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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.
5-LOX-IN-6 is a potent and selective inhibitor of 5-lipoxygenase (5-LO), exhibiting reversible inhibition. It effectively reduces 5-LO activity in human neutrophils and recombinant human 5-LO with IC50 values of 0.23 µM and 0.086 µM, respectively. By inhibiting leukotriene biosynthesis, 5-LOX-IN-6 serves as a valuable tool in the study of inflammatory and allergic disorders.
E 6080 is a specific inhibitor of 5-lipoxygenase (5-LOX), exhibiting an IC50 of 0.2 μM in rat basophilic leukemia cells. This compound effectively reduces leukotriene release, which is critical in the inflammatory response. E 6080 has demonstrated the ability to inhibit bronchospasm induced by antigen inhalation in sensitized guinea pigs, making it a valuable tool for asthma research and related inflammatory conditions.
A63162 is a selective inhibitor of 5-lipoxygenase (5-LOX), a key enzyme in the biosynthesis of leukotrienes. This compound effectively inhibits both mitogen-induced proliferation of horse mononuclear cells and the synthesis of leukotriene LTB4 in response to Calcimycin at equivalent concentrations. A63162 is useful in research focused on chronic obstructive pulmonary disease, arthritis, and inflammatory bowel disease, offering insights into inflammatory pathways and potential therapeutic interventions.
Canniprene is a potent inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase/microsomal prostaglandin E2 synthase (PGE2), with IC50 values of 0.4 μM and 10 μM, respectively. Derived from Cannabis sativa, Canniprene modifies the biosynthesis of inflammatory eicosanoids and prostaglandins, making it a valuable tool for researching inflammation and related pathways. Its unique mechanism of action positions Canniprene as a potential candidate for studying inflammatory diseases and therapeutic interventions targeting lipid mediators.
CV-6504 is a dual inhibitor targeting thromboxane A2 (TXA2) synthase and 5-lipoxygenase. This compound demonstrates significant biological activity by scavenging reactive oxygen species (ROS) and exhibiting antitumor properties. CV-6504 is applicable in research focused on cancer, inflammation, and cardiovascular diseases, providing valuable insights into therapeutic strategies and molecular mechanisms.
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E 3040 is an orally active inhibitor of both 5-lipoxygenase and thromboxane synthase, key enzymes involved in inflammatory processes. This dual inhibition provides significant anti-inflammatory activity, making E 3040 a valuable reagent for research into inflammatory diseases and related pathways. Its unique mechanism can facilitate studies on the modulation of leukotrienes and thromboxanes in various biological contexts.
E-6700 is a potent inhibitor of 5-lipoxygenase (5-LO) and thromboxane A2 (TXA2) synthetase, with IC50 values of 16.3 μM and 0.026 μM, respectively. This compound effectively inhibits the production of leukotriene B4 (LTB4) and thromboxane B2 (TXB2). E-6700 is suitable for applications in anti-inflammatory research, providing a valuable tool for investigating pathways associated with inflammatory responses.
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Phenethyl ferulate is a potent inhibitor of cyclooxygenase (COX) and 5-lipoxygenase (5-LOX), displaying IC50 values of 4.35 μM and 5.75 μM, respectively. This compound exhibits significant anti-inflammatory properties, making it a valuable tool for research into inflammation-related pathways. Its ability to modulate these key enzymes positions it as a promising candidate for studies focused on inflammatory diseases and therapeutic interventions.
FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and cyclooxygenase (COX), exhibiting IC50 values of 3.5 μM and 3.1 μM, respectively, in RBL-1 cells. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research into inflammatory pathways and related diseases. Its dual inhibition of leukotriene and prostaglandin synthesis positions FPL 62064 as a pertinent reagent for studies focusing on inflammation and related therapeutic interventions.
BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) enzymes, exhibiting an IC50 of 5 μM for 5-LO. It also demonstrates inhibitory activity against COX-1 and COX-2, with IC50 values of 0.65 and 1.2 μg/mL, respectively. This compound is valuable for research applications involving inflammation and other related pathways. Its ability to concurrently inhibit key lipid mediators makes BW 755C a useful tool in studies focused on arachidonic acid metabolism and signaling pathways.
Synonyms: NE-11740
Tebufelone is a selective dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LO). It exhibits significant anti-inflammatory, analgesic, and antipyretic properties, making it useful for research into inflammatory pathways. This compound is valuable for studying the roles of COX-2 and 5-LO in various biological processes and assessing novel therapeutic strategies for inflammatory diseases.
ER-34122 is a dual inhibitor of cyclooxygenase (COX) and 5-lipoxygenase (5-LO). This compound exhibits significant anti-inflammatory activity, making it valuable for research into inflammation-related pathways. ER-34122 is particularly relevant for studies investigating the interplay between COX and 5-LO pathways in various disease models and therapeutic contexts.
COX-2/5-LOX-IN-2 is a potent dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). This benzothiophen-2-yl pyrazole carboxylic acid derivative demonstrates significant analgesic and anti-inflammatory properties, exhibiting COX-2 inhibitory activity with an IC50 of 0.01 μM and 5-LOX inhibitory activity with an IC50 of 1.78 μM. COX-2/5-LOX-IN-2 is a valuable tool for research applications aimed at understanding and modulating inflammatory pathways.
P-8977 is a potent dual inhibitor of cyclooxygenase (CO) and 5-lipoxygenase (5-LO) with an IC50 of 0.01 µM and 0.53 µM, respectively. This compound exhibits significant anti-inflammatory activity, demonstrated by its ability to reduce ear edema. P-8977 is valuable for research focused on inflammatory skin conditions and their underlying biochemical mechanisms.
