Lipoxygenase Inhibitor

Umbelliprenin, a prenylated coumarin, is an antioxidant with anticancer, anti-inflammatory and immunomodulatory effects. Umbelliprenin inhibits lipoxygenase managing the inflammation pathways. In inflammatory macrophages, Umbelliprenin suppresses nitric oxide production as well as inducible nitric oxide synthase (NO synthase).

3-Hydroxycoumarin is an inhibitor of tyrosinase and lipoxygenase with an IC₅₀ for recombinant human tyrosinase (rHT) of 26 μM, and a K_i of 3.39 μM; its IC₅₀ for LOX is 9.5 μM. 3-Hydroxycoumarin has DPPH free radical scavenging activity (IC₅₀ = 31.2 μM). 3-Hydroxycoumarin has photoprotective effects on sea urchin zygotes and embryos.

Picrinine, an akuammiline alkaloid, is isolated from the leaves of Alstonia scholaris. Picrinine exhibits anti-inflammatory activity through inhibition of the 5-lipoxygenase enzyme.

Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation. Atreleuton is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Texasin is a natural product that can be isolated from Baptisia australis.

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..

Canniprene, an isoprenylated bibenzyl unique to Cannabis sativa, is a potent inhibitor of 5-lipoxygenase (5-LO) activity (IC₅₀=0.4 μM) and cyclooxygenase/microsomal prostaglandin E2 synthase (PGE₂; IC₅₀=10 μM). Canniprene inhibits the production of inflammatory eicosanoids and affects the generation of prostaglandins.

4-MMPB is a selective inhibitor of 15-lipoxygenase, with an IC₅₀ of 18 μM. 4-MMPB has IC₅₀s of 19.5 μM and 19.1 μM for soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (15-LOX-1), respectively. 4-MMPB has potential for the research of prostate cancer.

YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC₅₀ = 3.4 μM) and 5-lipoxygenase (5-LOX; IC₅₀ = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (K_D = 10-14 μM). YS121 dose-dependently reduces PGE₂ production with an EC₅₀ of 12 μM in IL-1β-stimulated A549 cells. YS121 (compound 9) activates PPAR-α and -γ (EC₅₀ = 1 and 3.6 μM, respectively). YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research.

CAY10698 (compound 1) is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC₅₀ of 5.1 μM. CAY10698 is inactive against 5-LOX, 15-LOX-1, 15-LOX-2 and COX-1/2.

BW 755C is a 5-lipoxygenase (5-LO) inhibitor with an IC₅₀ of 5 μM. BW 755C also inhibits cyclooxygenase (COX) with IC₅₀s of 0.65 and 1.2 μg/mL against COX-1 and COX-2, respectively.

REV 5901 is a competitive and orally active antagonist of leukotriene receptor, with a K_i of 0.7 μM. REV 5901 is also a 5-lipoxygenase inhibitor. REV 5901 can be used for the research of asthma in which leukotriene release be involved. REV 5901 can be used for the study of colon carcinoma.

Damnacanthol is a natural product that can be isolated from Damnacanthus major. Damnacanthol has anti-15-lipoxygenase activity and can inhibit nitric oxide production in LPS-activated macrophages RAW 264.7 cells.

Nordihydroguaiaretic acid (Standard) is the analytical standard of Nordihydroguaiaretic acid. This product is intended for research and analytical applications. Nordihydroguaiaretic acid is a 5-lipoxygenase (5LOX) (IC₅₀=8 μM) and tyrosine kinase inhibitor.

(±)15-HEDE is a racemic mixture of the monohydroxy fatty acids 15(R)-HEDE and 15(S)-HEDE. 15-HEDE is formed from eicosadienoic acid in macrophages. It inhibits 5-lipoxygenase (5-LO; IC₅₀=35 μM).

12R-LOX-IN-2 (compound 7b) is an inhibitor of 12R-lipoxygenase (12R-LOX). 12R-LOX-IN-2 inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and suppresses colony formation. 12R-LOX-IN-2 also reduced the protein level of Ki67 and the mRNA expression of IL-17A in IMQ-induced cells. 12R-LOX-IN-2 can be used in research into psoriasis and other skin-related inflammatory diseases.

3-Hydroxycoumarin (Standard) is the analytical standard of 3-Hydroxycoumarin. This product is intended for research and analytical applications. 3-hydroxycoumarin is a potent and redox inhibitor of human 15-LOX-1. 3-hydroxycoumarin is recently demonstrated to protect sea urchin reproductive cells against ultraviolet B damage.

6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-A receptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes.

Tebufelone (NE-11740), a nonsteroidal anti-inflammatory drug (NSAID), is a selective dual COX-2/5-lipoxygenase inhibitor. Tebufelone displays potent anti-inflammatory, analgesic and anti-pyretic properties.

CNB-001 is a potent and orally active 5-lipoxygenase (5-LOX) inhibitor. CNB-001 can decreases 5-LOX expression and increase proteasome activity. CNB-001 can inhibit accumulation of soluble Amyloid-β and ubiquitinated aggregated proteins. CNB-001 can inhibit apoptosis, ROS production and stabilize mitochondrial membrane potential. CNB-001 can reduce insulin resistance and increase glucose uptake. CNB-001 also exhibits anti-ischemic, anti-inflammatory effects. CNB-001 can be used for the researches of inflammation, neurological and metabolic disease, such as Alzheimer's disease, stroke and diabetes.