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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 is a nicotinic nitrosylated derivative. It activates ERK1 2 and PKCα, and activates Bcl2 phosphorylation at Ser70, as well as c-Myc at Thr58 and Ser62.It can be used to construct mouse models of lung cancer, as well as to induce proliferation and survival of human lung cancer cells.
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  • Nordihydroguaiaretic acid
    TJS2190500-38-9
    Nordihydroguaiaretic acid (NDGA) is a natural product, extracted from Pole Fork Kelaroa, and is a lipoxygenase (5-LOX) inhibitor (IC50=8 μM). Nordihydroguaiaretic acid possesses antioxidant and free radical scavenging properties.
    • $25
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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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  • Abietic Acid
    T3090514-10-3
    Abietic Acid (Sylvic acid) is a diterpene extracted from Pimenta racemosavar. grissea with antimicrobial, antiproliferative and anti-obesity activities. It inhibits lipoxygenase activity and may be studied in allergic diseases.
    • $45
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  • ML351
    T21902847163-28-4
    ML351 is a potent and selective inhibitor of human 15-lipoxygenase-1 (15 LOX)(IC50: 200 nM).
    • $48
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  • Kukoamine A
    TN101675288-96-9
    Kukoamine A possesses anticancer, cytoprotective, antioxidant, and anti-inflammatory activities, it also has neuroprotective effects through inhibiting oxidative stress and apoptosis after whole-brain irradiation (WBI) in rats.
    • $94
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  • Licoricesaponin A3
    TN1865118325-22-7
    Licoricesaponin A3 is a terpenoid saponin extracted from Gymnostachyum febrifugum Benth., which has good affinity for 5-LOX receptors.
    • $2,198
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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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  • 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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  • L 651896
    T2430699134-29-9In house
    L 651896 is a novel leukotriene biosynthesis and 5-lipoxygenase inhibitor for the study of respiratory and cardiovascular diseases.
    • $333 TargetMol
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  • Aureusidin
    TN563438216-54-5
    Aureusidin (Auresidin) shows antioxidant and lipoxygenase inhibitory activity with anti-inflammatory effects.
    • $219
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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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  • Tepoxalin
    T7724103475-41-8
    Tepoxalin (RWJ 20485) is a 5-lipoxygenase inhibitor potentially for the treatment of asthma, osteoarthritis. Tepoxalin inhibits COX-1, COX-2, and 5-LOX. Tepoxalin is a potent inhibitor of sheep seminal vesicle cyclooxygenase (COX) (IC50 = 4.6 microM), rat basophilic leukemia cell (RBL-1) lysate COX (IC50 = 2.85 microM) and COX from intact RBL-1 cells (IC50 = 4.2 microM).
    • $51
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  • ABT-963
    T26531266320-83-6In house
    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 TargetMol
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  • Pectolinarigenin
    T6S0413520-12-7
    1. Pectolinarigenin (Pectolinaringenin) exhibits hepatoprotective activity mainly via SOD antioxidant mechanism. 2. Pectolinarigenin possesses anti-inflammatory activity and that they may inhibit eicosanoid formation in inflammatory lesions.
    • $41
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  • Chebulagic acid
    TQ018023094-71-5
    Chebulagic acid, isolated from the Terminalia chebula Retz, is a COX-LOX dual inhibitor.
    • $72
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  • ML355
    T43471532593-30-8
    ML355, a specific, effective 12-Lipoxygenase(12-LOX) inhibitors(IC50=0.34 μM), possess favorable ADME properties.
    • $42
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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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  • 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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  • Xanthatin
    T3S015326791-73-1
    1. Xanthatin has cytotoxic activity. 2. Xanthatin has antibacterial and antifungal activies against MRSA. 3. Xanthatin may have therapeutic potential against NSCLC. 4. Xanthatin can inhibit murine melanoma B16-F1 cell proliferation possibly associated wit
    • $44
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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. It is involved in cell proliferation and differentiation in various biological systems and inhibits the adhesion of tumor cells to the vascular endothelium, while down-regulating IRGpIIb IIIa receptor expression at around 1 μM. Additionally, (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX) and often acts as an endogenous ligand to activate PPARγ. It induces mitochondrial dysfunction and airway epithelial damage.
    • $389
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  • Caffeic Acid
    T2807331-39-5
    Caffeic Acid is an orally bioavailable, hydroxycinnamic acid derivative and polyphenol, with potential anti-oxidant, anti-inflammatory, and antineoplastic activities.
    • $33
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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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  • 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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  • PD146176
    T75304079-26-9
    PD146176 (NSC-168807) is an inhibitor of 15-Lipoxygenase (15-LO) , it inhibits rabbit reticulocyte 15-LO with Ki of 197 nM and IC50 of 0.54 μM. PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.
