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Literature summary for 2.3.3.8 extracted from

  • Koerner, S.K.; Hanai, J.I.; Bai, S.; Jernigan, F.E.; Oki, M.; Komaba, C.; Shuto, E.; Sukhatme, V.P.; Sun, L.
    Design and synthesis of emodin derivatives as novel inhibitors of ATP-citrate lyase (2017), Eur. J. Med. Chem., 126, 920-928 .
    View publication on PubMed
Search for more literature for 2.3.3.8

Inhibitors

Inhibitors Comment Organism Structure
1,3,8-trihydroxy-2-(3-methoxyphenyl)-6-methylanthracene-9,10-dione
-
 Homo sapiens
1,3,8-trihydroxy-2-(4-methoxyphenyl)-6-methylanthracene-9,10-dione
-
 Homo sapiens
1,3,8-trihydroxy-2-iodo-6-methylanthracene-9,10-dione
-
 Homo sapiens
1,3,8-trihydroxy-6-methyl-2-(1-methyl-1H-pyrazol-4-yl)anthracene-9,10-dione
-
 Homo sapiens
1,3,8-trihydroxy-6-methyl-2-(3-methylphenyl)anthracene-9,10-dione
-
 Homo sapiens
1,3,8-trihydroxy-6-methyl-2-(pyridin-3-yl)anthracene-9,10-dione
-
 Homo sapiens
1,3,8-trihydroxy-6-methyl-2-phenylanthracene-9,10-dione
-
 Homo sapiens
1,3,8-trihydroxy-6-methyl-2-[(morpholin-4-yl)methyl]anthracene-9,10-dione
-
 Homo sapiens
1,3,8-trihydroxy-6-methyl-2-[(piperidin-1-yl)methyl]anthracene-9,10-dione
-
 Homo sapiens
1,3,8-trihydroxy-6-methyl-2-[[methyl(phenyl)amino]methyl]anthracene-9,10-dione
-
 Homo sapiens
1,3-dibromo-2,4,5-trihydroxy-7-methylanthracene-9,10-dione
-
 Homo sapiens
1-chloro-2,4,5-trihydroxy-7-methylanthracene-9,10-dione
-
 Homo sapiens
2,4,5-trihydroxy-7-methyl-1,3-di(pyridin-3-yl)anthracene-9,10-dione
-
 Homo sapiens
2-chloro-1,3,8-trihydroxy-6-methylanthracen-9(10H)-one
-
 Homo sapiens
2-chloro-1,3,8-trihydroxy-6-methylanthracene-9,10-dione
-
 Homo sapiens
3-(1,3-benzoxazol-5-yl)-5,7-dihydroxy-9-methyl-3,4-dihydro-2H-anthra[2,3-e][1,3]oxazine-6,11-dione
-
 Homo sapiens
4-chloro-1,3,8-trihydroxy-6-methylanthracen-9(10H)-one
-
 Homo sapiens
5,7-dihydroxy-9-methyl-3-phenyl-3,4-dihydro-2H-anthra[2,3-e][1,3]oxazine-6,11-dione
-
 Homo sapiens
BMS-303141
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P53396
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
ACL
-
 Homo sapiens
ATP citrate lyase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000283
-
 pH 8.0, 30°C Homo sapiens 2-chloro-1,3,8-trihydroxy-6-methylanthracen-9(10H)-one
0.000442
-
 pH 8.0, 30°C Homo sapiens BMS-303141
0.0029
-
 pH 8.0, 30°C Homo sapiens 1,3-dibromo-2,4,5-trihydroxy-7-methylanthracene-9,10-dione
0.0038
-
 pH 8.0, 30°C Homo sapiens 4-chloro-1,3,8-trihydroxy-6-methylanthracen-9(10H)-one
0.0075
-
 pH 8.0, 30°C Homo sapiens 1,3,8-trihydroxy-2-iodo-6-methylanthracene-9,10-dione
0.0096
-
 pH 8.0, 30°C Homo sapiens 1-chloro-2,4,5-trihydroxy-7-methylanthracene-9,10-dione
0.0126
-
 pH 8.0, 30°C Homo sapiens 2-chloro-1,3,8-trihydroxy-6-methylanthracene-9,10-dione
0.0133
-
 pH 8.0, 30°C Homo sapiens 1,3,8-trihydroxy-6-methyl-2-(1-methyl-1H-pyrazol-4-yl)anthracene-9,10-dione
0.0188
-
 pH 8.0, 30°C Homo sapiens 1,3,8-trihydroxy-2-(4-methoxyphenyl)-6-methylanthracene-9,10-dione
0.0211
-
 pH 8.0, 30°C Homo sapiens 1,3,8-trihydroxy-6-methyl-2-(pyridin-3-yl)anthracene-9,10-dione
0.0212
-
 pH 8.0, 30°C Homo sapiens 1,3,8-trihydroxy-2-(3-methoxyphenyl)-6-methylanthracene-9,10-dione
0.0235
-
 pH 8.0, 30°C Homo sapiens 2,4,5-trihydroxy-7-methyl-1,3-di(pyridin-3-yl)anthracene-9,10-dione
0.03
-
 pH 8.0, 30°C Homo sapiens 1,3,8-trihydroxy-6-methyl-2-(3-methylphenyl)anthracene-9,10-dione

Expression

Organism Comment Expression
Homo sapiens the enzyme is overexpressed in cancer cells up

General Information

General Information Comment Organism
malfunction siRNA knockdown of ATP citrate lyase limits cancer cell proliferation and reduces cancer stemness Homo sapiens
metabolism the enzyme plays a critical role in generating cytosolic acetyl CoA, a key building block for de novo fatty acid and cholesterol biosynthesis Homo sapiens