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Lipoxygenase (LOX) inhibitors block enzymes that insert molecular oxygen into arachidonic acid and related fatty acids. 5-Lipoxygenase (5-LOX) starts leukotriene synthesis, while 12-LOX and 15-LOX form hydroxylated lipid mediators linked to inflammation and ferroptosis. In 1990, leukotriene synthesis in intact cells was shown to require 5-lipoxygenase-activating protein (FLAP), a membrane partner of 5-LOX. The category covers both points of attack on the leukotriene pathway. Zileuton inhibits 5-LOX directly, whereas MK 886 suppresses leukotriene biosynthesis by binding FLAP. PD146176 is a 15-LOX inhibitor that also appears in ferroptosis research, where lipid peroxidation drives cell death. Baicalein, a flavone from Scutellaria baicalensis roots, is a plant-derived lipoxygenase inhibitor used across several of these models.
A-78773 is a potent inhibitor of 5-lipoxygenase, demonstrating significant inhibition of leukotriene B4 (LTB4) production in human whole blood and neutrophils, with IC50 values of 85 nM and 20 nM, respectively. This compound is valuable for research into inflammation-related diseases, providing insights into leukotriene-mediated pathways and potential therapeutic interventions.
Zileuton sulfoxide is a selective inhibitor of lipoxygenase 5-LOX, targeting the lipoxygenase pathway involved in inflammatory responses. It exhibits significant anti-asthmatic properties, making it valuable in studying respiratory conditions and related inflammatory diseases. This compound is useful for research applications focusing on the modulation of leukotriene biosynthesis and understanding the role of 5-LOX in various pathological processes.
L-651392 is a selective inhibitor of 5-lipoxygenase, effectively blocking the synthesis of leukotrienes. This compound demonstrates significant anti-inflammatory properties, particularly in the context of Escherichia coli pyelonephritis, by hindering the migration of inflammatory cells to the infection site and safeguarding renal tubules from inflammation-induced damage. L-651392 serves as a valuable tool for research focused on inflammatory processes and renal pathologies.
A-79175 is a potent inhibitor of 5-lipoxygenase, a key enzyme involved in the synthesis of leukotrienes. By suppressing leukotriene formation, A-79175 demonstrates significant potential for the investigation of various allergic and inflammatory conditions, such as asthma, allergic rhinitis, rheumatoid arthritis, and inflammatory bowel disease. Its mechanism of action makes it a valuable tool for research in the field of immunology and inflammation.
(E)-L-652343 is a selective inhibitor of lipoxygenase pathways, demonstrating potent activity against cyclooxygenase and 5-lipoxygenase. This compound effectively reduces the synthesis of inflammatory products associated with these pathways in vivo. Additionally, (E)-L-652343 displays high sensitivity and specificity for detecting geometric isomers in both canine and human plasma, with a notable difference in the elimination rates of its E and Z isomers. Its selective metabolism further supports its utility in biochemical research and therapeutic applications targeting inflammatory disorders.
LP117 is a potent inhibitor of 5-Lipoxygenase (5-LO), demonstrating an IC50 value of 1.1 μM. This compound impedes the synthesis of 5-LO products, thereby regulating inflammatory pathways. LP117 is applicable in research focused on inflammatory diseases, asthma, and other conditions influenced by leukotriene metabolism. Its selectivity and efficacy make it a valuable tool for studying lipoxygenase-related mechanisms in biological systems.
Lagunamycin is a selective inhibitor of 5-lipoxygenase, derived from the culture medium of Streptomyces sp. AA0310. It demonstrates significant inhibitory activity with an IC50 value of 6.08 μM against rat 5-lipoxygenase, effectively preventing leukotriene biosynthesis. Notably, lagunamycin achieves this inhibition without inducing lipid peroxidation, making it a valuable tool for studying inflammatory processes and potential therapeutic applications in conditions mediated by 5-lipoxygenase activity.
