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Lipoxygenase

Lipoxygenases are a family of (non-heme) iron-containing enzymes most of which catalyze the dioxygenation of polyunsaturated fatty acids in lipids containing a cis,cis-1,4- pentadiene into cell signaling agents that serve diverse roles as autocrine signals that regulate the function of their parent cells, paracrine signals that regulate the function of nearby cells, and endocrine signals that regulate the function of distant cells.The lipoxygenases are related to each other based upon their similar genetic structure and dioxygenation activity. However, one lipoxygenase, ALOXE3, while having a lipoxygenase genetic structure, possesses relatively little dioxygenation activity; rather its primary activity appears to be as an isomerase that catalyzes the conversion of hydroperoxy unsaturated fatty acids to their 1,5-epoxide, hydroxyl derivatives.

  • NNK
    T2053364091-91-4
    NNK (Nicotine-derived nitrosamine ketone) is a procarcinogen and a major tobacco-specific toxicant. It inhibits the expression of lysyl oxidase which is a tumor suppressor.
    • $55
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  • Abietic Acid
    T3090514-10-3
    Abietic Acid (Sylvic acid) is the primary component of resin acid isolated from rosin.
    • $83
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  • 2,5-Di-tert-butylhydroquinone
    T754088-58-4
    2,5-Di-tert-butylhydroquinone (BHQ) is an effective and selective endoplasmic reticulum Ca2+-ATPase inhibitor.
    • $29
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  • Malotilate
    T657659937-28-9
    Malotilate (Kantec) is a medicine used for the therapy of liver cirrhosis.
    • $45
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  • 5-LOX inhibitor
    T65427106461-41-0
    5-LOX inhibitor (1-(sec-Butyl)-4-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)-1H-1,2,4-triazol-5(4H)-one) is one of the impurities of itraconazole, a selective LOX-5 inhibitor.
    • $50
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  • 5-Aminosalicylic Acid
    T064689-57-6
    5-Aminosalicylic Acid (5-ASA) is an anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE.
    • $45
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  • ABT-963
    T26531266320-83-6
    ABT-963 is a potent and selective inhibitor of disubstituted pyridazinone cyclooxygenase-2 (LOX2) that dose-dependently reduces injury perception in a carrageenan model of nociceptive sensitization.ABT-963 is used in the study of arthritis.
    • $293
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  • CBS-1114 HCl
    T68037L33244-00-7In house
    CBS-1114 HCl (N-Phenylbenzamidrazone hydrochloride) is a 5-lipoxygenase inhibitor and an anti-inflammatory compound in a good eye-permeable model.CBS-1114 HCl maintains and improves cardiac function, attenuates cardiac dysfunction, as well as reduces epicardial adipose tissue and/or pericardial adipose tissue in subjects with cardiovascular disease.
    • $195
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  • S-2474
    T16817158089-95-3In house
    S-2474, an inhibitor of COX-2 and 5-lipoxygenase, has anti-inflammatory and neuroprotective activities and inhibits Abeta (25 - 35) and Abeta (1 - 40) induced cell death.
    • $293 TargetMol
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  • ER-34122
    T70188179325-62-3In house
    ER-34122, a novel orally available dual 5-lipoxygenase/cyclooxygenase inhibitor, exhibits potent anti-inflammatory activity in an arachidonic acid-induced ear inflammation model.
    • $195
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  • Linetastine
    T25737159776-68-8In house
    Linetastine (TMK-688) is a 5-lipoxygenase inhibitor (5-LOX) that inhibits leukotriene production and antagonizes the effects of histamine.Linetastine is used in studies of asthma, atherosclerosis, and peptic ulcers.
    • $130
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  • Butibufen
    T2692655837-18-8In house
    Butibufen (FF-106) is an orally active non-steroidal anti-inflammatory compound, a potential cyclooxygenase inhibitor with analgesic and antipyretic activity, and inhibits urea synthesis.Butibufen has been used in the study of rheumatic diseases.
    • $35
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  • REV 5901A
    T21821L92532-23-5In house
    REV 5901A (REV 5901 HCl) is an orally active leukotriene receptor antagonist and 5-lipoxygenase inhibitor with antimicrobial activity that attenuates colon cancer growth in mice.REV 5901A has been used in studies of asthma and myocardial infarction. REV 5901A is used to study asthma and myocardial infarction.
    • $195 TargetMol
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  • CJ-13,610 hydrochloride
    T27026L179420-27-0In house
    CJ-13,610 hydrochloride is an orally active nonredox-type inhibitor of 5-LOX and can be used in studies about the prevention of untoward pathophysiological effects of LTs.
    • $50
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  • 1-Naphthyl 3,5-dinitrobenzoate
    T2183893261-39-3
    1-Naphthyl 3,5-dinitrobenzoate (JMC-4) is an inhibitor of 5-LOX can be used in studies about inflammatory therapy.
