(3-hydroxypropoxy)phenyl]-4-(3-methoxyphenyl)piperidin-4-yl}methyl)urea
-
-
1-[4-amino-2,6-di(propan-2-yl)phenyl]-3-{[1-(2-butoxyphenyl)-4-(3-methoxyphenyl)piperidin-4-yl]methyl}urea
17alpha-hydroxyprogesterone
-
-
2,3,6,8-tetramethoxy-5-(piperidin-1-ylsulfonyl)-1,4-dihydro-9H-xanthen-9-one
-
10 microgram/ml, 10.53% inhibition
2,3,6,8-tetramethoxy-5-[(4-phenyl-3,6-dihydropyridin-1(2H)-yl)sulfonyl]-1,4-dihydro-9H-xanthen-9-one
-
10 microgram/ml, 51.34% inhibition
2,3,6,8-tetramethoxy-5-{[4-(3-methylphenyl)piperazin-1-yl]sulfonyl}-1,4-dihydro-9H-xanthen-9-one
-
10 microgram/ml, 64.8% inhibition
2,3,6,8-tetramethoxy-5-{[4-(4-methoxyphenyl)piperazin-1-yl]sulfonyl}-1,4-dihydro-9H-xanthen-9-one
-
10 microgram/ml, 36.92% inhibition
2,3,6,8-tetramethoxy-5-{[4-(pyridin-2-yl)piperazin-1-yl]sulfonyl}-1,4-dihydro-9H-xanthen-9-one
-
10 microgram/ml, 43.56% inhibition
2,3,6,8-tetramethoxy-9-oxo-N-(2-phenylpropyl)-4,9-dihydro-1H-xanthene-5-sulfonamide
-
10 microgram/ml, 10.78% inhibition
2,3,6,8-tetramethoxy-N-(naphthalen-2-ylmethyl)-9-oxo-4,9-dihydro-1H-xanthene-5-sulfonamide
-
10 microgram/ml, 25% inhibition
2-[(2E,6Z,8E,10E)-dodeca-2,6,8,10-tetraenoylamino]-1,1-dimethylethyl acetate
IC50: 0.0281 mM; IC50: 0.0875 mM
2-[(5aR,6R,8R,9aR,10R)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
-
-
2-[(5aR,6R,8R,9aR,10S)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
-
-
2-[(5aS,6S,8S,9aS)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
-
-
2-[(5aS,6S,8S,9aS,10R)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
-
-
2-[(5aS,6S,8S,9aS,10S)-6-(acetyloxy)-10-hydroxy-5a-methyl-1-oxo-3-(pyridin-3-yl)-6,7,8,9,9a,10-hexahydro-1H,5aH-pyrano[4,3-b][1]benzopyran-8-yl]-2-methylpropane-1,3-diyl diacetate
-
-
2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide
-
K-604
20-Methylcholesterol
-
inhibits esterification of endogenous cholesterol
20alpha-hydroxypregn-4-en-3-one
-
-
2alpha,3beta,23-trihydroxyolean-12-en-28-oic acid
-
arjunolic acid, at 0.1 mg/ml, 60.8% inhibition of isoform ACAT1, 5.3% inhibition of isoform ACAT2
2alpha,3beta-dihydroxyolean-12-en-28-oic acid
-
maslinic acid, at 0.1 mg/ml, 46.2% inhibition of isoform ACAT1, 17.3% inhibition of isoform ACAT2
2alpha,3beta-dihydroxyurs-12-en-28-oic acid
-
corosolic acid, at 0.1 mg/ml, 46.7% inhibition of isoform ACAT1, 3% inhibition of isoform ACAT2
3-(2,4-difluorophenyl)-1-heptyl-1-[5-[(5-phenylpyridazin-3-yl)amino]pentyl]urea
-
0.05 mg/ml, 46% inhibition
3-(2,4-difluorophenyl)-1-heptyl-1-[5-[(5-phenylpyridazin-3-yl)sulfanyl]pentyl]urea
-
0.05 mg/ml, 75% inhibition
3-(2,4-difluorophenyl)-1-heptyl-1-[5-[(5-phenylpyridazin-3-yl)sulfinyl]pentyl]urea
-
0.05 mg/ml, 62% inhibition
3-(2,4-difluorophenyl)-1-heptyl-1-[5-[(5-phenylpyridazin-3-yl)sulfonyl]pentyl]urea
-
0.05 mg/ml, 67% inhibition
3-(2,4-difluorophenyl)-1-heptyl-1-[5-[(6-phenylpyridazin-3-yl)amino]pentyl]urea
-