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BI-L-357 is a lipoxygenase inhibitor that serves as a precursor derived from BI-L-226. It enhances oral bioavailability and effectively inhibits 5-lipoxygenase-mediated leukotriene production, making it a valuable tool for research focused on inflammatory responses and related signaling pathways. This compound's ability to modulate leukotriene levels offers significant potential in studies investigating asthma, allergic reactions, and other inflammatory disorders.
Fenleuton is a potent inhibitor of 5-lipoxygenase, an enzyme involved in the synthesis of leukotrienes. By blocking this pathway, Fenleuton demonstrates significant potential for the study of leukotriene-mediated inflammatory diseases, particularly in exploring its role in asthma, rheumatoid arthritis, and other inflammatory conditions. This reagent is valuable for researchers investigating therapeutic strategies targeting leukotriene-related pathways.
SB 210661 is a potent and selective inhibitor of 5-lipoxygenase, a key enzyme involved in the biosynthesis of leukotrienes. By inhibiting this enzyme, SB 210661 modulates inflammatory responses and has potential applications in the study of asthma, arthritis, and other inflammatory diseases. This compound serves as a valuable tool for researchers investigating the role of leukotrienes in various biological processes.
Leukotriene A 3 methyl ester is a lipoxygenase metabolite derived from 5,8,11-eicosatrienoic acid through the 5-lipoxygenase (5-LO) pathway. This compound exhibits significant biological activity, particularly in the modulation of inflammatory responses and immune cell signaling. It is commonly used in research applications focused on leukotriene biosynthesis and related inflammatory processes.
Synonyms: LDP977
CMI977 is a potent inhibitor of 5-Lipoxygenase (5-LO), an enzyme involved in the biosynthesis of leukotrienes. By effectively inhibiting 5-LO, CMI977 demonstrates significant anti-inflammatory properties, making it a valuable tool for research in inflammation and related diseases. Its application extends to studies focused on the modulation of leukotriene-mediated pathways, providing insights into targeted therapies for various inflammatory conditions.
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Synonyms: LDP-392
CMI-392 is a dual inhibitor of 5-lipoxygenase and a platelet-activating factor (PAF) receptor antagonist, exhibiting IC50 values of 100 nM and 10 nM, respectively. This compound demonstrates significant anti-inflammatory activities by modulating leukotriene synthesis and PAF signaling pathways. CMI-392 is valuable for research applications focused on inflammatory diseases and related therapeutic targets.
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Synonyms: ZD 4407
AZD 4407 is a potent inhibitor of 5-lipoxygenase, an enzyme involved in the biosynthesis of leukotrienes. This compound exhibits significant anti-inflammatory properties, making it a valuable tool for research in areas such as asthma, arthritis, and other inflammatory diseases. AZD 4407 is utilized to study the modulation of leukotriene-mediated pathways in various biological contexts.
BI-0115 is a selective LOX-1 inhibitor with an IC50 of 5.4 μM, effectively blocking the cellular uptake of oxidized low-density lipoprotein (oxLDL). This compound disrupts receptor activity through the formation of dimers within the homodimeric ligand binding domain. BI-0115 is valuable for research focused on atherosclerosis and cardiovascular diseases, providing insight into the modulation of lipid metabolism and inflammatory processes.
DKI5, or (E)-N’-benzylidenehydrazinecarbothiohydrazide, is a selective inhibitor of LOX-1, with an IC50 value of 22.5 μM. This compound demonstrates potential anti-inflammatory properties by targeting the lectin-like oxidized low-density lipoprotein receptor-1 (LOX-1). DKI5 is suitable for research applications involving cardiovascular studies and the modulation of atherosclerosis-related pathways.
PXS-6302 hydrochloride is an irreversible inhibitor of lysyl oxidase (LOX) with potent inhibitory activity, exhibiting IC50 values of 3.7 μM for bovine LOX and as low as 0.3 μM for rh LOXL4. This compound demonstrates excellent skin penetration, leading to reductions in collagen deposition and noticeable improvements in scar appearance. PXS-6302 hydrochloride is primarily utilized in research focusing on fibrosis, wound healing, and tissue remodeling.