    • $73
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  • 12R-LOX-IN-2
    T77677
    12R-LOX-IN-2 is an inhibitor of 12R-lipoxygenase (12R-LOX).12R-LOX-IN-2 inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and inhibits colony formation.12R-LOX-IN-2 also decreases the protein level of Ki67 and the mRNA expression of IL-17A in IMQ-induced cells. 12R-LOX-IN-2 may be useful in the study of psoriasis and other skin-associated inflammatory diseases.
    • $40
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  • Efletirizine
    T27244150756-35-7In house
    Efletirizine (UCB-28754) is a histamine receptor antagonist with inhibitory effects on the enzyme 5-lipoxygenase (5-LO), and is useful in the topical treatment of allergic diseases.
    • $195
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  • A-69412
    T10208123606-23-5In house
    A-69412 (N-1-(Fur-3-ylethyl)-N-hydroxyurea) is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase. It has the potential to treat ulcerative colitis and asthma, and possibly other inflammatory and allergic conditions.
    • $117
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  • Croconazole
    T987877175-51-0In house
    Croconazole exhibited dose-dependent inhibitory activity on the 5-lipoxygenase (5-LOX) of neutrophils. Croconazole is an antimycotic agent. The IC50s for the synthesis of leukotriene B4 (LTB4) and 5-hydroxyeicosatetraenoic acid (5-HETE) is 7.8 +/- 1.7 and
    • $52
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  • 6-Hydroxyflavanone
    TN13084250-77-5
    6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.
    • $50
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  • Setileuton
    T34624910656-27-8In house
    Setileuton (MK0633) is a specific 5-LOX inhibitor and can be used in research on asthma and atherosclerosis.
    • $329
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  • (S)-Coriolic acid
    T3797429623-28-7In house
    (S)-Coriolic acid (13(S)-HODE) is an important intracellular signaling agent, generated by the reaction of linoleic acid with plant and mammalian lipoxygenases, and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid inhibits the adhesion of tumor cells to the vascular endothelium and down-regulates the expression of IRGpIIb/IIIa receptors at around 1 μM. (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX), which often acts as an endogenous ligand to activate PPARγ. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial damage.
    • $389
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  • Lonapalene
    T1680291431-42-4In house
    Lonapalene (RS4317) is a 5-lipoxygenase (5-LO) inhibitor with anti-psoriasis efficacy.Lonapalene topically blocks skin inflammation.
    • $179
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  • RWJ 63556
    T12784190967-35-2In house
    RWJ 63556 is an orally active inhibitor of COX-2 selective/5-lipoxygenase, shows anti-inflammatory activities.
    • $157
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  • ALOX15-IN-2
    T626062764818-23-5In house
    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.
    • $41
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  • PF-4191834
    T165031029317-21-2In house
    PF-4191834 is a noniron chelating and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) with an IC50 of 229 nM. PF-4191834 shows ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX and displays no activity toward the cyclooxygenase enzymes. PF-4191834
    • $48
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  • Utreloxastat
    T605071213269-96-5In house
    Utreloxastat (PTC857) is a novel 15-lipoxygenase inhibitor that can be used to study amyotrophic lateral sclerosis .
    • $108 TargetMol
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  • CJ-13,610
    T27026179420-17-8In house
    CJ-13,610 is an orally active and nonredox-type inhibitor of 5-lipoxygenase (5-LOX). CJ-13,610 inhibits the biosynthesis of leukotriene B4 and regulates the expression of IL-6 mRNA in macrophages.
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    • KKII5
      T772886381-55-1In house
      KKII5 is a potent inhibitor of the lipoxygenase LOX-1 with an IC50 of 19 μM.KKII5 inhibits lipid peroxidation and enhances the ability of the active centers of some compounds to receive electrons.
      • $36
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    • Zileuton
      T0477111406-87-2
      Zileuton (A 64077) is a synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma.
      • $30
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    • Montelukast
      T1677158966-92-8
      Montelukast (Singular) is an orally available leukotriene receptor antagonist which is widely used for the prophylaxis and chronic treatment of asthma and has been linked to rare cases of clinically apparent liver injury.
      • $29
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    • Resveratrol
      T1558501-36-0
      Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.
      • $36
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    • U-73122
      T6243112648-68-7
      U-73122 (U73122) , an effective PLC inhibitor, reduces agonist-induced Ca2+ increases in platelets and PMN.
      • $33
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    • Wedelolactone
      T3384524-12-9
      Wedelolactone (IKK Inhibitor II) inhibits NF-κB-mediated gene transcription in cells by blocking the phosphorylation and degradation of IκBα.
      • $30
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    • Nordihydroguaiaretic acid
      TJS2190500-38-9
      Nordihydroguaiaretic acid (NDGA) (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties.
      • $33
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    • Shogaol
      T6S1699555-66-8
      1. 6-Shogaol (6-Shogaol) has antipyretic and analgesic effects in addition to inhibitory effect on lipoxygenase activity. 2. 6-shogaol has anti-inflammatory property, reduces the inflammatory response and protected the femoral cartilage from damage produced in a CFA monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k/Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2/-9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.