0.05 mg/ml, 89% inhibition
3-(2,4-difluorophenyl)-1-heptyl-1-[5-[(6-phenylpyridazin-3-yl)sulfinyl]pentyl]urea
-
0.05 mg/ml, 55% inhibition
3-(2,4-difluorophenyl)-1-heptyl-1-[5-[(6-phenylpyridazin-3-yl)sulfonyl]pentyl]urea
-
0.05 mg/ml, 43% inhibition
3-(2,4-difluorophenyl)-1-octyl-1-[5-[(6-phenylpyridazin-3-yl)sulfanyl]pentyl]urea
-
0.05 mg/ml, 44% inhibition
3-(2,4-difluorophenyl)-1-[5-[(5,6-diphenylpyridazin-3-yl)amino]pentyl]-1-heptylurea
-
0.05 mg/ml, 87% inhibition
3-(2,4-difluorophenyl)-1-[5-[(5,6-diphenylpyridazin-3-yl)sulfanyl]pentyl]-1-heptylurea
-
0.05 mg/ml, 75% inhibition
3-(2,4-difluorophenyl)-1-[5-[(5,6-diphenylpyridazin-3-yl)sulfinyl]pentyl]-1-heptylurea
-
0.05 mg/ml, 65% inhibition
3-(2,4-difluorophenyl)-1-[5-[(5,6-diphenylpyridazin-3-yl)sulfonyl]pentyl]-1-heptylurea
-
0.05 mg/ml, 70% inhibition
3-[4-(3,6-dimethylpyrazin-2-yl)piperazin-1-yl]-5-phenylpyridazine
-
0.1 mg/ml, 57% inhibition
3beta,23-dihydroxyurs-12-en-28-oic acid
-
23-hydroxyursolic acid, at 0.1 mg/ml, 41.5% inhibition of isoform ACAT1, 22.2% inhibition of isoform ACAT2
3beta-hydroxylup-20(29)-en-28-oic acid
-
-
3beta-hydroxyolean-12-en-28-oic acid
-
oleanoic acid, at 0.1 mg/ml, 22.6% inhibition of isoform ACAT1, 10.2% inhibition of isoform ACAT2
3beta-hydroxyurs-12-en-28-al
-
ursolic aldehyde, at 0.1 mg/ml, 21.8% inhibition of isoform ACAT1, 13% inhibition of isoform ACAT2
3beta-hydroxyurs-12-en-28-oic acid
-
ursolic acid, at 0.1 mg/ml, 23.1% inhibition of isoform ACAT1, 16.7% inhibition of isoform ACAT2
5,5'-dibutoxy-2,2'-bifuran
-
-
5,5'-dithiobis-(2-nitrobenzoate)
-
50% inhibition of ACAT1 at 0.01 mM
5-(1-butoxy-2-{4-[(2S,3R,4S,5R)-5-(3,4-dimethoxyphenyl)-3,4-dimethyltetrahydrofuran-2-yl]-2-methoxyphenoxy}propyl)-1,3-benzodioxole
0.125 mM, 28% inhibition; IC50: 0.017 mM
5-(2-{4-[(2S,3R,4S,5R)-5-(3,4-dimethoxyphenyl)-3,4-dimethyltetrahydrofuran-2-yl]-2-methoxyphenoxy}-1-ethoxypropyl)-1,3-benzodioxole
0.125 mM, 29% inhibition; IC50: 0.031 mM
5-(2-{4-[(2S,3R,4S,5R)-5-(3,4-dimethoxyphenyl)-3,4-dimethyltetrahydrofuran-2-yl]-2-methoxyphenoxy}-1-methoxypropyl)-1,3-benzodioxole
0.125 mM, 45% inhibition; IC50: 0.035 mM
5-(2-{4-[(2S,3R,4S,5R)-5-(3,4-dimethoxyphenyl)-3,4-dimethyltetrahydrofuran-2-yl]-2-methoxyphenoxy}-1-propoxypropyl)-1,3-benzodioxole
0.125 mM, 33% inhibition; IC50: 0.014 mM
5-[(4-aminopiperazin-1-yl)sulfonyl]-2,3,6,8-tetramethoxy-1,4-dihydro-9H-xanthen-9-one
-
10 microgram/ml, 14.5% inhibition
5-[2-{4-[(2S,3R,4S,5R)-5-(3,4-dimethoxyphenyl)-3,4-dimethyltetrahydrofuran-2-yl]-2-methoxyphenoxy}-1-(heptyloxy)propyl]-1,3-benzodioxole
0.125 mM, 26% inhibition; IC50: 0.05 mM
5-[2-{4-[(2S,3R,4S,5R)-5-(3,4-dimethoxyphenyl)-3,4-dimethyltetrahydrofuran-2-yl]-2-methoxyphenoxy}-1-(hexyloxy)propyl]-1,3-benzodioxole
0.125 mM, 33% inhibition; IC50: 0.034 mM
5-[2-{4-[(2S,3R,4S,5R)-5-(3,4-dimethoxyphenyl)-3,4-dimethyltetrahydrofuran-2-yl]-2-methoxyphenoxy}-1-(nonyloxy)propyl]-1,3-benzodioxole
