Lipoxygenase

BI-0115 inhibits LOX-1, preventing oxLDL uptake by triggering receptor inhibition and dimer formation.

Applications p-Hexylresorcinol shows antiimnflammatory activity acting on the human 5-LO (5-Lipoxygenase) proinflammatory enzyme Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Filosa, R. et al.: Eur. j. Med. Chem., 67, 269 (2013);

LOX-IN-3 dihydrochloride is an inhibitor of lysyl oxidase (LOX).

CBS-1114 HCl: 5-lipoxygenase inhibitor, anti-inflammatory, improves heart function, reduces heart's fat.

Applications 2,4-Dichlorobenzoyl Chloride is a reactant used in the synthesis of aroyl(sulfamoylphenyl)thiourea derivatives as 15-lipoxygenase inhibitors. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Mahdavi, M., et. al.: Eur. J. Med. Chem., 82, 308 (2014)

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

1-Naphthyl 3,5-dinitrobenzoate (JMC-4) is an inhibitor of 5-LOX can be used in studies about inflammatory therapy.

Applications Nordihydro Guaiaretic Acid is a lipoxygenase inhibitor; polyphenol-bearing o-dihydroxy (catechol) structure. Inhibitor of broad bean lipoxygenase. The oxidation product from Resveratrol (R150000) showed a high inhibitory activity, whereas Resveratrol itself had no activity and its oxidation efficiency was low. References Brash, A., et al.: J. Biol. Chem., 274, 23679 (1999), Fujimoto, A., et al.: Bioorg. Med. Chem. Lett., 20, 7393 (2010), Ridolfi, M., et al.: J. Agric. Food Chem., 50, 835 (2002),

Applications MK-886 is a potent and selective inhibitor of FLAP and Cox-1. References Gillard, J., et al.: Can. J. Physiol. Pharmacol., 67, 456-464 (1989);

4',5-Dihydroxyflavone is a soybean LOX-1(Ki: 102.6 μM) and yeast α-Glucosidase inhibitor (IC50: 66 μM).

RWJ 63556 is an orally active inhibitor of COX-2 selective/5-lipoxygenase, shows anti-inflammatory activities.

Caffeic Acid is an orally bioavailable, hydroxycinnamic acid derivative and polyphenol, with potential anti-oxidant, anti-inflammatory, and antineoplastic

Applications Dimethyl (2-Oxoheptyl)phosphonate is a useful synthetic intermediate, and is used as a reagent to synthesize Caffeic acid (C080000) derivatives, which function as 5-lipoxygenase, 12-lipoxygenase, and prostaglandin synthase inhibitors. References Sugiura, M., et al.: Chem. Pharm. Bull., 37, 1039 (1989)

E 6080 HCl is a 5-lipoxygenase inhibitor and can be used to study bronchial diseases.

U-73122 (U73122) , an effective PLC inhibitor, reduces agonist-induced Ca2+ increases in platelets and PMN.

COX-2/15-LOX-IN-2 is a potent inhibitor of both COX-2 and 15-LOX, demonstrating IC50 values of 0.065 μM for COX-2 and 1.86 μM for 15-LOX.

Chebulagic acid, isolated from the Terminalia chebula Retz, is a COX-LOX dual inhibitor.

Setileuton (MK0633) is a specific 5-LOX inhibitor and can be used in research on asthma and atherosclerosis.

Oleoyl coenzyme A lithium (Oleoyl-CoA lithium) is a thioester of oleic acid and coenzyme A, acting as an allosteric inhibitor of h15-LOX-2.

3-Hydroxycoumarin is a natural compound, and is human 15-LOX-1 inhibitors

Butibufen (FF-106) is a non-steroidal anti-inflammatory compound and LOX inhibitor with analgesic and antipyretic activity for the study of rheumatic diseases.

Applications The principal constitutents of frankincense (olibanum). A specific, nonredox inhibitor of 5-lipoxygenase used to treat inflammation. References Safayhi, H. et al.: J. Pharmacol. Exp. Therap., 261, 1143 (1992); Siemoneit, U., et al.: Eur. J. Pharmacol., 606, 246 (2009); Cao, H. et al.: Pharamacol. Res., 61, 519 (2010);

PF-4191834: Non-iron, non-redox 5-LOX inhibitor, IC50 = 229 nM, 300x selective over 12/15-LOX, inactive on COX enzymes.

Linoleyl alcohol (CIS,CIS-9,12-OCTADECADIENOL), fatty alcohol, is a structural analog of Linoleic acid with no a-carboxyl group[1].

ML355, a specific, effective 12-Lipoxygenase(12-LOX) inhibitors(IC50=0.34 μM), possess favorable ADME properties.

S-(+)-Marmesin (marmesin) is a coumarin originally isolated from the mature bark of A. marmelos,exhibiting COX-2/5-LOX dual inhibitory activity.

