Lipoxygenase Inhibitor

BLX-3887 is a selective 15-lipoxygenase type 1 (15-LO-1) inhibitor with an IC₅₀ of 32 nM. BLX-3887 can be utilized in research related to the 15-LO pathways.

Lonapalene (RS4317) is a topically effective 5-lipoxygenase (5-LO) inhibitor.

Setileuton (MK-0633) is an inhibitor for 5-lipoxygenase, that inhibits the oxidation of arachidonic acid by recombinant human 5-LO, and the production of LTB4 in calcium ionophore-stimulated human whole blood, with IC₅₀ of 3.9 and 52 nM, respectively.

KKII5 is a potent Lipoxygenase (LOX-1) inhibitor with an IC₅₀ of 19 μM. KKII5 inhibits lipid peroxidation.

3-O-Acetyl-11-hydroxy-beta-boswellic acid is a potent 5-lipoxygenase (5-LO) inhibitor.

NCTT-956 is a very effective platelet 12-lipoxygenase (12-LOX) activity-specific inhibitor.

Lobaric acid is a depsipeptide metabolite isolated from Stereocaulon lichen with antioxidant, antiproliferative, antiviral and enzyme inhibitory activities. Lobaric acid scavenges superoxide free radicals (IC₅₀=97.9 μM) and inhibits cancer cell proliferation (EC₅₀ of 15.2-63.9 μg/mL against leukemia, colorectal, gastric, breast, ovarian, prostate, pancreatic and lung cancer cell lines). Lobaric acid inhibits protein tyrosine phosphatase 1B (PTP1B; IC₅₀=0.87 μM for human recombinant enzyme) and 12(S)-HETE produced by 12(S)-lipoxygenase (IC₅₀=28.5 μM). Lobaric acid (250 μM) also reduced pathological changes in tobacco leaves infected with tobacco mosaic virus (TMV).

MLS000536924 is a potent and selective inhibitor of human epithelial 15-lipoxygenase-2 with competitive activity. MLS000536924 exhibits more than 50-fold selectivity in inhibiting h15-LOX-2 and can be effectively applied to study its role in atherosclerosis, cystic fibrosis, and ferroptosis. The binding mode of MLS000536924 shows stronger restriction of protein movement than other inhibitors, further verifying its higher biological activity.

MLS000545091 is a potent and selective lipoxygenase-2 (LOX-2) inhibitor with an IC₅₀ value of 2.6 μM for h15-LOX-2.

1-Naphthyl 3,5-dinitrobenzoate is a potent 5-lipoxygenase inhibitor with IC₅₀ values of 1.04 µM and 3.6 µM for 5-LOX and mPGES-1, respectively. 1-Naphthyl 3,5-dinitrobenzoate has strong inhibition activity in the human whole blood (HWB) assay with an IC₅₀ value of 8.6 μM. 1-Naphthyl 3,5-dinitrobenzoate can be used in research of inflammation.

UCB-35440 is an orally active histamine H1 receptor antagonist and 5-lipoxygenase inhibitor. UCB-35440 can be used for the research of dermatologic inflammatory conditions.

(-)-Dihydroguaiaretic acid is a Lipoxygenase inhibitor that has antioxidant activity. (-)-Dihydroguaiaretic acid inhibits the oxidation of unsaturated fatty acids and removes free radicals. (-)-Dihydroguaiaretic acid also has anticancer activity with an IC₅₀ value of 7.49 μM (A549 cells).

15(S)-HETRE is the hydroxy-trienoic acid resulting from 15-lipoxygenation of dihomo-γ-linolenic acid. It is an inhibitor of 5-LO in human PMNL with an IC₅₀ value of 4.6 μM. In RBL cells, 15(S)-HETrE inhibits 5-LO, but is about 1/20 as potent as 15(S)-HpETE.

Ro 3-1314 (9a,12a-Octadecadiynoic acid) is a plant lipoxygenase inhibitor. Ro 3-1314 is a linoleic acid metabolism inhibitor. Ro 3-1314 stimulates the antigen-induced contraction of guinea-pig tracheal spirals and the immunological release of slow reacting substance of anaphylaxis (SRS-A) from actively sensitized guinea-pig lung fragments.

BW B70C is a potent, selective and orally activearachidonic acid 5-lipoxygenase inhibitor. BW B70C inhibits both acute and allergic bronchoconstriction and late-phase eosinophil accumulation subsequent to allergen inhalation in guinea-pigs. BW B70C prevents leukotriene C4 synthesis and reduces leucocyte migration to the airways lumen as well as albumin microvascular leakage. BW B70C has the potential for the research of anti-asthma agent.

L-674573 is a quinoline leukotriene synthesis inhibitor, inhibiting Calcimycin (HY-N6687)- and N-Formyl-Met-Leu-Phe (HY-P0224)-induced leukotriene production with IC₅₀s of 100 nM and 50 nM, respectively. L-674573 selectively inhibits Calcimycin- and N-Formyl-Met-Leu-Phe-induced 5-lipoxygenase translocation.

5-LOX-IN-1 (compound 2b) is an inhibitor of human 5-Lipoxygenase (5-LOX) with an IC₅₀ value of 2.3 μM. 5-LOX-IN-1 can be used for the research of inflammation.

3-Chloroiminodibenzyl (compound 8) is a dual inhibitor of sHE and 5-LOX. 3-Chloroiminodibenzyl inhibits sHE and 5-LOX with IC₅₀ of 140 μM and 6.5 μM, respectively.

ER-34122 is a dual 5-lipoxygenase/cyclooxygenase inhibitor with oral activity. ER-34122 has anti-inflammatory activity.

Eriodictyol chalcone is an antioxidant that inhibits multiple key enzymes including 5-LOX (IC₅₀=0.043 μM), aromatase/CYP19A1 (IC₅₀=2.8 μM), PTPase 1B (IC₅₀=1.26 μM), and COX (IC₅₀=34 μM). Eriodictyol chalcone exhibits excellent free radical scavenging activity. Eriodictyol chalcone not only inhibits the growth of plasmodia and enhances the efficacy of Artemisinin (HY-B0094), but also reduces depression-like behaviors in animal models. Eriodictyol chalcone serves as a biosynthetic precursor for Aureusidin (HY-N9834). Eriodictyol chalcone is a potential dietary supplement and herbicide, and it can be applied to research on malaria, depression, breast cancer and other related diseases.