Lipoxygenase

Cat. No.

A21493

CAS No.

80809-81-0

Docebenone

Synonyms: AA 861

Docebenone (AA 861) is a potent, selective and orally active 5-LO (5-lipoxygenase) inhibitor.

Cat. No.

A21831

CAS No.

118569-21-4

Zileuton sodium

Synonyms: A 64077 sodium; Abbott 64077 sodium; A64077

Zileuton sodium (A 64077 sodium) is a potent and selective inhibitor of 5-lipoxygenase, exhibiting inflammatory activities.

Cat. No.

A21969

CAS No.

2098884-53-6

PAT-1251 Hydrochloride

Synonyms: PAT 1251

PAT-1251 Hydrochloride is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively).

Cat. No.

A22517

CAS No.

684236-01-9

CAY10698

CAY10698 is an inhibitor of 12-LO with an IC50 value of 5.1 μM.

Cat. No.

A24207

CAS No.

6665-86-7

7-Hydroxyflavone

7-Hydroxyflavone is an orally active flavonoid isolated from *Clerodendrum phlomidis*, exhibiting notable anti-inflammatory activity. It protects renal cells from nicotine-induced cytotoxicity through activation of the ERK/Nrf2/HO-1 signaling pathway. Additionally, 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM, and suppresses COX-2 and 5-LOX with IC50 values of 27 μg/mL and 33 μg/mL, respectively.

Cat. No.

A24249

CAS No.

315705-04-5

LXG6403

LXG6403 is a highly potent and irreversible lysyl oxidase (LOX) inhibitor that efficiently suppresses cellular LOX activity in MDA-MB-231 cells with an IC50 of 1.3 μM. It exhibits over 3-fold selectivity for LOX over LOXL2 and shows no inhibitory activity against LOXL1, making it a valuable tool for studying LOX-specific functions in cancer and fibrosis research.

Cat. No.

A24322

CAS No.

92-43-3

Phenidone

Phenidone is an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX) pathways, exhibiting anti-inflammatory and immunomodulatory effects. It has been shown to ameliorate paralysis in rat models of experimental autoimmune encephalomyelitis (EAE), a model for multiple sclerosis. Phenidone also acts as a potent hypotensive agent in spontaneously hypertensive rats. Additionally, it has a long-standing application as a photographic developer due to its redox properties.

Cat. No.

A24657

CAS No.

1353567-32-4

EP6

EP6 is a selective 5-Lipoxygenase (5-LO) inhibitor that exhibits potent anti-tumor activity. It effectively reduces the viability of various tumor cell lines while demonstrating a lack of mutagenic properties. This compound is valuable for research applications focused on cancer therapy and the modulation of inflammatory pathways.

Cat. No.

A26844

CAS No.

2773428-48-9

FerroLOXIN-1

FerroLOXIN-1 is a potent inhibitor of the enzyme 15-lipoxygenase-2 (15LOX-2) that effectively reduces the production of pro-ferroptotic lipid species, specifically HOO-ETE-PE. This compound has demonstrated protective effects against RSL3-induced ferroptosis, making it a valuable tool in studying ferroptotic pathways. The selective interaction of FerroLOXIN-1 with the active site residues Y154, N155, and W158 of 15LOX-2 underscores its targeted mechanism of action, positioning it as a valuable reagent for research into lipid metabolism and ferroptosis.

Cat. No.

A26996

CAS No.

1213269-96-5

Utreloxastat

Synonyms: PTC857

Utreloxastat (PTC857) is a selective inhibitor of 15-lipoxygenase, capable of crossing the blood-brain barrier. This compound demonstrates a significant ability to reduce oxidative stress, inhibit the depletion of reduced glutathione, and prevent ferroptosis. Utreloxastat is particularly relevant in the research of neurodegenerative diseases associated with elevated oxidative stress and mitochondrial dysfunction, including conditions such as amyotrophic lateral sclerosis.

Cat. No.

A27167

CAS No.

