12-LOX Inhibitor

Onvoloxastat (ML355) is an orally active selective 12-LOX inhibitor with an IC₅₀ of 0.34 μM. Onvoloxastat inhibits platelet activation by blocking thrombin- or thromboxane A2-induced phosphorylation of Akt, PI3K and Erk1/2. At low doses (1-20 μM), it mainly acts by reducing ROS levels, while at high doses (50 μM), it functions via activating the cAMP pathway. Onvoloxastat can be used in research related to thrombosis and diabetes.

Mirificin (Puerarin apioside) is a blood-brain barrier-permeable tyrosinase inhibitor, with an IC₅₀ value of 12.66 μM against mushroom tyrosinase. Mirificin reduces the expression of ALOX12 in cardiomyocytes and alleviates hypoxia/reoxygenation-induced apoptosis. The neuroprotective effect of Mirificin depends on the activation of VEGFR2 and HSP1A1, which reduces cerebral infarct size and improves neurological function. Mirificin can be used in the research of hyperpigmentation, acute myocardial infarction and ischemic stroke.

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..

NCTT-956 is a very effective platelet 12-lipoxygenase (12-LOX) activity-specific 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.

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.