5-lox-in-2

5-LOx-in-2 is a 5-lipoxygenase inhibitor (5-LOX) with an IC50 value of 0.33 μM. 5-lox-in-2 inhibits 5-LOX action IN a dose-dependent manner. 5-LOX-IN-2 can reduce the cell activity of kidney cancer cells and induce apoptosis, and can be used in cancer research.

COX-2/5-LOX-IN-2 is a benzothiophen-2-ylpyrazole carboxylic acid derivative that inhibits both COX-2 and 5-LOX. COX-2/5-LOX-IN-2 (5b) has IC50 values of 5.40, 0.01, and 1.78 μM for COX-1, COX-2, and 5-LOX, respectively, and exhibits greater analgesic and anti-inflammatory activities than Celecoxib and Indomethacin.

15-LOX-IN-2 (Compound 2a) is an orally active inhibitor of COX-2/15-LOX and a partial agonist of PPARγ. It exhibits anti-inflammatory activity by inhibiting levels of 20-HETE, IL-1β, and TNF-α in LPS-treated RAW 264.7 cells. Additionally, it significantly enhances glucose uptake without the presence of insulin and is applicable in metabolic disease research.

COX-2/15-LOX-IN-2 is a potent inhibitor of COX-2 (IC50: 0.065 μM) and 15-LOX (IC50: 1.86 μM), also demonstrating significant antioxidant activity [1].

6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.

L-Homocysteine is a biological thiol involved in various diseases and pathological conditions. It is a marker for atherosclerosis and can exacerbate intestinal inflammation in inflammatory bowel disease (IBD) by promoting the expression of 5-LOX and COX-2, making it suitable for inducing vascular endothelial inflammation models.

LOX-IN-5 tosylate (compound 22) is a selective oral inhibitor of lysyl oxidase-like 2 (LOXL2) with an IC50 of less than 300 nM, and it exhibits anti-fibrotic properties.

AChE-IN-82 (compound 49) is an acetylcholinesterase (AChE) inhibitor. It inhibits eeAChE, eqBChE, hMAO-A, hMAO-B, and BACE-1 with IC50 values of 0.072, 9.81, 14.52, 0.024, and 2.42 μM, respectively. Additionally, AChE-IN-82 inhibits COX-1, COX-2, and 5-LOX with IC50 values of 60.41, 0.187, and 0.18 μM, respectively. The compound also demonstrates strong neuroprotective effects by significantly reducing H2O2-induced oxidative stress.

COX-2/LOX-IN-1 (compound 5) is a dual inhibitor of COX-2 and LOX enzymes, exhibiting IC50 values of 0.55 μM for COX-2 and 30 μM for LOX.

hMAO-B-IN-8 (Compound 23) is an inhibitor of hMAO-B, eeAChE, COX-2, and 5-LOX, with IC50 values of 0.037 μM, 0.071 μM, 14.3 μM, and 0.59 μM, respectively. This compound is utilized in research related to Alzheimer's disease.

2-TEDC is a potent lipoxygenase (LOX) inhibitor with inhibitory effects on 5-LOX, 12-LOX, and 15-LOX with IC50 values of 0.09 μM, 0.013 μM, and 0.5 μM, respectively.2-TEDC can be used in the study of atherosclerosis.

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

COX-2/5-LOX-IN-3 (compound 5b) is a powerful 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, showing promise for the investigation of inflammatory diseases [1].

COX-2/5-LOX-IN-1 (compound 3a), a benzothiophen-2-yl pyrazole carboxylic acid derivative, is a potent dual inhibitor of COX-2 and 5-LOX, exhibiting superior analgesic and anti-inflammatory properties compared to Celecoxib and Indomethacin. It demonstrates 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-2-IN-22 is a COX-2 inhibitor (IC50: 8.6 μM) that can cross the blood-brain barrier and also exhibits inhibitory effects on AChE (IC50: 2.8 μM), BChE (IC50: 6.3 μM), β-Secretase (IC50: 15.3 μM), LOX-5 (IC50: 13.9 μM) and DPPH ( IC50: 6.8 μM) showed inhibitory effects.

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

COX-2/15-LOX-IN-5 (Compound 4f) functions as a dual inhibitor of COX-2 and 15-LOX, demonstrating both anti-inflammatory and antioxidant properties [1]. This compound effectively reduces NF-κB activation in RAW 264.7 macrophages that is induced by lipopolysaccharide.

Compound 8o (5-LOX/sEH-IN-1) is a dual inhibitor with cardioprotective properties, targeting both 5-LOX and sEH with IC50 values of 3.05 μM and 2.20 nM respectively. It also inhibits the activity of COX-2 (IC50=10.50 μM). Possessing analgesic and anti-inflammatory properties, 5-LOX/sEH-IN-1 reduces ulcerogenicity, making it a potential candidate for developing anti-inflammatory agents with fewer gastrointestinal and cardiovascular side effects.

5-O-Demethylnobiletin (Standard) is a reference standard for research and analysis in studies involving 5-O-Demethylnobiletin. 5-O-Demethylnobiletin (5-DEMETHYLNOBILETIN) is a natual product, has anti-inflammatory activity, it may act through a direct inhibition of 5-LOX, without affecting the expression of COX-2.

Psoralidin (Standard) is a reference standard for research and analysis in studies involving Psoralidin. Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally. Psoralidin possesses anticancer and chemopreventive properties.

Pectolinarigenin (Standard) is a reference standard for research and analysis in studies involving Pectolinarigenin. 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.

S-(+)-Marmesin (Standard) is a reference standard for research and analysis in studies involving S-(+)-Marmesin. S-(+)-Marmesin (marmesin) is a coumarin originally isolated from the mature bark of A. marmelos,exhibiting COX-2/5-LOX dual inhibitory activity.