Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Cho, Y.S.; Kim, C.H.; Surh, J.H.; Kang, N.S.; Yoo, S.E.; Cheon, H.G.
    Identification of 4-[4-(4-fluoro-phenyl)-thiazol-2-ylamino]-2,6-dimethyl-phenol (KR-33749) as an inhibitor of 5-lipoxygenase with potent antiinflammatory activity (2010), Pharmacology, 86, 65-72.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.13.11.34 expressed in Sf-21 insect cells Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.13.11.34 4-[4-(4-fluoro-phenyl)-thiazol-2-ylamino]-2,6-dimethylphenol KR-33749, the compound exhibits a more than 1000fold selectivity for 5-LO against 12-LO and 15-LO Rattus norvegicus
1.13.11.34 zileuton
-
 Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.13.11.34 (6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate Rattus norvegicus
-
 leukotriene A4 + H2O
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.13.11.34 Rattus norvegicus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.13.11.34 RBL-1 cell
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.13.11.34 (6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate
-
 Rattus norvegicus leukotriene A4 + H2O
-
 ?
1.13.11.34 arachidonate + O2
-
 Rattus norvegicus (6E,8Z,11Z,14Z)-(5S)-hydroperoxyicosa-6,8,11,14-tetraenoate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.13.11.34 5-lipoxygenase
-
 Rattus norvegicus
1.13.11.34 5-LO
-
 Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.13.11.34 0.00007
-
 in 50 mM Tris-HCl buffer (pH 7.4) containing 0.4 mM CaCl2+ , 0.024 mg/ml alpha-phosphatidylcholine and 0.02 mM ATP, at 22°C Rattus norvegicus 4-[4-(4-fluoro-phenyl)-thiazol-2-ylamino]-2,6-dimethylphenol
1.13.11.34 0.00028
-
 in 50 mM Tris-HCl buffer (pH 7.4) containing 0.4 mM CaCl2+ , 0.024 mg/ml alpha-phosphatidylcholine and 0.02 mM ATP, at 22°C Rattus norvegicus zileuton