      • $36
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    • Esculetin
      T2798305-01-1
      Esculetin (Cichorigenin) is a coumarin derivative from various natural plant products with various biological and pharmaceutical properties including anti-edema, anti-inflammatory and anti-tumour effects. It inhibits lipoxygenases (LOs).
      • $45
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    • PXS-6302 hydrochloride
      T60438L2584947-79-3
      PXS-6302 hydrochloride is a potent irreversible lysine oxidase (LOX) inhibitor, inhibiting Bovine LOX, rh LOXL1, rh LOXL2, rh LOXL3, and rh LOXL4 with IC50 of 3.7 μM, 3.4 μM, 0.4 μM, 1.5 μM, and 0.3 μM, respectively. PXS-6302 hydrochloride penetrates easily through the skin and is able to reduce collagen accumulation, significantly improving the appearance of scars.
      • $228
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    • 2,3,4'-Trihydroxy-3',5'-dimethoxypropiophenone
      TN268833900-74-2
      2,3,4'-Trihydroxy-3',5'-dimethoxypropiophenone is a natural product obtained from Parinari hypochrysea (Chrysobalanaceae). 2,3,4'-Trihydroxy-3',5'-dimethoxypropiophenone is an antioxidant and lipoxygenase inhibitor. dimethoxypropiophenone has antioxidant activity and inhibits lipoxygenase.
      • $1,268
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    • Ligustroside
      TN187135897-92-8
      Ligustroside shows little antioxidant, and anti-inflammatory properties, it shows a significant inhibition effect on prostaglandin E2 (PGE2)-release. Ligustroside shows moderate antiviral activities against parainfluenza type 3 virus.
      • $1,698
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    • DKI5
      T678701101130-96-4
      DKI5 ((E)-N'-benzylidenehydrazinecarbothiohydrazide) is a LOX-1 inhibitor with an IC50 value of 22.5 μM.DKI5 may have anti-inflammatory and antioxidant activities and has shown anti-lipid peroxidation activity in in vitro bioassays.
      • $73
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    • Pinusolide
      TL001431685-80-0
      Pinusolide is a platelet activating factor ( PAF) antagonist, it may prove of therapeutic value in the treatment of hypotension, it has antileukemic potential, and could be used to treat neurodegenerative diseases. Pinusolide attenuates blockade of insulin signaling by enhancing IRS-1 tyrosine phosphorylation by the activating the AMPK pathway, indicates the targeting of AMPK represents a new therapeutic strategy for hyperglycemia-induced insulin resistance and type 2 diabetes.
      • $310
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    • 4-Methyldaphnetin
      TJS03152107-77-9
      4-Methyldaphnetin (DHMC) is a potent inhibitor (low micromolar) of lipid peroxidation and scavengers of superoxide anion radicals and of aqueous alkylperoxyl radicals, but may be pro-oxidant (enhancing generation of hydroxyl radicals) in the presence of free iron ions.2. 4-Methyldaphnetin(7,8-Dihydroxy-4-methylcoumarin) inhibits the proinflammatory 5-lipoxygenase enzyme at micromolar concentrations.
      • $39
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    • Isotachioside
      TN433131427-08-4
      Isotachioside has15-lipoxygenase (15-LO) inhibitory activities.
      • $210
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    • 5-LOX-IN-2
      T77528179691-97-5
      5-LOx-in-2 is a 5-lipoxygenase inhibitor (5-LOX) with an IC50 value of 0.33 μM. 5-lox-in-2 inhibits 5-LOX action IN a dose-dependent manner. 5-LOX-IN-2 can reduce the cell activity of kidney cancer cells and induce apoptosis, and can be used in cancer research.
      • $52
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    • Diethylcarbamazine citrate
      T14201642-54-2
      Diethylcarbamazine citrate (Caritrol) is an anthelmintic used primarily as the citrate in the treatment of filariasis, particular infestations with Wucheria bancrofti or Loa loa. It is an inhibitor of arachidonic acid metabolism in filarial microfilaria.
      • $36
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    • (+/-)-Sigmoidin A
      TN5020176046-04-1
      Sigmoidin A has moderate antioxidant, antimicrobial and anti-inflammatory activity.
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    • Phenidone
      T2239892-43-3
      Phenidone (1-phenyl-3-pyrazolidinone) is a dual inhibitor of cyclooxygenases and lipoxygenases that ameliorates rat paralysis in experimental autoimmune encephalomyelitis by suppressing its target enzymes[1]. The lipoxygenase inhibitor phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[2].
      • $41
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    • 3-O-Acetyl-11-hydroxy-beta-boswellic acid
      TN1255146019-25-2
      3-O-Acetyl-11-hydroxy-beta-boswellic acid is the precursor of 3-O-acetyl-9, 11-dehydro-beta-boswellic acid(a 5-lipoxygenase inhibitor ).
      • $129
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    • (-)-Bornyl ferulate
      T8065155511-07-4
      (-)-Bornyl ferulate is a dual inhibitor of 5-lipoxygenase and cyclooxygenase (COX), exhibiting half-maximal inhibitory concentrations (IC50s) of 10.4 μM for 5-lipoxygenase and 12.0 μM for COX [1].
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