Applications Ketoconazole-d3 is the labeled analogue of Ketoconazole (K186000), which inhibits cytochrome P-450 dependent steps in the biosynthesis of steroid hormones in vivo. Antimetastatic and antineoplastic activity. Orally active 5-lipoxygenase and thromboxane synthase inhibitor. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Lambert, A., et al.: Biochem. Pharmacol., 35, 3999 (1986); Van Wauwe, J.P. and Janssen, P.A.J., J. Med. Chem., 32, 2231 (1989); Nardone, P.A., et al.: . Surg. Res., 44, 425 (1988); Tucker, W.F.G., et al.: Br. Med. J., 293, 882 (1986)

Ferroleuton is a selective competitive inhibitor of 5-lipoxygenase with an IC50 of 0.21 μM. It demonstrates antioxidant properties, clearing 86% of DPPH at 50 μM and exhibiting activities in ABTS (EC50 = 19.42 μM) and FRAP (EC50 = 3.32 μM) assays.

AZD 4407 is a potent inhibitor of 5-lipoxygenase.

Masoprocol (meso-Nordihydroguaiaretic acid) is a LOX inhibitor with anticancer and antihyperglycemic activity.

Tepoxalin (RWJ 20485), potential asthma and osteoarthritis drug, inhibits COX-1, COX-2, and 5-LOX with low IC50 values.

5-O-Demethylnobiletin is a natural anti-inflammatory that inhibits 5-LOX without altering COX-2 expression.

CJ-13,610 hydrochloride is an orally active nonredox-type inhibitor of 5-LOX and can be used in studies about the prevention of untoward pathophysiological

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

Diethylcarbamazine citrate treats filariasis, targeting W. bancrofti and L. loa by inhibiting arachidonic acid in microfilaria.

Applications An inhibitor of 5-lipoxygenase, the initial enzyme in the biosynthesis of leukotrienes from Arachidonic Acid. Used as an antiasthmatic. References Carter, G.W., et al.: J. Pharmacol. Exp. Ther., 256, 929 (1991), Weinblatt, M.E., et al.: J. Rheumatol., 19, 1537 (1992), McGill, K and Busse, W.W.: Lancet, 348, 519 (1996)

Aureusidin (Auresidin) shows antioxidant and lipoxygenase inhibitory activity with anti-inflammatory effects.

S-2474, an inhibitor of COX-2 and 5-lipoxygenase, has anti-inflammatory and neuroprotective activities, and inhibits cell death.

Lonapalene is a topically effective inhibitor of 5-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

6-Hydroxyflavanone from Acorus calamus leaves targets COX-2, 5-LOX, opioid, and GABA-A receptors, reducing inflammation and neuropathic pain.

Compound 29, also known as 5-LOX-IN-5, is a 5-lipoxygenase (5-LOX) inhibitor with an inhibitory concentration 50 (IC50) of 56 nM, utilized in research

Zileuton (A 64077) inhibits 5-lipoxygenase, reduces leukotrienes, aids bronchodilation, lessens mucus/edema, and helps manage asthma symptoms.

Nordihydroguaiaretic acid (NDGA) is a natural lipoxygenase (5-LOX) inhibitor. Nordihydroguaiaretic acid has antioxidant effect. Cost-effective and quality-assured.

A-69412 is a reversible 5-lipoxygenase inhibitor, potentially treating ulcerative colitis and asthma.

KKII5 is a potent inhibitor of the lipoxygenase LOX-1 with an IC50 of 19 μM.KKII5 inhibits lipid peroxidation and enhances the ability of the active centers of

5-Lipoxygenase-In-1 (compound example 4.10) is a 5-Lipoxygenase inhibitor.

ThioLox, a 15-LOX-1 inhibitor (IC50: 12 μM), has anti-inflammatory, neuroprotective benefits, and guards against glutamate toxicity.

Wedelolactone (IKK Inhibitor II) inhibits NF-κB-mediated gene transcription in cells by blocking the phosphorylation and degradation of IκBα.

Applications Isotope labelled Acetone 2,4-Dinitrophenylhydrazone is a dinitrophenylhydrazone (DNPH) derivative of an aliphatic ketone found in mainstream cigarette smoke. Acetone 2,4-Dinitrophenylhydrazone showed inhibitory activity towards soybean lipoxygenase and renal prostaglandin synthetase. References Delgado, B. et al.: J. Liq. Chrom. Rel Technol., 31, 361 (2008); Miller, J.H. et al.: J. Chrom. Sci., 48, 12 (2010); Baumann, J. et al.: Agents Act., 12, 360 (1982);

Applications Belamcandol B is a compound isolated from the seeds of B. Chinensis. and known to be an starting compound in the synthesis of 5-lipoxygenase inhibitors. References Fukuyama, Y., et al.: Chem. Pharma. Bull., 39, 1877 (1991); Fukuyama, Y., et al.: Chem. Pharma. Bull., 41, 561 (1993);

Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally.

ZD-2138: Selective 5-LOX inhibitor, eases allergen-induced asthma attacks and airway constriction in guinea pigs.