target/COX/5

Target 5 has a wide range of applications in life science related research.

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-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].

COX-1/2-IN-5 (compound 2a) functions as a dual inhibitor of COX1/2, demonstrating inhibitory concentrations (IC50) of 2.650 μM and 0.958 μM, respectively, and exhibits anticancer activity by inhibiting liver cancer HepG2 cells with an IC50 of 60.75 μM [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].

COX-2/5-LOX-IN-2 is a benzothiophen-2-ylpyrazole carboxylic acid derivative. COX-2/5-LOX-IN-2 (5b) inhibited both COX-2 and 5-LOX. The IC50s of COX-2/5-LOX-IN-2 inhibiting COX-1, COX-2 and 5-LOX were 5.40, 0.01 and 1.78 μM, respectively. COX-2/5-LOX-IN-2 showed more analgesic and anti-inflammatory activities than Celecoxib and Indomethacin.

COX/5-LO-IN-1 is a cyclooxygenase and 5-lipoxygenase (5-LO) inhibitor, and used for inflammatory and allergic disease states.

15(R)-HETE, a monohydroxy fatty acid, is synthesized from arachidonic acid via aspirin-acetylated COX-2, leading to the formation of specialized pro-resolving mediators 15(R)-lipoxin A4 and B4 through a transcellular mechanism involving 5-lipoxygenase (5-LO). Additionally, this compound is produced by the cytochrome P450 (CYP) isoform CYP2C9 and can be generated from arachidonic acid by COX-1 in human mast cells, where it accumulates due to its resistance to conversion into 15-KETE by 15-hydroxyprostaglandin dehydrogenase (15-PGDH). As an agonist of PPARβ/δ, 15(R)-HETE induces the expression of a target gene in NIH3T3 cells, demonstrating its biological significance.