0.125 mM, 10% inhibition; 0.125 mM, 25% inhibition
5-[2-{4-[(2S,3R,4S,5R)-5-(3,4-dimethoxyphenyl)-3,4-dimethyltetrahydrofuran-2-yl]-2-methoxyphenoxy}-1-(octyloxy)propyl]-1,3-benzodioxole
0.125 mM: 19% inhibition; 0.125 mM: 44% inhibition
5-[2-{4-[(2S,3R,4S,5R)-5-(3,4-dimethoxyphenyl)-3,4-dimethyltetrahydrofuran-2-yl]-2-methoxyphenoxy}-1-(pentyloxy)propyl]-1,3-benzodioxole
0.125 mM, 33% inhibition; IC50: 0.02 mM
5-{[(2R,6S)-2,6-dimethylmorpholin-4-yl]sulfonyl}-2,3,6,8-tetramethoxy-1,4-dihydro-9H-xanthen-9-one
-
10 microgram/ml, 8.84% inhibition
5-{[3-(dimethylamino)pyrrolidin-1-yl]sulfonyl}-2,3,6,8-tetramethoxy-1,4-dihydro-9H-xanthen-9-one
-
10 microgram/ml, 20.96% inhibition
5alpha,8alpha-epidioxy-24(R)-methylcholesta-6,22-diene-3beta-ol
-
-
5alpha-Cholest-8(14)-en-3beta-ol-15-one
-
inhibits the esterification of cholesterol
5alpha-dihydroprogesterone
9-(benzo[d]oxazol-2-ylthio)-N-(2,6-diisopropylphenyl)-nonanamide
inhibitor obtained by combination of weak inhibitors N-(2,6-diisopropylphenyl)and 2-(methylthio)benzo[d]oxazole. At doses of 1 and 3 mg/kg, compound significantly decreases the lipid-accumulation areas in the aortic arch to 74 and 69%, respectively without reducing the plasma total cholesterol level in high fat- and cholesterol-fed F1B hamsters
Acetic anhydride
-
2 distinct tissue types with difference in reactivity, the inhibitor appears to modify a histidine residue
acetone
acetylshikonin
-
-
acyl-CoA binding protein
-
3fold decrease in activity
-
acyl-CoA binding protein/oleoyl-CoA complexes
-
strongly inhibit
-
ADP
-
inactivates
AM-251
-
selective antagonist of cannobinoid receptor CB1. Additionally, reatment of cells reduces cholesteryl ester synthesis in unstimulated and acetylated low densitixy lipoprotein-stimulated Raw 264.7 macrophages, CB2 +/+ and CB2-/- peritoneal macrophages, as well as in vitro, in mouse liver microsomes. Consistent with inhibition of ACAT, the development of foam cell characteristics in macrophages by treatment with acetylated low density lipoprotein is reduced
androstenedione
-
-
androsterone
-
inhibits esterification of endogenous cholesterol
ATP
-
inactivates
aurasperone A
isolation from the culture broth of Aspergillus species; isolation from the culture broth of Aspergillus species
aurasperone D
isolation from the culture broth of Aspergillus species; isolation from the culture broth of Aspergillus species
avasimibe
averufanin
isolation from the culture broth of Aspergillus species; isolation from the culture broth of Aspergillus species
beauvericin
beauveriolide I
beauveriolide III
beta-hydroxyisovalerylshikonin
-
-
beta-sanshool
extracted from Zanthoxylum piperitum DC; IC50: 0.012 mM; IC50: 0.039 mM
beta-sanshool acetate
semi-synthetic compound
betulin
IC50: 0.083 mM, hACAT-1
biseokeaniamide A
-
biseokeaniamide B
