12R-LOX-IN-1 (Compound 4a), with an IC50 of 28.25 µM, is an inhibitor of 12R-LOX. It suppresses the hyperproliferative condition and the ability to form colonies in Imiquimod-induced psoriatic keratinocytes, as well as reducing levels of reactive oxygen species, Ki67, IL-17A, TNF-α, and IL-6. This compound has utility in antipsoriatic research [1].

XO/COX/LOX-IN-1 is a potent inhibitor of xanthine oxidase/cyclooxygenase/lipoxygenase XO/COX/LOX. XO/COX/LOX-IN-1 can be used in the study of inflammatory, cancer and metabolic diseases.

COX-2/15-LOX-IN-1 (Compound 14) is a COX-2 and 15-lipoxygenase (15-LOX) inhibitor that acts on COX-1 (IC50: 10.65 μM), COX-2 (IC50: 0.075 μM) and 15-LOX (IC50: 2.98 μM). 25 has an anti-inflammatory effect.

9c(i472) is an inhibitor of 15-lipoxygenase-1 (15-LO-1; IC50 = 0.19 μM).1 It decreases LPS- and IFN-γ-induced NF- B activity in RAW-Blue cells when used at concentrations of 0.2, 1, and 5 μM. 9c(i472) reduces LPS- and IFN-γ-induced increases in Nos2 expression and lipid peroxidation in RAW 264.7 cells when used at a concentration of 5 μM.

Compound 105 (h15-LOX-2 inhibitor 1) is a potent inhibitor of human epithelial 15-lipoxygenase-2 (h15-LOX-2), exhibiting an IC50 of 0.34 μM [1].

COX-2/5-LOX-IN-1 (compound 3a), a benzothiophen-2-yl pyrazole carboxylic acid derivative, is a potent and dual inhibitor of COX-2 / 5-LOX. It exhibits superior analgesic and anti-inflammatory properties compared to Celecoxib and Indomethacin. COX-2/5-LOX-IN-1 displays strong inhibitory activity against COX-1, COX-2, and 5-LOX, with IC50 values of 12.13 μM, 0.4 μM, and 4.96 μM, respectively [1].

COX/5-LOX-IN-1 (compound 6b) is a potent COX/5-LOX dual inhibitor with the potential for inflammation diseases research. COX/5-LOX-IN-1 has IC50s of 1.07, 0.55, and 0.28 μM for COX-1, COX-2, and 5-LOX enzyme, respectively [1].

5-LOX-IN-1 is a 5-Lipoxygenase (5-LOX) inhibitor (IC50: 2.3 μM).5-LOX-IN-1 can be used for cancer research.

Iptacopan (LNP023) is an inhibitor with high affinity for factor B.

5-LOX inhibitor (1-(sec-Butyl)-4-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)-1H-1,2,4-triazol-5(4H)-one) is one of the impurities of itraconazole, a selective LOX-5 inhibitor.

S-2474, an inhibitor of COX-2 and 5-lipoxygenase, has anti-inflammatory and neuroprotective activities and inhibits Abeta (25 - 35) and Abeta (1 - 40) induced cell death.

A-69412 (N-1-(Fur-3-ylethyl)-N-hydroxyurea) is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase. It has the potential to treat ulcerative colitis and asthma, and possibly other inflammatory and allergic conditions.

5-amino-1-[4-(trifluoromethyl)phenyl]-1H-pyrazole-4-carbonitrile is a compound used as a molecular structural unit and is considered to be an inhibitor of enzymes such as COX-2, 5-LOX, etc., and possesses a wide range of biochemical and physiological effects including antitumor activity, anti-inflammatory effects and antioxidant activity.

1-Naphthyl 3,5-dinitrobenzoate (JMC-4) is an inhibitor of 5-LOX can be used in studies about inflammatory therapy.

(S)-Coriolic acid (13(S)-HODE) is an important intracellular signaling agent, generated by the reaction of linoleic acid with plant and mammalian lipoxygenases, and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid inhibits the adhesion of tumor cells to the vascular endothelium and down-regulates the expression of IRGpIIb/IIIa receptors at around 1 μM. (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX), which often acts as an endogenous ligand to activate PPARγ. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial damage.

