BI-0115 is a selective small molecule inhibitor of LOX-1 that blocks cellular uptake of oxLDL.

Silychristin, a natural product isolated and purified from the herbs of Silybum marianum (L.) Gaertn., is a plant growth regulator, an anti-hepatotoxic agent, and an inhibitor of horseradish peroxidases and lipoxygenase.

5-Hydroxy-3',4',7-trimethoxyflavone, a natural product isolated and purified fromt Lippia nodiflora L., shows prominent inhibitory activity against soybean lipoxygenase.

ML351 is a novel chemotype and the first reported selective inhibitor of 15-LOX-1 with IC50 value of 200 nM.

ML355 is a selective 12-lipoxygenase inhibitor with an IC50 value of 0.34 µM, with much less potency against 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >100 µM).

2-TEDC is a potent inhibitor of 5-, 12-, and 15-lipoxygenase with IC50s of 0.09, 0.013 and 0.5 μM respectively.

PD 146176 is a specific, non-competitve 15-lipoxygenase (15-LOX) inhibitor with Ki of 197 nM.

Malotilate is hepatotrophic drug which can selectively inhibit the 5-lipoxygenase, whereas both the 12- and the 15-lipoxygenase pathways were stimulated, with antifibrotic and hepatoprotective properties.

Zileuton is a reversible 5-lipoxygenase inhibitor with IC50 value of 0.5 µM in rat basophilic leukemia-1 (RBL-1) cells. It also potently inhibited leukotriene B4 production with an IC50 value of 0.6 µM in purified human peripheral blood polymorphonuclear leukocytes (PMNL).

Phenidone inhibited both the lipoxygenase and Cox pathways

2-(3,4-Dihydroxyphenyl)ethanol is a potent and specific inhibitor of lipoxygenase activities, inhibits platelet 12-LO activity with IC50 of 4.2 mM and PMNL 5-LO activity with IC50 of 13 mM. It's a natural product isolated and purified from the herbs of Canarium album with antioxidant property.

Wedelolactone, a natural compound derived from Chinese herbal medicine Eclipta prostrate L, is an anti-cancer agent for breast and prostate carcinomas in vitro and in vivo targeting multiple cellular proteins including androgen receptors, 5-lipoxygenase and topoisomerase IIα.