15-lo

Lonapalene (RS4317) is a 5-lipoxygenase (5-LO) inhibitor with anti-psoriasis efficacy.Lonapalene topically blocks skin inflammation.

PD146176 (NSC-168807) is an inhibitor of 15-Lipoxygenase (15-LO) , it inhibits rabbit reticulocyte 15-LO with Ki of 197 nM and IC50 of 0.54 μM. PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.

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 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.

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.

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.

15-LOX-1 inhibitor 2 (Compound 5i) is a potent inhibitor of 15-lipoxygenase-1 (15-LOX-1), with an IC50 of 1.7 μM. By inhibiting the activity of the 15-LOX-1 enzyme, it reduces the production of lipid peroxides, thereby preventing lipid peroxidation and protecting cells from RSL3-induced cell death. This compound is valuable for research into cell death mechanisms and oxidative stress-related conditions.

15-LOX-IN-1 (Compound 7c) is a 15-LOX inhibitor with an IC50 value of 1.92 μM and demonstrates anti-inflammatory properties.

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.

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-2/15-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.

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

Utreloxastat (PTC857) is a novel 15-lipoxygenase inhibitor that can be used to study amyotrophic lateral sclerosis .

BLX3887 is a highly potent and selective inhibitor of 15-lipoxygenase type 1 (15-LO-1), exhibiting an IC50 of 32 nM in cell-free enzyme assays, with marked selectivity over 15-LO-2, which it does not inhibit, as well as over 5-LO (IC50 = 472 nM) and 12-LO (IC50 = 3,310 nM). BLX3887 selectively suppresses 15-LO metabolite production in eosinophils over neutrophils at 10 μM while additionally inhibiting endocytosis and migration of human peripheral blood mononuclear cell–derived dendritic cells in vitro, highlighting its utility in inflammatory and immune cell signaling research.

mPGES-1/5-LOX-IN-1 (compound 3j) is a potent, orally active dual inhibitor of mPGES-1 and 5-LOX, with IC50 values of 0.92 and 1.89 µM, respectively. Additionally, mPGES-1/5-LOX-IN-1 exhibits anti-inflammatory properties.

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

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-2-IN-26 is a potent, orally active, selective COX-2 inhibitor, acting 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 possesses a gastrointestinal safety profile.

COX-2-IN-28 is a potent and selective COX-2 inhibitor, with IC50 values of 0.054 μM for COX-2, 2.14 μM for 15-LOX, and 13.21 μM for COX-1.

ThioLox is a competitive 15-lipoxygenase-1 (15-LOX-1) inhibitor with an IC50 value of 12 μM, demonstrating significant anti-inflammatory and neuroprotective properties, including strong protection against glutamate toxicity.