KKII5 is a potent inhibitor of the lipoxygenase LOX-1 with an IC50 of 19 μM.KKII5 inhibits lipid peroxidation and enhances the ability of the active centers of some compounds to receive electrons.

MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.

HPGDS inhibitor 1 is a novel and selective inhibitor for Hematopoietic Prostaglandin D Synthase (HPGDS) with an IC50 Value of 0.7 nM.

Golocdacimab (MEDI6570) is a fully human monoclonal antibody targeting LOX-1 with potential application in type 2 diabetes research [1].

DKI5 ((E)-N'-benzylidenehydrazinecarbothiohydrazide) is a LOX-1 inhibitor with an IC50 value of 22.5 μM.DKI5 may have anti-inflammatory and antioxidant activities and has shown anti-lipid peroxidation activity in in vitro bioassays.

Phenidone (1-phenyl-3-pyrazolidinone) is a dual inhibitor of cyclooxygenases and lipoxygenases that ameliorates rat paralysis in experimental autoimmune encephalomyelitis by suppressing its target enzymes[1]. The lipoxygenase inhibitor phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[2].

sEH/FLAP-IN-1 (Compound 46A) serves as a dual inhibitor targeting both sEH and FLAP. It effectively suppresses 5-LOX product formation with an EC50 of 11 nM in SACM-stimulated PBMCs and also inhibits sEH activity (EC50: 18 nM) as well as thromboxane production. This compound is utilized in the study of inflammatory diseases [1].

Trichosanatine and squamosamide, as potential candidates as lead compounds for further study in drug development process with the PP2A- α protein. Trichosanatine can alleviate oxidized low-density lipoprotein induced endothelial cells injury via inhibiting the LOX-1/p38 MAPK pathway.

FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and COX (IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase, respectively).

Selaginellin has a neuroprotective effect against L-glutamate-induced neurotoxicity through mechanisms related to anti-oxidation and anti-apoptosis via scavenging reactive oxygen species and up-regulating the expression of klotho gene. Selaginellin shows

1. Pectolinarigenin (Pectolinaringenin) exhibits hepatoprotective activity mainly via SOD antioxidant mechanism. 2. Pectolinarigenin possesses anti-inflammatory activity and that they may inhibit eicosanoid formation in inflammatory lesions.

COX-2-IN-31 (compound 7b) is an orally active dual inhibitor targeting COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM). Additionally, it inhibits the activity of transmembrane hCA IX (Ki=48.9 nM) and hCA XII (Ki=5.8 nM). This compound demonstrates anti-inflammatory and analgesic activity [1].

Compound 29, also known as 5-LOX-IN-5, is a 5-lipoxygenase (5-LOX) inhibitor with an inhibitory concentration 50 (IC50) of 56 nM, utilized in research pertaining to neurodegenerative diseases [1].

17(S)-HpDHA, primarily produced by the 15-Lipoxygenase (LOX) isoenzymes h15-LOX-1 and h15-LOX-2 from docosahexaenoic acid (DHA), is a key regulator in epoxide synthesis through allosteric modulation. Additionally, it effectively inhibits platelet aggregation, demonstrating an EC50 of approximately 1 μM [1].

BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) pathways.

PGS-IN-1 (KME-4) is a potent inhibitor of prostaglandin synthetase (PGS, IC50: 0.28 μM) and 5-lipoxygenase (IC50: 1.05 μM).

4',5-Dihydroxyflavone is a soybean LOX-1(Ki: 102.6 μM) and yeast α-Glucosidase inhibitor (IC50: 66 μM).

Compound 5f (Antioxidant agent-13) is an antioxidant that demonstrates inhibition of DPPH and FRAP with half maximal inhibitory concentrations (IC50s) of 80.33 µM and 85.69 µM, respectively. Additionally, it inhibits the enzymes lipoxygenase (LOX) and xanthine oxidase (XO) with IC50s of 16.85 µM and 23.01 µM, respectively [1].

LOX-IN-3 dihydrochloride is an inhibitor of lysyl oxidase (LOX). LOX-IN-3 dihydrochloride inhibited bovine LOX (IC50<10 μM) and human LOXL2 (IC50<1 μM)activities.

