lox-2

ABT-963 is a potent and selective inhibitor of disubstituted pyridazinone cyclooxygenase-2 (LOX2) that dose-dependently reduces injury perception in a carrageenan model of nociceptive sensitization.ABT-963 is used in the study of arthritis.

Compound 10 (h15-LOX-2 inhibitor 2) suppresses h15-LOX activity, exhibiting IC 50 and K i values of 26.9 μM and 16.4 μM, respectively.

Compound 13, identified as h15-LOX-2 inhibitor 3, exhibits inhibitory activity against h15-LOX, with IC50 and Ki values of 25 μM and 15.1 μM, respectively.

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].

12R-LOX-IN-2 is an inhibitor of 12R-lipoxygenase (12R-LOX).12R-LOX-IN-2 inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and inhibits colony formation.12R-LOX-IN-2 also decreases the protein level of Ki67 and the mRNA expression of IL-17A in IMQ-induced cells. 12R-LOX-IN-2 may be useful in the study of psoriasis and other skin-associated inflammatory diseases.

COX-2 15-LOX-IN-6 (Compound 5l) is a dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.201 μM and 11.723 μM, respectively. In serum, it suppresses the expression of PGE, TNF-α, IL-6, and iNOS, and demonstrates anti-inflammatory activity in a carrageenan-induced rat edema model.

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 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.

COX-2 15-LOX-IN-1 (Compound 14) is a dual inhibitor of COX-2 and 15-lipoxygenase (15-LOX) with IC50 values of 10.65 μM for COX-1, 0.075 μM for COX-2, and 2.98 μM for 15-LOX, exhibiting an anti-inflammatory effect.

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 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].

COX-2 15-LOX-IN-3 (compound 5k) is a dual inhibitor of COX-2 and 15-LOX with inhibitory concentrations (IC50) of 0.075 μM and 1.97 μM, respectively. This compound effectively suppresses LPS-induced production of pro-inflammatory cytokines (IL-6, ROS, and NO), exhibiting targeted anti-inflammatory effects [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 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.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

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.

2,5-Di-tert-butylhydroquinone (BHQ) is an effective and selective endoplasmic reticulum Ca2+-ATPase inhibitor.

ML351 is a potent and selective inhibitor of human 15-lipoxygenase-1 (15 LOX)(IC50: 200 nM).

MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, acting by inhibiting the 5-lipoxygenase-activating protein (FLAP), and serves as a moderately potent PPARα antagonist.

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.

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).

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

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.