5-LOX-IN-9 is a 5-lipoxygenase and cyclooxygenase inhibitor, with an IC50 of 0.2 pM against guinea pig 5-LOX and an IC50 of 0.7 pM against bovine COX. 5-LOX-IN-9 inhibits 5-lipoxygenase via a redox-mediated mechanism. 5-LOX-IN-9 inhibits cyclooxygenase through hydrogen donor action and hydrophobicity-dependent activity [1].
In Vitro, 5-LOX-IN-9 (Compound 3) acts as a dual inhibitor, potently inhibiting bovine seminal vesicle COX with an IC50 of 7 × 10-7 μM and guinea pig lung 5-LOX with an IC50 of 2 × 10-7 μM[1]. 5-LOX-IN-9 in its cis-b conformation exhibits an MEP map with an extended negative region around its R3 aromatic ring, a feature associated with dual COX/5-LOX inhibitory activity[1]. 5-LOX-IN-9 in its cis-b conformation has dual hydrophobic interaction areas (consistent with dual COX/5-LOX inhibition) and a strong ferric iron cation interaction, which correlates with its potent 5-LOX inhibitory activity[1].
References:
[1]. Ruiz J, et al. QSAR study of dual cyclooxygenase and 5-lipoxygenase inhibitors 2,6-di-tert-butylphenol derivatives. Bioorganic & medicinal chemistry. 2003 Sep 15;11(19):4207-16.
In Vitro, 5-LOX-IN-9 (Compound 3) acts as a dual inhibitor, potently inhibiting bovine seminal vesicle COX with an IC50 of 7 × 10-7 μM and guinea pig lung 5-LOX with an IC50 of 2 × 10-7 μM[1]. 5-LOX-IN-9 in its cis-b conformation exhibits an MEP map with an extended negative region around its R3 aromatic ring, a feature associated with dual COX/5-LOX inhibitory activity[1]. 5-LOX-IN-9 in its cis-b conformation has dual hydrophobic interaction areas (consistent with dual COX/5-LOX inhibition) and a strong ferric iron cation interaction, which correlates with its potent 5-LOX inhibitory activity[1].
References:
[1]. Ruiz J, et al. QSAR study of dual cyclooxygenase and 5-lipoxygenase inhibitors 2,6-di-tert-butylphenol derivatives. Bioorganic & medicinal chemistry. 2003 Sep 15;11(19):4207-16.