CAY10698 is a 12-lipoxygenase inhibitor (12-LO; IC50 of 5.1 µM).

Angiotensin II human TFA, a potent vasoconstrictor within the renin/angiotensin system, plays a pivotal role in human blood pressure regulation primarily through interactions with the G-protein-coupled receptors Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). It not only prompts sympathetic nervous stimulation, aldosterone biosynthesis, and renal effects but also fosters growth in vascular smooth muscle cells and boosts collagen type I and III synthesis in fibroblasts. This action results in the thickening of the vascular wall and myocardium, alongside fibrosis. Additionally, Angiotensin II human TFA triggers apoptosis and encourages capillary formation from endothelial cells through the LOX-1 dependent redox-sensitive pathway [1] [2] [3] [4].

LOX-IN-3, an orally active inhibitor of lysyl oxidase (LOX), holds potential application in the fields of fibrosis, cancer, and angiogenesis research[1].

Angiotensin II human acetate (DRVYIHPF acetate) is a vasoconstrictor that mainly acts on the AT1 receptor.

WES-1 (Compound 8g), a carbonic anhydrase IX inhibitor (Ki: 55.9 μM), exhibits broad-spectrum antiproliferative activity against various cancer cell lines, including leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI-H460), colon cancer (HCT 116 and HCT-15), and melanoma (LOX IMVI) [1].

COX-2/15-LOX-IN-4 (compound 5i) is a dual inhibitor with IC50 values of 0.075 μM for COX-2 and 1.97 μM for 15-LOX. It inhibits LPS-induced production of pro-inflammatory cytokines (IL-6, ROS) and exhibits targeted anti-inflammatory effects [1].

COX-2-IN-28 is a potent and selective COX-2 inhibitor capable of acting on COX-2 (IC50: 0.054 μM), 15-LOX (IC50: 2.14 μM) and COX-1 (IC50: 13.21 μM).

COX-2/5-LOX-IN-3 (compound 5b) is a powerful and dual inhibitor of COX-2 and 5-LOX, with IC50 values of 45.73 μM, 5.45 μM, and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. This compound, COX-2/5-LOX-IN-3, shows promise for the investigation of inflammatory diseases [1].

PXS-4787 is a potent and selective inhibitor of lysyl oxidase (LOX) with broad-spectrum activity. It effectively suppresses lysyl oxidase activity by acting on its mechanisms. The compound displays inhibitory effects with IC50 values of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), and 0.2 μM (rh LOXL4), respectively [1].

3-Hydroxycoumarin is a natural compound, and is human 15-LOX-1 inhibitors

COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1].

COX-2/15-LOX-IN-2 is a potent inhibitor of both COX-2 and 15-LOX, demonstrating IC50 values of 0.065 μM for COX-2 and 1.86 μM for 15-LOX. Additionally, it exhibits significant antioxidant activity [1].

COX-2-IN-26 is a potent, orally active, selective COX-2 inhibitor that acts on COX-1 (IC50: 10.61 μM), COX-2 (IC50: 0.067 μM), and 15-LOX (IC50: 1.96 μM).COX-2-IN-26 is anti-inflammatory and has a gastrointestinal safety profile.

Lipoxygenase (LOX), a dioxygenase, plays a crucial role in biochemistry by catalyzing the transformation of polyunsaturated fatty acids, including linoleic and arachidonic acids, into their respective hydroperoxides [1].

YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 ( mPGES-1; IC 50 =3.4 μM) and 5-lipoxygenase ( 5-LOX; IC 50 =6.5 μM). YS121 dose-dependently reduces the production of PGE2 with EC 50 =12 μM in IL-1β-stimulated A549 cells [1].

Tepoxalin (RWJ 20485) is a 5-lipoxygenase inhibitor potentially for the treatment of asthma, osteoarthritis. Tepoxalin inhibits COX-1, COX-2, and 5-LOX. Tepoxalin is a potent inhibitor of sheep seminal vesicle cyclooxygenase (COX) (IC50 = 4.6 microM), rat basophilic leukemia cell (RBL-1) lysate COX (IC50 = 2.85 microM) and COX from intact RBL-1 cells (IC50 = 4.2 microM).