Lipoxygenase

Efletirizine (UCB-28754), a histamine blocker and 5-LO inhibitor, aids in topical allergy treatment.

DKI5, a LOX-1 inhibitor with 22.5 μM IC50, may exhibit anti-inflammatory, antioxidant, and anti-lipid peroxidation effects in vitro.

(-)-Bornyl ferulate is a dual inhibitor of 5-lipoxygenase and cyclooxygenase (COX), exhibiting half-maximal inhibitory concentrations (IC50s) of 10.4 μM for 5-

CJ-13,610 is an orally active and nonredox-type inhibitor of 5-lipoxygenase (5-LOX). CJ-13,610 inhibits the biosynthesis of leukotriene B4 and regulates the expression of IL-6 mRNA in macrophages.

ER-34122, a novel orally available dual 5-lipoxygenase/cyclooxygenase inhibitor with potent anti-inflammatory activity.

Pectolinarigenin has hepatoprotective and anti-inflammatory properties, acting through SOD and inhibiting eicosanoids.

Linetastine (TMK-688) inhibits 5-LOX, blocks leukotrienes, counters histamine; researched for asthma, atherosclerosis, ulcers.

Malotilate (Kantec) is a medicine used for the therapy of liver cirrhosis.

BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) pathways.

Indirubin-3'-monoxime (Indirubin-3'-oxime) is a potent inhibitor of GSK3β (IC50: 22 nM) and also inhibits CDKs ( (IC50s: 100/180/250 nM for Cdk5/p35, Cdk1/

ABT-963: COX-2 inhibitor for osteoarthritis/pain with high selectivity, potency, and gastric safety.

Terameprocol (EM-1421), a synthetic NDGA derivative, shows potent anti-HIV, antiangiogenic, and anticancer properties.

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

Applications 1,1-Bis(hydroxymethyl)cyclopropane is used in the synthesis of morphine alkaloids. It also serves as an inhibitor of 5-lipoxygenase. References Evans, D.A. et al.: Tetrahedron Lett., 23, 285 (1982); Arai, Y. et al.: J. Med. Chem., 26, 72 (1983);

5-LOX inhibitor (1-(sec-Butyl)-4-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)-1H-1,2,4-triazol-5(4H)-one) is an itraconazole impurity, a LOX-5 inhibitor.

12R-LOX-IN-2 is a 12R-LOX inhibitor that inhibits the hyperproliferation of psoriatic cells and can be used in the study of psoriasis and other skin diseases.

Applications Benzo[b]thien-2-yl ketone is an impurity of Zileuton (Z420000), an inhibitor of 5-lipoxygenase that is used to treat patients with asthma. Benzo[b]thien-2-yl ketone is used as a reagent to synthesize Bis(1H-2-indolyl)methanone, compounds that inhibit the activity of growth factor receptor kinase. Benzo[b]thien-2-yl ketone is also used as a reagent to prepare annulated oligothiophenes, compounds that are used in organic light-emitting devides (OLEDs). References Israel, E., et al.: JAMA, 275, 931 (1996); Mahboobi, S., et al.: J. Med. Chem., 45, 1002 (2002); Mitschke, U. & Bäuerle, P.: J. Chem. Soc. Perk. Trans., 1, 740 (2001); Nenajdenko, V., et al.: Russ. Chem. Bull., 61, 1456 (2012)

15-Lipoxygenase Inhibitor 1 is a selective inhibitor of 15-lipoxygenase, with an IC50 of 18 μM.

Applications N-Dehydroxyzileuton is a pharmacologically inactive metabolite of Zileuton (Z420000), an inhibitor of 5-lipoxygenase that is used to treat patients with asthma. References Awni, W., et al.: Clin. Pharm., 29, 62 (1995); Machinist, J., et al.: Clin. Pharm., 29, 34 (1995); Remko, M., et al.: Phys. Chem. Chem. Phys., 2, 2511 (2000);

β-Boswellic acid (Beta-boswellic acid) and its derivatives (the major constituents of Boswellin) have anti-carcinogenic, anti-tumor, and anti-hyperlipidemic