    • $41
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  • Silychristin
    T387933889-69-9
    Silychristin (Silicristin) is a plant growth regulator. Silychristin is an anti-hepatotoxic agent. Silychristin is the inhibitor of horseradish peroxidases and lipoxygenase.
    • $43
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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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  • 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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  • 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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  • β-Boswellic acid
    TN1097631-69-6
    β-Boswellic acid (Beta-boswellic acid) and its derivatives (the major constituents of Boswellin) have anti-carcinogenic, anti-tumor, and anti-hyperlipidemic activities.
    • $89
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  • Masoprocol
    T6069227686-84-6
    Masoprocol (meso-Nordihydroguaiaretic acid) is a potent, orally active lipoxygenase inhibitor that exhibits antihyperglycemic activity, making it potentially valuable for type II diabetes research. In vivo, Masoprocol reduces glucose and hepatic triglyceride concentrations [1] [2] [3].
    • $166
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  • Phenethyl ferulate
    TN233071835-85-3
    Phenethyl ferulate (Caffeic Acid 3-Methyl Phenethyl Ester) has chemopreventive properties against chemically induced colon carcinogenesis. It enhances apoptosis in azoxymethane induced colon tumors. It shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively.
    • $54
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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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  • Psoralidin
    T339918642-23-4
    Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally. Psoralidin possesses anticancer and chemopreventive properties.
    • $57
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  • S-(+)-Marmesin
    T575913849-08-6
    S-(+)-Marmesin (marmesin) is a coumarin originally isolated from the mature bark of A. marmelos,exhibiting COX-2 5-LOX dual inhibitory activity.
    • $30
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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
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  • Embelin
    T6485550-24-3
    Embelin (Embelic acid), isolated from the Japanese Ardisia herb, is an inhibitor of the X-linked inhibitor of apoptosis (IC50: 4.1 uM).
    • $50
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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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  • 11-​Keto-​beta-​boswellic acid
    TN118217019-92-0
    11-Keto-beta-boswellic acid, a novel Nrf2 activator, and a selective 5-lipoxygenase (5-LOX) inhibitor; it exerts dose dependent cardioprotective effect manifested by dose-dependent reduction in serum lactate dehydrogenase
    • $55
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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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  • 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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  • Indirubin-3'-monoxime
    T5200160807-49-8
    Indirubin-3'-monoxime (Indirubin-3'-oxime) is a potent inhibitor of GSK3β (IC50: 22 nM) and also inhibits CDKs ( (IC50s: 100 180 250 nM for Cdk5 p35, Cdk1 cyclin B, Cdk2 cyclin E).
    • $37
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  • LOX-IN-3 dihydrochloride
    T399862409964-23-2
    LOX-IN-3 dihydrochloride, an inhibitor of lysyl oxidase (LOX), inhibits bovine LOX (IC50<10 μM) and human LOXL2 (IC50<1 μM) activities.
    • $52
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  • 4',5-Dihydroxyflavone
    T82606665-67-4
    4',5-Dihydroxyflavone is a soybean LOX-1 inhibitor (Ki: 102.6 μM) and a yeast α-Glucosidase inhibitor (IC50: 66 μM).
    • $34
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  • CAY10698
    T8950684236-01-9
    CAY10698 is a 12-lipoxygenase inhibitor (12-LO; IC50 of 5.1 µM).
    • $34
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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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  • 5-O-Demethylnobiletin
    T57142174-59-6
    5-O-Demethylnobiletin (5-DEMETHYLNOBILETIN) is a natual product, has anti-inflammatory activity, it may act through a direct inhibition of 5-LOX, without affecting the expression of COX-2.
    • $59
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  • BI-0115
    T91084929-23-1
    BI-0115 is a selective small molecule inhibitor of LOX-1 that blocks cellular uptake of oxLDL. It binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain. The structure of LOX-1 bound to BI-0115 shows that inte
    • $112
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  • Licofelone
    T6568156897-06-2
    Licofelone (ML-3000) is a dual COX LOX inhibitor potentially for treating osteoarthritis, acting as both an analgesic and anti-inflammatory. By inhibiting 5-LOX, it may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase).
    • $38
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  • Cirsiliol
    T1082134334-69-5
    Cirsiliol is a 5-lipoxygenase (5-LOX) inhibitor and low affinity benzodiazepine receptor ligand.Cirsiliol inhibits cell proliferation and promotes apoptosis of OS cells.Cirsiliol shows antitumor activity against OS cells in an in situ xenograft tumor model and can be used to study colon cancer.
    • $55
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