2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Lipoxygenase

Lipoxygenase

LOX

Lipoxygenase

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Lipoxygenases (LOXs) are a family of enzymes that are responsible for the metabolism of arachidonic and docosahexaenoic acid and for the formation of several eicosanoids and docosanoids, including leukotrienes, lipoxins and neuroprotectins. Depending on cells' redox state and other milieu conditions, these enzymes are engaged in oxidative stress and cell death mechanisms or in cell protection. Lipoxygenases are lipid peroxidizing enzymes, implicated in the pathogenesis of inflammatory and hyperproliferative diseases, which represent potential targets for pharmacological intervention.

Lipoxygenases are classified on the basis of site of arachidonate oxygenation into 5-, 8-, 9-, 11-, 12- and 15-LOX. The prominent animal LOXs are 5-LOX, 8-LOX, 12-LOX and 15-LOX, while the plant LOXs are mostly 5-LOX and 15-LOX. Among these, 5-LOX is the most predominant isoform associated with the formation of 5-hydroperoxyeicosatetraenoic acid (5-HpETE) and other bioactive lipid mediators.

Lipoxygenase Isoform Specific Products:

Lipoxygenase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-162166
    COX-2/15-LOX/mPGES1-IN-1
    		Inhibitor
    COX-2/15-LOX/mPGES1-IN-1 (Compound 2c) is an inhibitor of COX-2, 15-LOX, and mPGES-1 enzymes with IC50 values of 0.057, 2.39, and 2.8 μM, respectively. COX-2/15-LOX/mPGES1-IN-1 possesses anti-inflammatory activity and can inhibit rat paw edema in vivo experiments.
    COX-2/15-LOX/mPGES1-IN-1
  • HY-100148
    ICI 211965
    		Inhibitor
    ICI 211965 (ZM-211965) is a selective and orally potent 5-Lipoxygenase (5-LPO) inhibitor.
    ICI 211965
  • HY-159169
    5-LOX/sEH-IN-1
    		Inhibitor
    5-LOX/sEH-IN-1 (Compound 8o) is a dual 5-LOX/sEH-IN-1 inhibitor with cardioprotective effects, exhibiting IC50 values of 3.05 μM and 2.20 nM respectively, and 5-LOX/sEH-IN-1 can also inhibit the activity of COX-2 (IC50=10.50 μM). 5-LOX/sEH-IN-1 has analgesic and anti-inflammatory effects, while reducing ulcer pathogenicity, and can be used to develop anti-inflammatory agents with fewer gastrointestinal and cardiovascular side effects.
    5-LOX/sEH-IN-1
  • HY-B1452S1
    Licofelone-d6
    Licofelone-d6 is the deuterium labeled Licofelone. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.
    Licofelone-d<sub>6</sub>
  • HY-178214
    CSBP ligand 1
    		Inhibitor
    CSBP ligand 1 (Compound 36) is a ligand of CSBP, with an IC50 of 0.08 μM for CSBP binding. CSBP ligand 1 can inhibit the production of TNF in mice treated with LPS (HY-D1056). CSBP ligand 1 has no significant inhibitory activity against PGHS-1 (IC50: 16 μM) and 5-LO (IC50: 60 μM). CSBP ligand 1 can be used in the research of inflammation-related diseases.
    CSBP ligand 1
  • HY-124674
    CCT365623
    CCT365623 is a potent and orally active LOX inhibitor with an IC50 of 0.9 μM. CCT365623 has potent anti-metastatic efficacy in vivo.
    CCT365623
  • HY-N8480
    Atractylochromene
    		Inhibitor
    Atractylochromene is a potent dual inhibitor of 5-LOX/COX-1 with IC50s of 0.6 and 3.3 μM, respectively.
    Atractylochromene
  • HY-121099
    Cgp 8065
    		Inhibitor
    L-689065 is a 5-lipoxygenase inhibitor.
    Cgp 8065
  • HY-151173
    XO/COX/LOX-IN-1
    		Inhibitor
    XO/COX/LOX-IN-1 (compound 7i) is a potent xanthine oxidase/cyclooxygenases/lipoxygenases (XO/COX/LOX) inhibitor. XO/COX/LOX-IN-1 can be used in studies of inflammation, cancer and metabolic diseases.
    XO/COX/LOX-IN-1
  • HY-123103
    Linetastine
    		Inhibitor
    Linetastine is an orally active and potent 5-Lipoxygenase inhibitor. Linetastine shows antihistamine activity. Linetastine inhibits leukotriene production and antagonizes the effect of histamine. Linetastine inhibits the release of leukotrienes B4 and C4 from calcium ionophore-stimulated human leukocytes.
