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Literature summary for 1.13.11.34 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
Search for more literature for 1.13.11.34

Cloned(Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
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
zileuton
-
 Rattus norvegicus

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
RBL-1 cell
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
5-lipoxygenase
-
 Rattus norvegicus
5-LO
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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