Lipoxygenase Inhibitor

SB 203580 sulfone is an analog of p38 MAP kinase inhibitor SB 203580. SB 203580 sulfone inhibits the IL-1 production (IC₅₀ of 0.2 μM in monocytes) and binds competitively with CSAID binding proteins (CSBP), inhibits it mediated stress response signaling with an IC₅₀ of 0.03 μM. SB 203580 sulfone inhibits 5-LO with an IC₅₀ value of 24 µM. SB 203580 sulfone can be used in the research of inflammatory diseases.

Kukoamine A, a spermine alkaloid, is an orally active and brain-penetrant component found in the root barks of Lycium chinense (L. chinense) Miller. Kukoamine A inhibits purified Crithidia fasciculata trypanothione reductase and soybean lipoxygenase, activates μ-opioid receptor. Kukoamine A can inhibt cancer cell proliferation, migration and invasion, cause G0/G1 phase cell cycle arrest and induce apoptosis. Kukoamine A exerts neuroprotective effect and can induce autophagy . Kukoamine A inhibits LPS (HY-D1056)-induced NO, ROS, PGE₂, TNF-α, IL-1β, IL-6 production and COX-2 activity. Kukoamine A reverses palmitic acid-induced insulin resistance, lipid accumulation, and oxidative stress via downregulation of Srebp-1c. Kukoamine A can be used for the research of cancer, infection, inflammation, metabolic and neurological disease, such as glioblastoma and Parkinson's disease.

β-Boswellic acid is isolated from the gum resin of Boswellia serrata with anticancer, antioxidant activity, anti-inflammatory activity and anti-arthritic pain.β-Boswellic acid is an orally active nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation. β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells with IC₅₀ values ranging from 0.6 to 7.1 μM. β-Boswellic acid is promising for research of diabetes, inflammatory and arthritic diseases.

11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.

Stearidonic acid (6Z,9Z,12Z,15Z-Octadecatetraenoic acid) is an orally active polyunsaturated fatty acid found in blackcurrant seed oil. Stearidonic acid can inhibit 5-lipoxygenase and reduce leukotriene and 5-HETE synthesis. Stearidonic acid can increase the content of eicosapentaenoic acid (EPA) in red blood cells. Stearidonic acid can be used for the research of metabolic disease.

Zileuton sodium (A 64077 sodium) is a potent and selective inhibitor of 5-lipoxygenase, exhibiting inflammatory activities.

Benoxaprofen (LRCL 3794) is a nonsteroidal anti-inflammatory agent that blocks the biosynthesis of inflammatory mediators such as leukotrienes and prostaglandins by inhibiting 5-LOX, PGH2 synthase and cytochrome P-450. Benoxaprofen exhibits significant toxicity: it not only alters cellular redox status, uncouples oxidative phosphorylation and disrupts calcium ion homeostasis, but also causes liver injury through the formation of covalent adducts between its active metabolites and hepatic proteins. Benoxaprofen shows strong phototoxicity under ultraviolet irradiation, and induces erythrocyte lysis, mast cell degranulation and histamine release. Benoxaprofen is widely used in studies of urticaria and related phototoxic mechanisms.

15-LOX-1 inhibitor 1 is a potent inhibitor of 15-LOX-1 (15-lipoxygenase-1) with an IC₅₀ value of 0.19 μM. 15-LOX-1 inhibitor 1 protects macrophages from lipopolysaccharide-induced cytotoxicity. 15-LOX-1 inhibitor 1 inhibits NO formation and lipid peroxidation.

Triphenylphosphinechlorogold (Chloro(triphenylphosphine)gold(I)) is a gold complex, Apoptosis inducer, and catalyst. Triphenylphosphinechlorogold exhibits high LOX inhibitory activity. Triphenylphosphinechlorogold induces cell cycle arrest and apoptosis. Triphenylphosphinechlorogold catalyzes the peroxidation of linoleic acid. A weak interaction exists between Triphenylphosphinechlorogold and DNA. Triphenylphosphinechlorogold displays antiproliferative activity against breast cancer cells.

Cirsiliol is a potent and selective 5-lipoxygenase inhibitor and a competitive low affinity benzodiazepine receptor ligand.

Caffeic acid (Standard) is the analytical standard of Caffeic acid. This product is intended for research and analytical applications. Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO).

4',5-Dihydroxyflavone (Compound 2c; Compound B3) is a type of flavonoid compound. 4',5-Dihydroxyflavone can inhibit various oxidases and its IC₅₀ values for collagenase A (ColA) and α-glucosidase are less than 1 μM and 66 μM respectively; for soybean lipoxygenase-1 (LOX-1), its K_i value is 102.6 μM. 4',5-Dihydroxyflavone can be used in studies on anti-toxicity and anti-diabetes.

ALOX15-IN-1 (compound 8b) is a potent inhibitor of the linoleate oxygenase activity of rabbit and human ALOX15 with _IC50s of 0.04 and 2.06 μM for ALOX15 0rthologs linoleic acid (LA) and arachidonic acid (AA), respectively.

Tenidap (CP-66248) is an orally active dual inhibitor of 5-LOX and COX with anti-inflammatory and immunomodulatory properties. Tenidap downregulates the expression of IL-1 receptors in chondrocytes, reduces the release of pro-inflammatory cytokines such as IL-1, IL-6 and TNF-α, and inhibits MMP production and cartilage degradation. Tenidap also blocks bone resorption and leukocyte adhesion to vascular endothelium, interferes with ion and pH changes associated with mouse sperm capacitation, and selectively enhances the activity of hKir2.3 channels (EC₅₀=1.3 μM). Tenidap is applicable to research related to rheumatoid arthritis.

Tepoxalin is an orally active dual inhibitor of Cyclooxygenase/Lipoxygenase, with IC₅₀ values of 4.6 μM (sheep cyclooxygenase), 2.85 μM (rat cyclooxygenase), 0.15 μM (rat 5-lipoxygenase), and 3.0 μM (h12-lipoxygenase), respectively. Tepoxalin inhibits ROS production and NF-κB activation. Tepoxalin suppresses the production of thromboxane B₂, leukotriene B₄, prostaglandins and cytokines, and blocks platelet aggregation. Tepoxalin exhibits potent anti-inflammatory activity in rats with adjuvant-induced arthritis. Tepoxalin possesses analgesic activity. Tepoxalin shows no ulcerogenic activity within the anti-inflammatory dose range. Tepoxalin can be used in studies related to adjuvant-induced arthritis, skin inflammation and Alzheimer's disease.

ALOX15-IN-2 (compound 8a) is a potent inhibitor of the linoleate oxygenase activity of rabbit and human ALOX15 with _IC50s of 1.55 and 2.79 μM for ALOX15 0rthologs linoleic acid (LA) and arachidonic acid (AA), respectively.

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.

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.

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.

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.