5-lipoxygenase

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

5-Lipoxygenase-IN-3 (Compound 14), with an IC50 of less than 1 μM, serves as an inhibitor of 5-Lipoxygenase. This compound is utilized in the research of inflammatory diseases, cancer, stroke, and Alzheimer's disease [1].

Zileuton (A 64077) is a synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma.

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

CBS-1114 HCl (N-Phenylbenzamidrazone hydrochloride) is a 5-lipoxygenase inhibitor and an anti-inflammatory compound in a good eye-permeable model.CBS-1114 HCl maintains and improves cardiac function, attenuates cardiac dysfunction, as well as reduces epicardial adipose tissue and/or pericardial adipose tissue in subjects with cardiovascular disease.

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.

ER-34122, a novel orally available dual 5-lipoxygenase/cyclooxygenase inhibitor, exhibits potent anti-inflammatory activity in an arachidonic acid-induced ear inflammation model.

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.

Croconazole exhibited dose-dependent inhibitory activity on the 5-lipoxygenase (5-LOX) of neutrophils. Croconazole is an antimycotic agent. The IC50s for the synthesis of leukotriene B4 (LTB4) and 5-hydroxyeicosatetraenoic acid (5-HETE) is 7.8 +/- 1.7 and

Efletirizine (UCB-28754) is a histamine receptor antagonist with inhibitory effects on the enzyme 5-lipoxygenase (5-LO), and is useful in the topical treatment of allergic diseases.

6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.

REV 5901A (REV 5901 HCl) is an orally active leukotriene receptor antagonist and 5-lipoxygenase inhibitor with antimicrobial activity that attenuates colon cancer growth in mice.REV 5901A has been used in studies of asthma and myocardial infarction. REV 5901A is used to study asthma and myocardial infarction.

Linetastine (TMK-688) is a 5-lipoxygenase inhibitor (5-LOX) that inhibits leukotriene production and antagonizes the effects of histamine.Linetastine is used in studies of asthma, atherosclerosis, and peptic ulcers.

L 651896 is a novel leukotriene biosynthesis and 5-lipoxygenase inhibitor for the study of respiratory and cardiovascular diseases.

PF-4191834 is a noniron chelating and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) with an IC50 of 229 nM. PF-4191834 shows ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX and displays no activity toward the cyclooxygenase enzymes. PF-4191834

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.

Veliflapon is an orally active and selective inhibitor of 5-lipoxygenase activating protein (FLAP). Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.

ZD-2138 is a potent and selective specific inhibitor of 5-lipoxygenase (5-LOX) that inhibits allergen-induced pulmonary bronchoconstriction and reduces neurally-induced fast-acting kallikrein-ergic constriction of isolated airways in guinea pigs.ZD-2138 can be used for the treatment of asthma disease.

RWJ 63556, an orally active inhibitor of COX-2 selective [5-lipoxygenase], exhibits anti-inflammatory activities.

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

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

U-73343 is an inactive analog of U-73122 and can be used as a negative control. It dose-dependently inhibits acid secretion irrespective of the stimulant. It is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 μM for PLC.

WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal.

Ciclopirox (HOE296b) exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. Ciclopirox is a synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, the organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).

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

Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300 CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.

MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, acting by inhibiting the 5-lipoxygenase-activating protein (FLAP), and serves as a moderately potent PPARα antagonist.

Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH) inhibitor, exhibiting marked anti-inflammatory efficacy and high target selectivity.

Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally. Psoralidin possesses anticancer and chemopreventive properties.

5-O-Demethylnobiletin (5-DEMETHYLNOBILETIN) is a natual product, has anti-inflammatory activity, it may act through a direct inhibition of 5-LOX, without affecting the expression of COX-2.

