5-lo

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

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.

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

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.

Bunaprolast (U66858) is a novel and potent leukotriene B4 (LTB4) inhibitor.Bunaprolast exhibits oxidative degradation activity and inhibits lipoxygenase and TXB2 release.

CMI-392 is a dual inhibitor of 5-lipoxygenase and a receptor antagonist for platelet-activating factor (PAF) with IC50 values of 100 nM and 10 nM, respectively.

Atreleuton (ABT-761) is a potent and selective inhibitor of leukotriene formation[1][2][3]. As a reversible and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor, Atreleuton (ABT-761) exhibits selectivity.

CMI977 is a potent inhibitor of 5-Lipoxygenase (5-LO).

Docebenone is a selective and orally active inhibitor of 5-LO.

LP117 is a novel and effective inhibitor of 5-Lipoxygenase (5-LO) product synthesis (IC50: 1.1 μM).

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.

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.

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.

Compound 3, known as 5-LOX/MAOs-IN-1, acts as an inhibitor of 5-LOX/MAOs and is an effective free radical scavenger, displaying antioxidant characteristics. It has demonstrated neuroprotective effects in cell models damaged by oxidative stress and is capable of activating the neurogenesis microenvironment in adult mouse neural stem cells. This compound is utilized in research focused on neurodegenerative 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.

5-LOX/NO-IN-1 (Compound 7e) is a dual inhibitor of 5-LOX and nitric oxide release. It exhibits an IC50 value of 2.833 μM for 5-LOX and demonstrates anti-inflammatory properties.

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.

5-LOX-IN-8 is a 5-LOX inhibitor with anti-inflammatory properties. It suppresses IL-6, IL-1β, TNF-α, and IFN-γ in macrophages and reduces IL-8 secretion in SW480 cells. Additionally, 5-LOX-IN-8 decreases the disease activity index in DSS colitis models. This compound is applicable for research in inflammatory bowel disease (IBD).

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.

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.

COX-2/5-LOX-IN-5 is an inhibitor targeting both COX-2 and 5-LOX, with IC50 values of 0.84 μM and 0.46 μM, respectively. This compound binds to the active sites of COX-2 and 5-LOX, effectively inhibiting inflammation mediated by prostaglandins and leukotrienes. COX-2/5-LOX-IN-5 is applicable in the study of inflammation.