18810-05-4

Asperenone

Asperenone is a potent inhibitor of 15-lipoxygenase (15-LOX), with an IC50 value of 0.3 mM, and effectively inhibits platelet aggregation at an IC50 of 0.23 mM. This compound also exhibits antifungal properties, demonstrating the ability to inhibit the growth of pathogenic fungi such as Ophiostoma crassivaginatum and O. piliferum. Asperenone is valuable for research in cardiovascular disease and antifungal therapy, providing a multifaceted approach to studying inflammatory processes and infection control.

Cat. No.

A27855

CAS No.

549-23-5

Sclerotiorin

Sclerotiorin is a reversible uncompetitive inhibitor of soybean lipoxygenase-1 (LOX-1), with an IC50 value of 4.2 μM. This compound exhibits significant antioxidant activity by scavenging free radicals (ED50: 0.12 μM) and inhibiting nonenzymatic lipid peroxidation. Additionally, Sclerotiorin demonstrates antifungal properties and the ability to inhibit platelet aggregation. It can be isolated from the fermented broth of Penicillium frequentans, making it a valuable reagent for research in antifungal mechanisms and oxidative stress studies.

Cat. No.

A31098

CAS No.

928853-86-5

4-MMPB

4-MMPB is a selective inhibitor of 15-lipoxygenase, exhibiting an IC50 of 18 μM. It demonstrates competitive inhibition with IC50 values of 19.5 μM for soybean 15-lipoxygenase and 19.1 μM for human 15-lipoxygenase-1. This compound may hold promise for research applications focused on prostate cancer, providing insights into the role of 15-lipoxygenase in tumor biology.

Cat. No.

A31270

CAS No.

1019110-87-2

CNB-001

CNB-001 is a potent inhibitor of 5-lipoxygenase (5-LOX), demonstrating strong oral bioavailability. This compound effectively reduces 5-LOX expression and enhances proteasome activity, leading to the inhibition of soluble Amyloid-β accumulation and ubiquitinated protein aggregates. It also exhibits neuroprotective properties by inhibiting apoptosis and reactive oxygen species (ROS) production while stabilizing mitochondrial membrane potential. Additionally, CNB-001 addresses insulin resistance and enhances glucose uptake, making it valuable for research into inflammation, neurological disorders, and metabolic diseases such as Alzheimer's disease, stroke, and diabetes.

Cat. No.

A33907

CAS No.

299460-62-1

UCB-35440

UCB-35440 is an orally active antagonist of the histamine H1 receptor and a selective inhibitor of 5-lipoxygenase. It demonstrates significant inhibition of leukotriene B4 (LTB4) formation in human whole blood, as well as a reduction in polymorphonuclear cell infiltration in mouse models. UCB-35440 also effectively inhibits histamine-induced bronchoconstriction and alleviates skin inflammation in guinea pig studies. This compound is suitable for research applications related to asthma and inflammatory skin conditions.

Cat. No.

A34111

CAS No.

159776-68-8

Linetastine

Linetastine is a potent, orally active inhibitor of 5-Lipoxygenase, an enzyme critical in the synthesis of leukotrienes. By inhibiting this pathway, Linetastine demonstrates significant antihistamine activity, effectively reducing leukotriene B4 and C4 release from calcium ionophore-stimulated human leukocytes. This compound is particularly useful in research applications focused on inflammatory processes and allergic responses, providing insights into the modulation of leukotriene-mediated pathways.

Cat. No.

A37714

CAS No.

631-69-6

β-Boswellic acid

β-Boswellic acid, a potent inhibitor of 5-lipoxygenase (5-LO), is derived from the gum resin of Boswellia serrata. This compound exhibits significant anticancer, antioxidant, anti-inflammatory, and anti-arthritic properties. Its mechanism involves direct interaction with 5-LO or inhibition of its translocation, leading to reduced synthesis of DNA, RNA, and protein in human leukemia HL-60 cells, with IC50 values ranging from 0.6 to 7.1 μM. β-Boswellic acid holds potential for research into diabetes and inflammatory disorders, particularly those related to arthritis.

Cat. No.

A38115

CAS No.