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COX-2/15-LOX-IN-5 is a potent dual inhibitor of cyclooxygenase-2 (COX-2) and 15-lipoxygenase (15-LOX). This compound effectively attenuates lipopolysaccharide-induced NF-κB activation in RAW 264.7 macrophages, highlighting its role in modulating inflammatory responses. COX-2/15-LOX-IN-5 exhibits significant anti-inflammatory and antioxidant properties, making it a valuable tool for research into inflammatory diseases and other related biological processes.
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SKF-105809 is a dual inhibitor of lipoxygenase and cyclooxygenase (COX), targeting key enzymes involved in the inflammatory pathway. This compound demonstrates a significant reduction in edema and inflammatory cell infiltration in murine models of ear, paw, and peritoneal inflammation. Additionally, SKF-105809 reduces the production of acute-phase reactive proteins in models of arthritis and exhibits analgesic effects in abdominal contraction assays while preventing ulceration. Its applications extend to the study of inflammatory and immune system disorders, including peritonitis and arthritis.
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COX-2/15-LOX-IN-1 is a dual inhibitor of cyclooxygenase-2 (COX-2) and 15-lipoxygenase (15-LOX), exhibiting IC50 values of 10.65 μM for COX-1, 0.075 μM for COX-2, and 2.98 μM for 15-LOX. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research into inflammatory pathways and related diseases. Its ability to modulate key enzymes involved in arachidonic acid metabolism positions COX-2/15-LOX-IN-1 as a promising candidate for therapeutic investigation in inflammatory conditions.
Atractylochromene is a dual inhibitor targeting 5-lipoxygenase (5-LOX) and cyclooxygenase-1 (COX-1), exhibiting IC50 values of 0.6 μM and 3.3 μM, respectively. This compound serves as a valuable tool in research related to inflammatory pathways and can facilitate the study of related conditions influenced by leukotrienes and prostaglandins. Its inhibitory effects position Atractylochromene as a potential candidate for therapeutic exploration in inflammatory diseases.
XO/COX/LOX-IN-1 is a potent inhibitor of xanthine oxidase, cyclooxygenases, and lipoxygenases. This compound exhibits significant anti-inflammatory activity, making it valuable for research in inflammation, cancer, and metabolic diseases. Its multifaceted inhibition profile positions XO/COX/LOX-IN-1 as a critical tool for exploring pathways involved in these pathological conditions.
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COX-2/5-LOX-IN-4 is a potent dual inhibitor targeting both cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX), with IC50 values of 0.05 μM and 0.003 μM, respectively. By disrupting the arachidonic acid metabolism pathway, this compound effectively decreases the synthesis of prostaglandins and leukotrienes, leading to reduced inflammatory responses. In vivo studies using a rat ear edema model demonstrate its substantial anti-inflammatory activity, with intravenous doses resulting in up to 44% reduction in edema. COX-2/5-LOX-IN-4 is an important tool for investigating the mechanisms underlying inflammatory diseases.
COX-2/15-LOX-IN-7 is a selective dual inhibitor targeting cyclooxygenase-2 (COX-2) and 15-lipoxygenase (15-LOX) with IC50 values of 0.022 and 1.19 μM, respectively. It also demonstrates inhibition of COX-1 with an IC50 of 28.081 μM. This compound exhibits low cytotoxicity in human colorectal cancer cell lines (HT-29 and HCT116) with IC50 values exceeding 100 μM, and shows a non-ulcerogenic profile. COX-2/15-LOX-IN-7 is valuable for cancer research applications, facilitating the study of inflammatory pathways and therapeutic interventions.
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CI-986 is a dual inhibitor of cyclooxygenase (COX) and 5-lipoxygenase (5-LOX), effectively preventing coronary vasoconstriction and the excessive production of leukotrienes, including LTB4 and LTC4. This compound exhibits notable anti-inflammatory and analgesic properties, making it a valuable tool for research into inflammation and cardiovascular diseases, including conditions like arthritis. CI-986's unique mechanism positions it as an important reagent in studies focused on the modulation of inflammatory pathways and vascular health.
COX-2/5-LOX-IN-1 is a dual inhibitor targeting cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX), represented as a benzothiophen-2-yl pyrazole carboxylic acid derivative. This compound exhibits significant analgesic and anti-inflammatory properties, demonstrating enhanced efficacy compared to traditional nonsteroidal anti-inflammatory drugs. COX-2/5-LOX-IN-1 displays potent inhibition of COX-1, COX-2, and 5-LOX, with IC50 values of 12.13, 0.4, and 4.96 μM, respectively, making it a valuable tool for research in pain and inflammation pathways.
Speranskoside is a dual inhibitor of cyclooxygenase-2 (COX-2) and lipoxygenase-15 (5-LOX), exhibiting an IC50 of 2.62 μg/mL for COX-2 and 5.51 μg/mL for 5-LOX. This compound demonstrates significant anti-inflammatory activity, making it valuable for the investigation of gastric ulcers and related disorders. Its unique mechanism of action provides a foundational tool for research into inflammatory pathways and therapeutic interventions.
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COX-2/5-LOX-IN-3 is a potent dual inhibitor of cyclooxygenase-2 (COX-2) and lipoxygenase (5-LOX), exhibiting IC50 values of 45.73 µM for COX-1, 5.45 µM for COX-2, and 4.33 µM for 5-LOX. This compound is valuable for studying inflammatory diseases, as it effectively modulates the associated biochemical pathways. Its dual inhibition may provide insights into the complex roles of COX-2 and 5-LOX in mediating inflammatory responses.
