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Literature summary for 5.4.99.7 extracted from

  • Ceruti, M.; Rocco, F.; Viola, F.; Balliano, G.; Milla, P.; Arpicco, S.; Cattel, L.
    9-Methylidine-2,3-oxidosqualene derivatives as stereospecific mechanism-based inhibitors of liver and yeast oxidosqualene cyclase (1998), J. Med. Chem., 41, 540-554.
    View publication on PubMed
Search for more literature for 5.4.99.7

Inhibitors

Inhibitors Comment Organism Structure
(18E)-29-Methylidene-2,3-oxidohexanorsqualene IC50: 0.0015 mM, irreversible; potent, irreversible Saccharomyces cerevisiae
(18E)-29-Methylidene-2,3-oxidohexanorsqualene IC50: 0.0035 mM, irreversible; potent, irreversible Sus scrofa
(18Z)-29-Methylidene-2,3-oxidohexanorsqualene IC50: 0.015 mM; potent, irreversible Saccharomyces cerevisiae
(18Z)-29-Methylidene-2,3-oxidohexanorsqualene IC50: 0.02 mM; potent, irreversible Sus scrofa
(5E,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-vinyl-2,5,9,13,17-tricosapentaene IC50: 0.018 mM Saccharomyces cerevisiae
(5E,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-vinyl-2,5,9,13,17-tricosapentaene IC50: 0.032 mM Sus scrofa
(6E,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene IC50: 0.005 mM Saccharomyces cerevisiae
(6E,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene IC50: 0.004 mM Sus scrofa
(6Z,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene IC50: 0.001 mM Saccharomyces cerevisiae
(6Z,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene IC50: 0.0004 mM Sus scrofa
18,19-dihydro-29-methylidene-2,3-oxidosqualene IC50: 0.1 mM Sus scrofa
18-heptanor-2,3-oxidosqualene IC50: 0.07 mM Saccharomyces cerevisiae
18-heptanor-2,3-oxidosqualene IC50: 0.015 mM Sus scrofa

Organism

Organism UniProt Comment Textmining
Saccharomyces cerevisiae
-
-
-
Sus scrofa
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Sus scrofa
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(S)-squalene-2,3-epoxide
-
 Sus scrofa Lanosterol
-
 ?
(S)-squalene-2,3-epoxide
-
 Saccharomyces cerevisiae Lanosterol
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0004
-
 IC50: 0.0004 mM Sus scrofa (6Z,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene
0.001
-
 IC50: 0.001 mM Saccharomyces cerevisiae (6Z,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene
0.0015
-
 IC50: 0.0015 mM, irreversible Saccharomyces cerevisiae (18E)-29-Methylidene-2,3-oxidohexanorsqualene
0.0035
-
 IC50: 0.0035 mM, irreversible Sus scrofa (18E)-29-Methylidene-2,3-oxidohexanorsqualene
0.004
-
 IC50: 0.004 mM Sus scrofa (6E,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene
0.005
-
 IC50: 0.005 mM Saccharomyces cerevisiae (6E,10E,14E,18E)-22,23-epoxy-2,10,15,19,23-pentamethyl-6-vinyl-2,6,10,14,18-tetracosapentaene
0.015
-
 IC50: 0.015 mM Saccharomyces cerevisiae (18Z)-29-Methylidene-2,3-oxidohexanorsqualene
0.015
-
 IC50: 0.015 mM Sus scrofa 18-heptanor-2,3-oxidosqualene
0.018
-
 IC50: 0.018 mM Saccharomyces cerevisiae (5E,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-vinyl-2,5,9,13,17-tricosapentaene
0.02
-
 IC50: 0.02 mM Sus scrofa (18Z)-29-Methylidene-2,3-oxidohexanorsqualene
0.032
-
 IC50: 0.032 mM Sus scrofa (5E,9E,13E,17E)-21,22-epoxy-2,9,14,18,22-pentamethyl-5-vinyl-2,5,9,13,17-tricosapentaene
0.07
-
 IC50: 0.07 mM Saccharomyces cerevisiae 18-heptanor-2,3-oxidosqualene
0.1
-
 IC50: 0.1 mM Sus scrofa 18,19-dihydro-29-methylidene-2,3-oxidosqualene