Lipoxygenase Inhibitor

ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC₅₀ of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2. ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D.

Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenase inhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of type II diabetes.

Chebulagic acid is a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz, on angiogenesis. Chebulagic acid is a M2 serine to asparagine 31 mutation (S31N) inhibitor and influenza antiviral. Chebulagic acid also against SARS-CoV-2 viral replication with an EC₅₀ of 9.76 μM.

7-Hydroxyflavone is a flavonoid isolated from Clerodendrum phlomidis, with anti-inflammatory activity. 7-Hydroxyflavone protects renal cells from nicotine (NIC)-associated cytotoxicity via the ERK/Nrf2/HO-1 pathway. 7-Hydroxyflavone inhibits PKM2 with an IC₅₀ of 2.12 μM. 7-Hydroxyflavone inhibits COX-2 and 5-LOX with IC₅₀ of 27 µg/mL and 33 µg/mL. 7-Hydroxyflavone is orally active.

Wedelolactone (Standard) is the analytical standard of Wedelolactone. This product is intended for research and analytical applications. Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibits the IKK Complex. Wedelolactone also inhibits 5-lipoxygenase (5-Lox) with an IC50 of 2.5 μM. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Wedelolactone can extract from Eclipta alba, and it can be used for the research of cancer.

Zileuton (Standard) is the analytical standard of Zileuton. This product is intended for research and analytical applications. Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.

Triphenylphosphinechlorogold (Chloro(triphenylphosphine)gold(I)) is a gold complex, Apoptosis inducer, and catalyst. Triphenylphosphinechlorogold exhibits high LOX inhibitory activity. Triphenylphosphinechlorogold induces cell cycle arrest and apoptosis. Triphenylphosphinechlorogold catalyzes the peroxidation of linoleic acid. A weak interaction exists between Triphenylphosphinechlorogold and DNA. Triphenylphosphinechlorogold displays antiproliferative activity against breast cancer cells.

Caffeic acid (Standard) is the analytical standard of Caffeic acid. This product is intended for research and analytical applications. Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO).

4',5-Dihydroxyflavone (Compound 2c; Compound B3) is a type of flavonoid compound. 4',5-Dihydroxyflavone can inhibit various oxidases and its IC₅₀ values for collagenase A (ColA) and α-glucosidase are less than 1 μM and 66 μM respectively; for soybean lipoxygenase-1 (LOX-1), its K_i value is 102.6 μM. 4',5-Dihydroxyflavone can be used in studies on anti-toxicity and anti-diabetes.

ALOX15-IN-1 (compound 8b) is a potent inhibitor of the linoleate oxygenase activity of rabbit and human ALOX15 with _IC50s of 0.04 and 2.06 μM for ALOX15 0rthologs linoleic acid (LA) and arachidonic acid (AA), respectively.

Tepoxalin is an orally active dual inhibitor of Cyclooxygenase/Lipoxygenase, with IC₅₀ values of 4.6 μM (sheep cyclooxygenase), 2.85 μM (rat cyclooxygenase), 0.15 μM (rat 5-lipoxygenase), and 3.0 μM (h12-lipoxygenase), respectively. Tepoxalin inhibits ROS production and NF-κB activation. Tepoxalin suppresses the production of thromboxane B₂, leukotriene B₄, prostaglandins and cytokines, and blocks platelet aggregation. Tepoxalin exhibits potent anti-inflammatory activity in rats with adjuvant-induced arthritis. Tepoxalin possesses analgesic activity. Tepoxalin shows no ulcerogenic activity within the anti-inflammatory dose range. Tepoxalin can be used in studies related to adjuvant-induced arthritis, skin inflammation and Alzheimer's disease.

ALOX15-IN-2 (compound 8a) is a potent inhibitor of the linoleate oxygenase activity of rabbit and human ALOX15 with _IC50s of 1.55 and 2.79 μM for ALOX15 0rthologs linoleic acid (LA) and arachidonic acid (AA), respectively.

2-TEDC is a potent inhibitor of 5-, 12-, and 15-lipoxygenase with IC₅₀ values of 0.09 μM, 0.013 μM and 0.5 μM, respectively. 2-TEDC can be used for the research of atheroscrelosi.

LXG6403 is an orally active and irreversible LOX inhibitor (IC₅₀ = 1.3 μM). LXG6403 is ~3.5-fold more specific for LOX than LOXL2 and does not inhibit LOXL1. LXG6403 inhibits FAK signaling and induces ROS generation and DNA damage, leading to G1 arrest and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines. LXG6403 alters the extracellular matrix (ECM) and collagen structure, reducing collagen cross-linking and deposition, thereby increasing drug penetration and reducing tumor stiffness. LXG6403 overcomes Doxorubicin (HY-15142) resistance in chemoresistant TNBC PDX in vivo and can be used to study high-stiffness resistant tumors.

3-Aminobutanoic acid is a β-amino acid. 3-Aminobutanoic acid can protect plant against a challenge infection with P. infestans. 3-Aminobutanoic acid has various levels of susceptibility for the pathogen.

Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) is a potent 12/15-Lipoxygenases (LO) inhibitor. Cinnamyl-3,4-dihydroxy-α-cyanocinnamate has the potential for the research of type 1 diabetes mellitus.

CJ-13,610, a nonredox-type 5-LO inhibitor, dose dependently suppresses 5-LO product formation in ionophore A23187-stimulated PMNL in the absence of exogenous AA with an IC₅₀ of about 70 nM. PMNL: polymorphonuclear leukocytes; AA: arachidonic acid

FPL 62064 is a potent 5-lipoxygenase (5-LOX) and COX dual inhibitor, with IC₅₀ values of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase (cyclooxygenase), respectively. FPL 62064 has potent anti-inflammatory activity.

3-Hydroxy-2-pyrone (Compound 12d) is a metalloenzyme inhibitor. 3-Hydroxy-2-pyrone shows an inhibition rate of approximately 50% for matrix metalloproteinases (MMP) and the inhibition rate for non-heme iron enzyme 5-lipoxygenase (5-LOX) was over 70% at 1 mM. 3-Hydroxy-2-pyrone also has certain inhibitory activity against copper-dependent enzyme tyrosinase. 3-Hydroxy-2-pyrone can be used for the research of cancer, infection and inflammation.

ThioLox is a competitive 15-lipoxygenase-1 (15-LOX-1) inhibitor with a K_i of 3.30 μM. ThioLox shows anti-inflammatory and neuroprotective properties.