3026677-37-9

12R-LOX-IN-2

12R-LOX-IN-2 is a potent inhibitor of 12R-lipoxygenase (12R-LOX), demonstrating significant biological activity in the modulation of keratinocyte proliferation. This compound effectively inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and suppresses colony formation. Additionally, 12R-LOX-IN-2 decreases protein levels of Ki67 and mRNA expression of IL-17A in IMQ-treated cells, making it a valuable reagent for research on psoriasis and related skin inflammatory conditions.

Cat. No.

A38362

CAS No.

857758-13-5

12R-LOX-IN-1

12R-LOX-IN-1 is a selective inhibitor of 12-lipoxygenase (12R-LOX), with an IC50 of 28.25 μM. This compound effectively reduces the hyper-proliferative state and colony-forming ability of Imiquimod-induced psoriatic keratinocytes. Additionally, 12R-LOX-IN-1 modulates key inflammatory markers by inhibiting the production of reactive oxygen species, Ki67, IL-17A, TNF-α, and IL-6. It is a valuable tool for antipsoriatic research and the investigation of related biological pathways.

Cat. No.

A38988

CAS No.

38216-54-5

Aureusidin

Aureusidin is a potent lipoxygenase inhibitor known for its significant antioxidant properties. It exhibits anti-inflammatory effects, making it a valuable compound for research focused on inflammatory pathways and oxidative stress responses. Aureusidin is applicable in studies investigating the modulation of lipoxygenase activity and its implications in various diseases.

Cat. No.

A39988

CAS No.

916482-17-2

YS121

YS121 is a dual inhibitor targeting microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LOX), with IC50 values of 3.4 μM and 6.5 μM, respectively. It demonstrates specific, reversible binding to mPGES-1, indicated by a KD of 10-14 μM. YS121 reduces PGE2 production in IL-1β-stimulated A549 cells with an EC50 of 12 μM and activates PPAR-α and PPAR-γ, with EC50 values of 1 μM and 3.6 μM, respectively. Additionally, YS121 exhibits significant anti-inflammatory effects in human whole blood and in vivo, making it a valuable tool for pleurisy research.

Cat. No.

A43485

CAS No.

68422-00-4

Timosaponin A1

Timosaponin A1 is a natural steroidal saponin that acts as an inhibitor of 5-lipoxygenase (5-LO), cyclooxygenase-2 (COX-2), and dipeptidyl peptidase 4 (DPP-4), with IC50 values of 3.29 µM, 36.43 µM, and 33.25 µM, respectively. This compound exhibits anti-inflammatory properties and is relevant for research on conditions such as asthma and diabetes. Its inhibitory effects on key enzymes involved in inflammatory pathways make it a valuable tool for exploring therapeutic strategies in related biological studies.

Cat. No.

A43925

CAS No.

2315406-63-2

IMA-1

IMA-1 is an inhibitor of the interaction between arachidonic acid 12-lipoxygenase (ALOX12) and acetyl-CoA carboxylase 1 (ACC1). This compound has demonstrated significant efficacy in blocking the progression of diet-induced non-alcoholic steatohepatitis (NASH) in male mice and crab-eating monkeys, while not inducing hyperlipidemia. IMA-1 serves as a valuable tool for investigating the underlying mechanisms and potential treatments for NASH.

Cat. No.

A45103

CAS No.

2080300-52-1

Naloxone fluorescein acetate

Naloxone fluorescein acetate is a fluorescent derivative of Naloxone, an opioid antagonist that serves as a critical antidote for reversing opioid overdose effects. This compound enables the visualization of Naloxone's pharmacological activity in biological systems through fluorescent detection. Key applications for this reagent include opioid research, overdose studies, and the development of novel therapeutic strategies in addiction and pain management.

Cat. No.

A46854

CAS No.

134762-03-1

A-71497

A-71497 is a tosufloxacin derivative that serves as a prodrug, generating elevated plasma levels of tosufloxacin following both oral and subcutaneous administration in murine models. This compound is primarily utilized in antibiotic research to explore its pharmacokinetics and therapeutic efficacy. Its ability to enhance bioavailability makes it a valuable tool for studying antibiotic treatment strategies in preclinical settings.