exhibits moderate cytotoxicity against HeLa cancer cells; exhibits moderate cytotoxicity against HeLa cancer cells
biseokeaniamide C
-
bovine serum albumin
-
butanol
celludinone A1
celludinone A2
celludinone B
cholestyramine
CI-1011
-
-
CI-976
CI976
CL-283,546
CP113818
-
recombinant enzyme, 80-90% inhibition at 0.0002 mM
Cycloartenol
-
inhibits esterification of exogenous cholesterol
dehydroisoandrosterone
-
-
dehydropipernonaline
dehydroretrofractamide
deoxycorticosterone
Detergents
diazepam
-
competes with oleoyl-CoA for its binding to microsomal membranes
diethyl dicarbonate
-
2 distinct tissue types with difference in reactivity, DEP-sensitive subtype typified by aortic ACTAT, DEP-resistant subtype typified by liver ACAT, irreversible inhibition, the inhibitor appear to modify a histidine residue
DuP 128
ergosterol
-
inhibits esterification of exogenous cholesterol
esculeogenin A
esculeoside A
-
-
estradiol-17beta
-
-
ethanol
ethyl 1-[(2,3,6,8-tetramethoxy-9-oxo-4,9-dihydro-1H-xanthen-5-yl)sulfonyl]piperidine-3-carboxylate
-
10 microgram/ml, 7.99% inhibition
ethyl N-methyl-N-[(2,3,6,8-tetramethoxy-9-oxo-4,9-dihydro-1H-xanthen-5-yl)sulfonyl]glycinate
-
10 microgram/ml, 16.79% inhibition
FD-549
flavasperone
isolation from the culture broth of Aspergillus species, selective for isoform ACAT2
gamma-sanshool
extracted from Zanthoxylum piperitum DC; IC50: 0.0797 mM; IC50: 0.0826 mM
GERI-BP001M
-
0.1 mg/ml, 82% inhibition
GERIBP001M
-
0.05 mM, 83% inhibition
glabrol
glisoprenin A
HWY-289
-
50% inhibition at 0.0132 mM
hydroxy-beta-sanshool
low inhibition; low inhibition
Inhibitor from rabbit liver
-
fatty acid ester, mostly stearate, of a pentacyclic triterpene acid, irreversible inhibition, which is prevented by incubation with bovine serum albumin, half-maximal inhibition occurs at an inhibitor concentration of 0.02 mM
-
isobutyrylshikonin
-
-
K-604
selective for isoform ACAT-1, use to measure the individual enzymatic activities of isoforms ACAT-1 and ACAT-2; selective for isoform ACAT-1, use to measure the individual enzymatic activities of isoforms ACAT-1 and ACAT-2
K97-0239A
K97-0239B
lanosterol
lidocaine
lupeol
IC50: 0.048 mM, hACAT-1
manassantin B
inhibition of both isoforms ACAT-1 and ACAT-2; inhibition of both isoforms ACAT-1 and ACAT-2
methyl (3S,4aR,6S,6aS,12R,12aS,12bS)-3-(acetyloxy)-6-[(4-cyanobenzoyl)oxy]-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-4-carboxylate
-
methyl N-[(2,3,6,8-tetramethoxy-9-oxo-4,9-dihydro-1H-xanthen-5-yl)sulfonyl]glycinate
-
10 microgram/ml, 5.13% inhibition
MgATP2-
miconazole
-
50% inhibition at 0.0224 mM
N'-(3,6-dimethylpyrazin-2-yl)-N,N-diheptylbutane-1,4-diamine
-
0.1 mg/ml, 55% inhibition
N'-(3,6-dimethylpyrazin-2-yl)-N,N-diheptylpentane-1,5-diamine
-
0.1 mg/ml, 58% inhibition
N'-(3,6-dimethylpyrazin-2-yl)-N,N-diheptylpropane-1,3-diamine
-
0.1 mg/ml, 52% inhibition
N'-(3,6-dimethylpyrazin-2-yl)-N-heptyl-N-(5-phenylpyridazin-3-yl)butane-1,4-diamine
-
0.1 mg/ml, 87% inhibition
N'-(3,6-dimethylpyrazin-2-yl)-N-heptyl-N-(5-phenylpyridazin-3-yl)heptane-1,7-diamine
-
0.1 mg/ml, 58% inhibition
N'-(3,6-dimethylpyrazin-2-yl)-N-heptyl-N-(5-phenylpyridazin-3-yl)hexane-1,6-diamine
-
0.1 mg/ml, 79% inhibition; 0.1 mg/ml, 95% inhibition
N'-(3,6-dimethylpyrazin-2-yl)-N-heptyl-N-(5-phenylpyridazin-3-yl)octane-1,8-diamine
-
0.1 mg/ml, 76% inhibition
N'-(3,6-dimethylpyrazin-2-yl)-N-heptyl-N-(5-phenylpyridazin-3-yl)pentane-1,5-diamine
-
0.1 mg/ml, 79% inhibition
N'-(3,6-dimethylpyrazin-2-yl)-N-heptyl-N-(5-phenylpyridazin-3-yl)propane-1,3-diamine
-
0.1 mg/ml, 70% inhibition
N,N-diethyl-1-[(2,3,6,8-tetramethoxy-9-oxo-4,9-dihydro-1H-xanthen-5-yl)sulfonyl]piperidine-3-carboxamide
-
10 microgram/ml, 12.59% inhibition
N-(3,6-dimethylpyrazin-2-yl)-N'-(5-phenylpyridazin-3-yl)hexane-1,6-diamine
-
0.1 mg/ml, 89% inhibition
N-(3-chlorobenzyl)-2,3,6,8-tetramethoxy-9-oxo-4,9-dihydro-1H-xanthene-5-sulfonamide
-
10 microgram/ml, 15.76% inhibition
N-(4,6-dimethyl-1-pentylindolin-7-yl)-2,2-dimethylpropanamide
-
KY-455, an anti-oxidative ACAT inhibitor
N-(4-amino-2, 6-diisopropylphenyl)-N'-[1-butyl-4-[3-(3-hydroxypropoxy) phenyl]-2-oxo-1,2-dihydro-1,8-naphthyridin-3-yl] urea hydrochloride monohydrate
-
SMP-797
N-(4-fluorobenzyl)-2,3,6,8-tetramethoxy-9-oxo-4,9-dihydro-1H-xanthene-5-sulfonamide
-
10 microgram/ml, 10.24% inhibition
N-(5,6-diphenylpyridazin-3-yl)-N'-(5-phenylpyridazin-3-yl)hexane-1,6-diamine
-
0.1 mg/ml, 88% inhibition
N-(5-phenylpyridazin-3-yl)hexane-1,6-diamine
-
0.1 mg/ml, 72% inhibition
N-(6-chloropyridazin-3-yl)-N'-(5-phenylpyridazin-3-yl)hexane-1,6-diamine
-
0.1 mg/ml, 83% inhibition
N-(6-methoxypyridazin-3-yl)-N'-(5-phenylpyridazin-3-yl)hexane-1,6-diamine
-
0.1 mg/ml, 83% inhibition
N-(benzyloxy)-2,3,6,8-tetramethoxy-9-oxo-4,9-dihydro-1H-xanthene-5-sulfonamide
-
10 microgram/ml, 16.76% inhibition
N-ethylmaleimide
-
50% inhibition of ACAT1 at 0.5 mM
N-[2-(3,4-dimethylphenyl)ethyl]-2,3,6,8-tetramethoxy-9-oxo-4,9-dihydro-1H-xanthene-5-sulfonamide
-
10 microgram/ml, 11.86% inhibition
N-[3-(3,4-dimethoxyphenyl)propyl]-2,3,6,8-tetramethoxy-N-methyl-9-oxo-4,9-dihydro-1H-xanthene-5-sulfonamide
-
10 microgram/ml, 30.06% inhibition
naphthalene-1-carboxylic acid [3-(6-bromo-imidazo[1,2-a]pyridin-2-yl)-phenyl]-amide
-
48% inhibition at 0.025 mg/ml
naphthalene-2-carboxylic acid (3-[6-(2,4-difluoro-phenyl)-imidazo[1,2-a]pyridin-2-yl]-phenyl)-amide
-
23.6% inhibition at 0.025 mg/ml
naphthalene-2-carboxylic acid [3-(6-bromo-imidazo[1,2-a]pyridin-2-yl)-phenyl]-amide
-
56% inhibition at 0.025 mg/ml
naphthalene-2-carboxylic acid [3-(6-naphtalen-2-yl-imidazo-[1,2-a]pyridin-2-yl)-phenyl]-amide
-
7.1% inhibition at 0.025 mg/ml
nevanimibe
-
octimibate
-
inhibits
octyl beta-D-glucopyranoside
presence of octylglucoside dissociates ACAT1 to form a dimeric species
oleic acid anilide
-
-
oleoyl-CoA
-
inhibits at high concentrations, the inhibition is prevented by serum albumin
organic solvents
-
p-chloromercuribenzene sulfonic acid
-
50% inhibition of ACAT1 at 0.01 mM, Cys467 is one of the major targets for inhibition
p-mercuribenzoate
-
100% inhibition of liver and aortic enzyme at 1 mM
pactimibe sulfate
PD138412
-
recombinant enzyme, 80-90% inhibition at 0.003 mM
-
pellitorin
phenochalasin A
Phenylglyoxal
-
concentration-dependent inhibition of liver enzyme with 65% inhibition at 5 mM
phosphatidylinositol
-
-
phosphatidylserine
piperchabamide D
pipercide
Polyoxyethylated cholesterol
-
-
-
Pregn-5-en-3beta-ol
-
inhibits esterification of endogenous cholesterol
pregnenolone
progesterone
purpactin A
purpactin B
purpactin C
pyripyropene A
pyripyropene B
pyripyropene C
pyripyropene D
retrofractamide A
saucemeol B
0.125 mM, 57% inhibition; IC50: 0.043 mM
SC-31769
sespendole
shikonin
-
-
sitosterol
-
inhibits esterification of exogenous cholesterol
SM-32504
-
IC50: 11 nM
sphingomyelin
-
-
spylidone
SR144528
-
selective antagonist of cannobinoid receptor CB1. Additionally, reatment of cells reduces cholesteryl ester synthesis in unstimulated and acetylated low densitixy lipoprotein-stimulated Raw 264.7 macrophages, CB2 +/+ and CB2-/- peritoneal macrophages, as well as in vitro, in mouse liver microsomes. Consistent with inhibition of ACAT, the development of foam cell characteristics in macrophages by treatment with acetylated low density lipoprotein is reduced
stanolone
-
inhibits esterification of endogenous cholesterol
sterigmatocystin
isolation from the culture broth of Aspergillus species, selective for isoform ACAT2
stigmasterol
-
inhibits esterification of exogenous cholesterol
terpendole C
testosterone
Tetracaine
Tetranitromethane
-
100% inhibition of liver and aortic enzyme at 1 mM
Triton WR1339
-
90% inhibition at 0.3% wt./vol.
Triton X-100
presence of Triton X-100 dissociates ACAT1 to form a dimeric species
VULM 1457
-
-
YM-750
-
-
[(3S,4aR,6S,6aS,12R,12aS,12bS)-3,6-bis(acetyloxy)-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-4-yl]methyl 2-methylpropanoate
-
[(3S,4aR,6S,6aS,12R,12aS,12bS)-3,6-bis(acetyloxy)-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-4-yl]methyl 3-phenylpropanoate
-
[(3S,4aR,6S,6aS,12R,12aS,12bS)-3,6-bis(acetyloxy)-12-hydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-2H,11H-naphtho[2,1-b]pyrano[3,4-e]pyran-4-yl]methyl propanoate
-
[4-(2-(3-[(naphthalene-2-carbonyl)-amino]-phenyl)-imidazo[1,2-a]pyridin-6-yl)-phenoxy]-acetic acid
-
15% inhibition at 0.025 mg/ml
[4-(2-(3-[(naphthalene-2-carbonyl)-amino]-phenyl)-imidazo[1,2-a]pyridin-6-yl)-phenoxy]-acetic acid ethyl ester
-
8.7% inhibition at 0.025 mg/ml
[7-(2,2-dimethylpropanamido)-4,6-dimethyl-1-octylindolin-5-yl]acetic acid hemisulfate
-
pactimibe sulfate
additional information
-