PXS-4787 hydrochloride is a selective pan-lysyl oxidase (LOX) inhibitor, effectively disrupting lysyl oxidase activity. It demonstrates potent inhibition with IC50 values of 2 μM for Bovine LOX, 3.2 μM for recombinant human LOXL1, 0.6 μM for rh LOXL2, 1.4 μM for rh LOXL3, and 0.2 μM for rh LOXL4. PXS-4787 hydrochloride has been shown to reduce the deposition and crosslinking of collagen I in human fibroblasts, making it a valuable tool for studying fibrosis and connective tissue disorders.
PXS-6302 is an irreversible inhibitor of lysyl oxidase (LOX) with a competitive profile against various isoforms, showing IC50 values of 3.7 μM for bovine LOX, 3.4 μM for recombinant human LOXL1, 0.4 μM for recombinant human LOXL2, 1.5 μM for recombinant human LOXL3, and 0.3 μM for recombinant human LOXL4. This compound demonstrates significant biological activity by reducing collagen deposition and enhancing the aesthetic appearance of scars. PXS-6302 is particularly valuable in research applications focusing on fibrosis, wound healing, and skin remodeling.
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PXS-4787 is a selective pan-lysyl oxidase (LOX) inhibitor that effectively abrogates the activity of this enzyme. It demonstrates inhibitory potency with IC50 values of 2 μM for bovine LOX, 3.2 μM for recombinant human LOXL1, 0.6 μM for recombinant human LOXL2, 1.4 μM for recombinant human LOXL3, and 0.2 μM for recombinant human LOXL4. PXS-4787 is valuable for research applications involving connective tissue remodeling, fibrosis, and other LOX-related pathologies.
5-LOX-IN-7 is a potent lipoxygenase (LOX) inhibitor that demonstrates significant inhibitory effects on LOX-mediated pathways. Its primary mechanism is to modulate inflammatory responses, making it a valuable tool for studying the underlying mechanisms of inflammatory and allergic diseases, as well as certain cancer types. This compound is suitable for research applications in evaluating the role of LOX in pathophysiology and therapeutic strategies.
Methyl 9-hydroxyoctadeca-10,12,15-trienoate is a potent inhibitor of soybean lipoxygenase (LOX), which plays a critical role in the metabolism of arachidonic acid to leukotrienes. This compound has demonstrated significant anti-inflammatory activity by effectively inhibiting TPA-induced ear edema in murine models. Methyl 9-hydroxyoctadeca-10,12,15-trienoate is valuable for research in inflammation and related signaling pathways.
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Synonyms: 9(R)-Hydroxyeicosatetraenoic acid
9(R)-HETE is an enantiomer of 9-HETE, comprising 50% of the racemic mixture (±)9-HETE. It functions as an activator of RXRγ-dependent transcription, demonstrating a 1.5-fold increase in activity at a concentration of 300 nM compared to controls. The stereochemical characterization of the (R) enantiomer is supported by chiral HPLC retention time comparisons with published data. This compound is valuable for studies investigating RXR signaling pathways and lipid metabolism.
L-699333 is a selective inhibitor of 5-lipoxygenase (5-LO), belonging to the thieno[2,3,4-cd]indole class. This compound effectively reduces the biosynthesis of 5-hydroxyeicosatetraenoic acid (5-HPETE) and leukotriene B4 (LTB4), with ICm values of 22 nM in human neutrophils and 3.8 pM in whole blood. L-699333 demonstrates anti-inflammatory and antiasthmatic properties across various animal models, including those of rat pleurisy, antigen-induced wheezing, and asthma in macaques and sheep. The compound exhibits high selectivity for 5-LO, showing less inhibition of human 15-LO and porcine 12-LO, positioning it as a valuable tool for investigating inflammatory pathways.
