alox15

ALOX15-IN-2 is a potent inhibitor of ALOX15 linoleate oxygenase activity, inhibiting the oxidation of linoleic acid (LA) and arachidonic acid (AA), the immediate homologs of ALOX15, with IC50s of 1.55 and 2.79 μM, respectively.

ALOX15-IN-1 (compound 8b) is a selective and potent inhibitor of rabbit and human ALOX15 linoleate oxygenase activity, targeting the direct homologues of ALOX15 linoleic acid (LA) with an IC50 of 0.04 μM and arachidonic acid (AA) with an IC50 of 2.06 μM.

Lipid-derived lipoxins are produced at the site of vascular and mucosal inflammation where they down-regulate polymorphonuclear leukocyte recruitment and function. 15(R)-Lipoxin A4 (15(R)-LXA4) is derived from the aspirin-triggered formation of 15(R)-HETE from arachidonic acid. [1] [2] 15(R)-LXA4 inhibits LTB4-induced chemotaxis, adherence, and transmigration of neutrophils with twice the potency of LXA4 demonstrating activity in the nM range.[2] [3] The anti-inflammatory effects of aspirin may be ascribed in part to the ability of 15(R)-LXA4 to regulate leukocyte function.[4] 15(R)-LXA4 is reported to promote resolution of inflammation in LPS-treated stromal cells derived from intermediate-stage diseased supraspinatus tendons as evidenced by increased expression of the STAT-6 pathway target genes, ALOX15 and CD206.[5]