    Linetastine
  • HY-105396
    L 670630
    		Inhibitor
    L 670630 is a potent and orally active inhibitor of 5-lipoxygenase, with the IC50 of 23 nM.
    L 670630
  • HY-173180
    5-LOX-IN-8
    		Inhibitor
    5-LOX-IN-8 is a 5-LOX inhibitor with anti-inflammatory activity. 5-LOX-IN-8 suppresses IL-6, IL-1β, TNF-α and IFN-γ in macrophages and reduces IL-8 secretion in SW480 cells. 5-LOX-IN-8 reduces disease activity in a DSS colitis model. 5-LOX-IN-8 can be used for research of inflammatory bowel disease (IBD).
    5-LOX-IN-8
  • HY-120760
    L-691831
    L-691831 is a ligand for 5-lipoxygenase activating protein binding assays that has utility as a tool for studying 5-lipoxygenase activating protein (FLAP) related activities. L-691831 can be used to measure the affinity of FLAP on the leukocyte membrane for leukotriene synthesis inhibitors, with binding being correlated with inhibition of leukotriene synthesis.
    L-691831
  • HY-101579
    LY 178002
    		Antagonist
    LY 178002 is a potent inhibitor of 5-lipoxygenase (5-LPO), phospholipase A2, with IC50 of 0.6 μM for 5-lipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.
    LY 178002
  • HY-N11845
    Sigmoidin B
    		Inhibitor
    Sigmoidin B, a prenylated flavanone, is a selective 5-lipoxygenase inhibitor. Sigmoidin B is a potent scavenger of the DPPH radical. Sigmoidin B has antigenotoxic activity that inhibits genotoxicity induced by Aflatoxin B1 (HY-N6615), with an IC50 of 18.7 μg/mL. Sigmoidin B has anti-inflammatory activity and antioxidant properties.
    Sigmoidin B
  • HY-173115
    15-LOX-IN-2
    		Inhibitor
    15-LOX-IN-2 (Compound 2a) is an orally active COX-2/15-LOX inhibitor and a partial agonist of PPARγ. 15-LOX-IN-2 has anti-inflammatory activity and inhibits the levels of 20-HETE, IL-1β and TNF-α in RAW 264.7 cells treated with LPS (HY-D1056). In addition, 15-LOX-IN-2 has significant glucose uptake capacity in the absence of insulin. 15-LOX-IN-2 can be used for the research of metabolic diseases.
    15-LOX-IN-2
  • HY-121586
    Nafazatrom
    		Inhibitor
    Nafazatrom (Bay g 6575) is an orally active cardioprotective agent that protects against ischemic damage. Nafazatrom dose-dependently inhibits neutrophil aggregation, superoxide anion generation, arachidonic acid metabolism, and to a lesser extent the release of β-glucosidase, platelet aggregation or arachidonic acid in vitro. Acid metabolism has no significant effect. In a dog ischemia-reperfusion model, Nafazatrom (10 mg/kg; po) reduced infarct size and the occurrence of arrhythmias and rescued ischemic myocardial function without affecting any hemodynamic changes. The basis of Nafazatrom's cardioprotection may be inhibition of neutrophil function and cellular infiltration in vitro.
    Nafazatrom
  • HY-121987
    15(S)-HEDE
    		Inhibitor
    15(S)-HEDE (Compound 8) is an analogue of 15-HEDE (HY-121987A) that inhibits 5-lipoxygenase with an IC50 value of 26 μM. 15(S)-HEDE is promising for research of inflammatory disease.
    15(S)-HEDE
  • HY-N3451
    Isothymusin
    		Inhibitor
    Isothymusin is a potent anti-oxidant agent. Isothymusin shows radical scavenging activities. Isothymusin shows anti-proliferative activities in cancer cell lines. Isothymusin inhibited the enzymes associated with the promotion stage of cancer, including cycloxygenase- 2 and lipoxygenase-5.
    Isothymusin
  • HY-173055
    Ferroleuton
    		Inhibitor
    Ferroleuton is a competitive, selective inhibitor for 5-lipoxygenase with an IC50 of 0.21 μM. Ferroleuton exhibits antioxidant activity in DPPH (scavenges 86% DPPH-H at 50 μM), ABTS (EC50=19.42 μM) and FRAP (EC50=3.32 μM) assays.
    Ferroleuton
Cat. No. Product Name / Synonyms Application Reactivity
Lipoxygenase Isoform Comparison

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