Lipoxygenase

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.

Phenethyl ferulate is a chemopreventive against colon cancer, enhancing apoptosis in tumors and inhibiting COX/5-LOX (IC50: 4.35/5.75 μM).

PGS-IN-1 (KME-4) is a potent inhibitor of prostaglandin synthetase (PGS, IC50: 0.28 μM) and 5-lipoxygenase (IC50: 1.05 μM).

Phenidone inhibits COX/LOX, reducing rat autoimmune paralysis and lowering blood pressure in hypertensive rats.

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].

Applications Deuterated Ketoconazole, an inhibitor of 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)

PXS-6302 hydrochloride is a potent irreversible lysine oxidase (LOX) inhibitor, inhibiting Bovine LOX, rh LOXL1, rh LOXL2, rh LOXL3, and rh LOXL4 with IC50 of 3

Meclofenoxate HCl (Lucidril) boosts memory and cognition; it's a DIMETHYLAMINOETHANOL and p-chlorophenoxyacetic acid ester.

ALOX15-IN-2: Potent ALOX15 inhibitor. IC50: 1.55 μM for LA; 2.79 μM for AA. Stops linoleic/arachidonic acid oxidation.

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.

Applications PD-146176 is a potent and selective 15-LO inhibitor.

COX-2/15-LOX-IN-3 (compound 5k) serves as a dual inhibitor for COX-2 and 15-LOX, demonstrating inhibitory concentrations (IC50) of 0.075 μM and 1.97 μM,

11-Keto-beta-boswellic acid, a novel Nrf2 activator, and a selective 5-lipoxygenase (5-LOX) inhibitor, exerts dose dependent cardioprotective effect manifested.

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

Lipoxygenase (LOX) is a dioxygenase that catalyzes the peroxidation of linoleic acid (LA) or arachidonic acid (AA) in the presence of molecular oxygen.

6-Shogaol: anti-inflammatory, analgesic, antipyretic, protects cartilage, arrests cancer cell growth, inhibits metastasis.

Enazadrem is a 5-lipoxygenase inhibitor with antiinflammatory activities.

Licofelone (ML-3000) is a dual COX/LOX inhibitor potentially for the treatment of osteoarthritis.

Benoxaprofen (NSC-299582) is a non-steroidal anti-inflammatory drug.

5-LOX-IN-1 is a 5-Lipoxygenase (5-LOX) inhibitor (IC50: 2.3 μM).5-LOX-IN-1 can be used for cancer research.

3-O-Acetyl-11-hydroxy-beta-boswellic acid is the precursor of 3-O-acetyl-9, 11-dehydro-beta-boswellic acid(a 5-lipoxygenase inhibitor ).

SKF-86002 is an effective inhibitor of p38 MAP kinase (IC50: 0.5-1 uM); inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50: 1 μM).

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

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

LOX-IN-5 (compound 22) is a non-selective LOX inhibitor.

CCT365623 hydrochloride is an orally active inhibitor of lysyl oxidase (LOX) (IC50: 0.89 μM). It suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF.