2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Lipoxygenase
  5. 12-LOX Isoform

12-LOX

12-Lipoxygenase (12-LOX) catalyzes the oxygenation of arachidonic acid and other polyunsaturated fatty acids, generating bioactive lipid mediators that regulate cellular signaling and inflammation[1][2]. Mechanistically, platelet 12-LOX is activated via the collagen receptor glycoprotein VI (GPVI) and downstream src-tyrosine kinases, PI3-kinase, and Ca2+ mobilization, while PKC inhibition potentiates its activity[3]. 12-LOX exhibits isoform-specific functions distinct from 15-LOX and 5-LOX, including intrinsic hepoxilin A3 synthase activity and selective platelet oxylipin production[4][5][6]. In disease models, 12-LOX contributes to diabetes pathogenesis through modulation of β-cell inflammation and to neuroinflammation by activating NLRP3 inflammasomes[1][7][8][2]. Isoform-targeted inhibitors, such as ML351 for 12/15-LOX, reduce ischemia-induced lipid peroxidation, cytokine release, and inflammasome activation, highlighting its experimental relevance[7][8]. Additionally, dietary polyunsaturated fatty acids, including dihomo-γ-linolenic acid, serve as substrates for 12-LOX-mediated generation of anti-thrombotic oxylipins, providing mechanistic insight into vascular protection[5]. Comparative studies indicate that 12-LOX activity is distinct in substrate specificity, signaling regulation, and physiological outcomes from related LOX isoforms, facilitating selective pharmacological intervention and functional studies in cellular and animal models[9][4][5][7].

References:

12-LOX Related Products (6):

Cat. No. Product Name Effect Purity
  • HY-12341
    ML355
    		Inhibitor 98.11%
    ML355 is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 0.34 μM, shows excellent selectivity over related lipoxygenases and cyclooxygenases, and possesses favorable ADME properties.
  • HY-W089800
    trans-2-Nonenal
    		Inhibitor 98.99%
    trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc..
  • HY-139055
    NCTT-956
    		Inhibitor
    NCTT-956 is a very effective platelet 12-lipoxygenase (12-LOX) activity-specific inhibitor.
  • HY-182696
    CGS 24891
    		Inhibitor
    CGS 24891 is an orally active 5-lipoxygenase (5-LO) inhibitor, with an IC50 value of 0.051 μM in guinea pigs and 0.11 μM in dogs. CGS 24891 inhibits the production of 5-hydroxyeicosatetraenoic acid (5-HETE) and leukotriene B4 (LTB4) from arachidonic acid. CGS 24891 weakly inhibits 12-lipoxygenase (12-LO) with an IC50 of 0.41 μM. CGS 24891 is applicable to research on inflammation and allergic reactions.
  • HY-175970
    MLS000099089
    		Inhibitor
    MLS000099089 is a 12/15-lipoxygenase (12/15-LOX) inhibitor with IC50 values of 3.4 μM and 10 μM for human and mice 12/15-LOX, respectively. MLS000099089 displays higher selectivity for 12/15-LOX over 5-LOX and COX-2. MLS000099089 can be used for the study of stroke.
  • HY-N16694
    6,7-Dehydroferruginol
    		Control
    6,7-Dehydroferruginol is a diterpenoid compound that can be isolated from the dichloromethane extract of Juniperus communis wood. At a concentration of 100 μg/mL, 6,7-Dehydroferruginol showed no inhibitory activity against 12(S)-LOX and did not inhibit the production of 12(S)-HETE.