11-Keto-beta-boswellic acid, a novel Nrf2 activator, and a selective 5-lipoxygenase (5-LOX) inhibitor; it exerts dose dependent cardioprotective effect manifested by dose-dependent reduction in serum lactate dehydrogenase

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

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

Etalocib (LY293111) is a novel diaryl ether carboxylic acid derivative, is a selective and potent inhibitor of the lipoxygenase pathway either via antagonism of the leukotriene B4 (LTB4) receptor or directly through 5'-lipoxygenase. It has antineoplastic activities.

4-Methyldaphnetin (DHMC) is a potent inhibitor (low micromolar) of lipid peroxidation and scavengers of superoxide anion radicals and of aqueous alkylperoxyl radicals, but may be pro-oxidant (enhancing generation of hydroxyl radicals) in the presence of free iron ions.2. 4-Methyldaphnetin(7,8-Dihydroxy-4-methylcoumarin) inhibits the proinflammatory 5-lipoxygenase enzyme at micromolar concentrations.

Quiflapon (MK-591) causes cell apoptosis. Quiflapon is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor (IC50: 1.6 nM in a FLAP binding assay) and is also an effective and orally active Leukotriene biosynthesis (LT) inhibitor (IC50: 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively).

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

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 synthetase, respectively).

1. Xanthatin has cytotoxic activity. 2. Xanthatin has antibacterial and antifungal activies against MRSA. 3. Xanthatin may have therapeutic potential against NSCLC. 4. Xanthatin can inhibit murine melanoma B16-F1 cell proliferation possibly associated wit

Tepoxalin (RWJ 20485) is a 5-lipoxygenase inhibitor potentially for the treatment of asthma, osteoarthritis. Tepoxalin inhibits COX-1, COX-2, and 5-LOX. Tepoxalin is a potent inhibitor of sheep seminal vesicle cyclooxygenase (COX) (IC50 = 4.6 microM), rat basophilic leukemia cell (RBL-1) lysate COX (IC50 = 2.85 microM) and COX from intact RBL-1 cells (IC50 = 4.2 microM).

9,11-Dehydro-β-boswellic acid is a compound with urease inhibitory activity and acts as an inhibitor of 5-lipoxygenase (5-LO), a critical enzyme in leukotriene biosynthesis.

CGS 23885 is a 5-lipoxygenase inhibitor.

PD 127443 is a Leukotriene B4 antagonist, it is also a dual inhibitor of cyclooxygenase and 5-lipoxygenase.

L 739059 is a radioiodinated analog of arachidonic acid that binds 5-lipoxygenase-activating protein.

Abroquinone A, a natural isoflavanquinone, has been shown to block cytosolic phospholipase A(2) and 5-lipoxygenase activation in neutrophils, it may have pharmaceutical potential as an antiallergic agent.

RG 6866 is a inhibitor of 5-lipoxygenase.

Dual cyclooxygenase-2 (COX-2)/5-lipoxygenase (5-LO) inhibitors are potential therapeutic agents for inflammatory diseases and for prostate cancer. CAY10416 is a dual COX-2/5-LO inhibitor with IC50 values of 50 and 3 nM, respectively. The selectivity of CAY10416 for COX is greater than 200-fold for COX-2 versus COX-1. COX-2/5-LO inhibitors such as CAY10416 are also apoptosis-inducing agents and are potentially useful in prostate cancer chemotherapy. In the PC3 human carcinoma cell line, CAY10416 exhibits a 45% inhibition of proliferation at 100 μM. In the LNCaP human carcinoma cell line, CAY10416 inhibits growth with an IC50 value of 83 μM.

12(S)-HEPE is a monohydroxy fatty acid synthesized from EPA by the action of 12-LO. Unstimulated neutrophils metabolize 12(S)-HEPE to 12(S),20-diHEPE, while stimulated neutrophils produce 5(S),12(S)-HEPE via the 5-lipoxygenase pathway. The competitive action of 12(S)-HEPE with arachidonic acid as a substrate for 5-LO in leukotriene formation may underlie the anti-inflammatory potential of ω-3 fatty acids.

(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) with an IC50 of 1.7 nM for FLAP binding.