1. シグナル伝達
  2. Metabolic Enzyme/Protease
  3. Lipoxygenase

Lipoxygenase

LOX

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.

製品番号 製品名 製品効果 純度 構造式
  • HY-133159
    Resolvin E2 98.5%
    Resolvin E2 ((-)-Resolvin E2) is an endogenous lipid mediator produced from eicosapentaenoic acid (EPA) under the catalysis of 5-lipoxygenase (5-LOX), and its production increases in hypoxic environments. Resolvin E2 antagonizes BLT1, partially activates ChemR23, and promotes ubiquitin-proteasome-mediated degradation of COX-2. Resolvin E2 reduces the production of prostaglandin E2, blocks polymorphonuclear leukocyte infiltration, and promotes the resolution of airway inflammation. Resolvin E2 ameliorates lipopolysaccharide (LPS) (HY-D1056)-induced depressive-like behaviors. Resolvin E2 can be used in research related to depression, murine peritonitis, neonatal asthma, and other conditions.
    Resolvin E2
  • HY-W010144
    Phenidone Inhibitor 98.96%
    Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat. Phenidone is used as a photographic developer.
    Phenidone
  • HY-W012399
    2,5-Di-tert-butylhydroquinone

    2,5-Di-tert-butylhydroquinone

    Modulator 99.90%
    2,5-Di-tert-butylhydroquinone (BHQ) (Compound 2), an indirect food additive, is a Sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) inhibitor with an IC50 of 400 nM. 2,5-Di-tert-butylhydroquinone disrupts the gating function of the residue Glu309 which prevents Ca2+ from reaching their binding site. 2,5-Di-tert-butylhydroquinone regulates the activity of 5-lipoxygenase and COX-2 (IC50: 1.8 and 14.1 μM for 5-LO and COX-2, respectively).
    2,5-Di-tert-butylhydroquinone
  • HY-171955
    LXG6403 Inhibitor 99.85%
    LXG6403 is an orally active and irreversible LOX inhibitor (IC50 = 1.3 μM). LXG6403 is ~3.5-fold more specific for LOX than LOXL2 and does not inhibit LOXL1. LXG6403 inhibits FAK signaling and induces ROS generation and DNA damage, leading to G1 arrest and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines. LXG6403 alters the extracellular matrix (ECM) and collagen structure, reducing collagen cross-linking and deposition, thereby increasing drug penetration and reducing tumor stiffness. LXG6403 overcomes Doxorubicin (HY-15142) resistance in chemoresistant TNBC PDX in vivo and can be used to study high-stiffness resistant tumors.
    LXG6403
  • HY-W749694
    Cannflavin B Inhibitor 98.36%
    Cannflavin B is a flavonoid compound that can be isolated from Cannabis sativa L. Cannflavin B is inhibitors of PGE2 release (IC50: 0.7 μM), mPGES-1 (IC50: 3.7 μM), and 5-lipoxygenase. Cannflavin B has multiple activities such as anti-inflammatory, antioxidant, anti-glycation, anti-ferroptosis, anti-tumor, and anti-Leishmania (IC50: 14 μM). Cannflavin B can also inhibit the TrkB-BDNF signaling pathway.
    Cannflavin B
  • HY-130675A
    15(S)-HEPE 99.9%
    15(S)-HEPE is a monohydroxy fatty acid. 15(S)-HEPE is biosynthesized from eicosapentaenoic acid by 15-lipoxygenase (15-LO). Serum levels of 15(S)-HEPE are elevated in patients with asthma.
    15(S)-HEPE
  • HY-101051
    2-TEDC Inhibitor 99.58%
    2-TEDC is a potent inhibitor of 5-, 12-, and 15-lipoxygenase with IC50 values of 0.09 μM, 0.013 μM and 0.5 μM, respectively. 2-TEDC can be used for the research of atheroscrelosi.
    2-TEDC
  • HY-W009248
    Phenethyl ferulate Inhibitor 99.66%
    Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively.
    Phenethyl ferulate
  • HY-12886
    Docebenone Inhibitor 99.02%
    Docebenone (AA 861) is a potent, selective and orally active 5-LO (5-lipoxygenase) inhibitor.
    Docebenone
  • HY-124108
    Eicosatetraynoic acid

    Eicosatetraynoic acid

    Inhibitor 99.9%
    Eicosatetraynoic acid (ETYA) is a non-metabolizable analog of Arachidonic acid (HY-109590) and also an inhibitor of the lipoxygenase (LOX)/cyclooxygenase (COX) pathway (ID50 = 8 μM and 4 μM). Eicosatetraynoic acid acts as a suicide substrate to inhibit the production of inflammatory mediators such as leukotrienes and prostaglandins. Eicosatetraynoic acid acts directly on cell membranes and membrane proteins to exert a wide range of effects, including blocking potassium channels, increasing cell membrane fluidity, elevating intracellular calcium levels, inhibiting DNA synthesis in tumor cells, inducing differentiation of certain cells, and specifically inhibiting the assembly and replication of orthopoxviruses. Eicosatetraynoic acid alleviates acute lung injury induced by chemicals such as phosgene.
    Eicosatetraynoic acid
  • HY-117048
    PF-4191834

    PF-4191834

    Inhibitor 99.48%
    PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain.
    PF-4191834
  • HY-W008833
    3-Aminobutanoic acid Inhibitor 98.0%
    3-Aminobutanoic acid is a β-amino acid. 3-Aminobutanoic acid can protect plant against a challenge infection with P. infestans. 3-Aminobutanoic acid has various levels of susceptibility for the pathogen.
    3-Aminobutanoic acid
  • HY-132845
    Utreloxastat Inhibitor 99.32%
    Utreloxastat (PTC857) is an orally active and blood-brain barrier-permeable 15-lipooxygenase inhibitor. Utreloxastat is a weak inhibitor of CYP1A2 and 2B6 with an IC50 of >5.3 μM. Utreloxastat reduces oxidative stress and inhibits the consumption of reduced glutathione and ferroptosis. Utreloxastat can be used in the study of neurodegenerative diseases characterized by high levels of oxidative stress and mitochondrial pathology, such as amyotrophic lateral sclerosisc.
    Utreloxastat
  • HY-N1942
    5-O-Demethylnobiletin Inhibitor 99.91%
    5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Citrus jambhiri Lush., is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM.
    5-O-Demethylnobiletin
  • HY-138688
    Cinnamyl-3,4-dihydroxy-α-cyanocinnamate Inhibitor 99.41%
    Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) is a potent 12/15-Lipoxygenases (LO) inhibitor. Cinnamyl-3,4-dihydroxy-α-cyanocinnamate has the potential for the research of type 1 diabetes mellitus.
    Cinnamyl-3,4-dihydroxy-α-cyanocinnamate
  • HY-105024
    FPL 62064 Inhibitor 99.25%
    FPL 62064 is a potent 5-lipoxygenase (5-LOX) and COX dual inhibitor, with IC50 values of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase (cyclooxygenase), respectively. FPL 62064 has potent anti-inflammatory activity.
    FPL 62064
  • HY-N6079
    Timosaponin A1 Inhibitor 99.70%
    Timosaponin A1, a natural steroidal saponin, is a 5-lipoxygenase (5-LO), COX-2, and dipeptidyl peptidase 4 (DPP-4) inhibitor with IC50s of 3.29 µM, 36.43 µM, and 33.25 µM, respectively.
    Timosaponin A1
  • HY-139196
    ThioLox Inhibitor 99.74%
    ThioLox is a competitive 15-lipoxygenase-1 (15-LOX-1) inhibitor with a Ki of 3.30 μM. ThioLox shows anti-inflammatory and neuroprotective properties.
    ThioLox
  • HY-N7012
    7,3',4'-Tri-O-methylluteolin Inhibitor 99.28%
    7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid with multiple biological activities. 7,3',4'-Tri-O-methylluteolin inhibits soybean lipoxygenase (LOX), with an IC50 value of 23.97 µg/mL. 7,3',4'-Tri-O-methylluteolin possesses anti-inflammatory effects in Lipopolysaccharides (HY-D1056) (LPS)-induced RAW 264.7 macrophages. 7,3',4'-Tri-O-methylluteolin inhibits the binding of MDM2 with p53 and induces apoptosis in MCF-7 breast cancer cells. 7,3',4'-Tri-O-methylluteolin also has antioxidant, antifungal and antitrypanosomal activitiessup>[4]sup>[5].
    7,3',4'-Tri-O-methylluteolin
  • HY-106200
    CJ-13,610

    CJ-13,610

    Inhibitor 98.10%
    CJ-13,610, a nonredox-type 5-LO inhibitor, dose dependently suppresses 5-LO product formation in ionophore A23187-stimulated PMNL in the absence of exogenous AA with an IC50 of about 70 nM. PMNL: polymorphonuclear leukocytes; AA: arachidonic acid
    CJ-13,610
製品番号 製品名 / Synonyms Application Reactivity

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