Xanthine Oxidase

Baicalein (5,6,7-Trihydroxyflavone) is a xanthine oxidase inhibitor.

Broussochalcone A is a natural antioxidant and xanthine oxidase inhibitor (IC50 = 2.21 μM) that scavenges free radicals, inhibits iron-induced lipid peroxidation, and reduces nitric oxide synthesis in LPS-activated macrophages. Broussochalcone A induces apoptosis in human renal carcinoma cells by increasing ROS levels and activating the FOXO3 signaling pathway. Broussochalcone A is also a novel NR4A1 inhibitor that induces apoptosis in pancreatic cancer cells through NR4A1-dependent pathways.

Febuxostat (TEI 6720) is a xanthine oxidase inhibitor.

Niraxostat (Y-700) is one of the isocytosine derivatives as xanthine oxidase inhibitors.

Benzbromarone (Desuric) is a CYP2C9 inhibitor with Ki value of 19.3 nM.

Forsythoside F (Arenarioside) is a natural compound with GI50 values ranging from 10 to 16 μM against B16F10 cells.

Oxypurinol is a xanthine oxidase inhibitor. Oxipurinol is potentially used for the treatment of congestive heart failure.

Purpurogallin, a naturally occurring phenol extracted from Quercus spp. plants, exhibits potent xanthine oxidase inhibitory activity (IC50: 0.2 μM) and also possesses antioxidant and anti-inflammatory effects.

Allopurinol (Zyloric) is a Xanthine Oxidase Inhibitor. The mechanism of action of allopurinol is as a Xanthine Oxidase Inhibitor.

Phytic acid (Fytic Acid) is a complexing agent for removal of traces of heavy metal ions. It acts also as a hypocalcemic agent.

Amflutizole used for the treatment of gout, and is a Xanthine oxidase inhibitor

Tigulixostat (LC350189) is a novel xanthine oxidase inhibitor (XOI) that reduces uric acid production and may be used in studies of gout-related diseases.

Nequinate is an anticoccidial agent, preventing coccidiosis .

Topiroxostat (FYX-051) is a selective xanthine oxidase inhibitor developed for the treatment and management of hyperuricemia and gout.

6-Formylpterin (Pterin-6-aldehyde) is an inhibitor of Xanthine Oxidase (Ki ~0.6 nM) with potent neuroprotective effects against transient IRI in gerbils.6-Formylpterin induces intracellular ROS generation in HL-60 cells as well as apoptosis ( 6-Formylpterin inhibits the expression of iNOS, produces hydrogen peroxide intracellularly and restores the impaired bactericidal activity of human neutrophils.

Myricetin 3-O-galactoside (Myricetin 3-O-beta-D-galactopyranoside) can inhibit xanthine oxidase (xanthine oxidase; XO) activity, lipid peroxidation and scavenging free radicals. Myricetin 3-O-galactoside has many effects, including cytotoxicity, anti-oxidation, anti-genotoxicity, anti-infectivity, anti-inflammatory and antioxidant activities, and its main effect is to inhibit the synthesis of inducible nitric oxide synthase (iNOS). The IC50 of Myricetin 3-O-galactoside inhibited lipid peroxidation was 160 μg mL.

8-Azaadenine (NSC-32797) is an inhibitor of xanthine oxidase with IC50 of 0.54 μM and Ki of 0.66 μM.

4-Hydroxyacetophenone (4-Acetylphenol) is a potent xanthine oxidase inhibitor.

Phytic acid dodecasodium salt hydrate (myo-Inositol, hexakis(dihydrogen phosphate) dodecasodium salt hydrate) is a phosphorus storage compound of seeds and cereal grains. Phytic acid dodecasodium salt hydrate inhibits the enzymatic superoxide source xanthine oxidase with an IC50 of 6 mM and has antioxidative, neuroprotective, and anti-inflammatory effects.

Prudomestin (3,5,7-Trihydroxy-4',8-dimethoxyflavone) is a natural product isolated from the heartwood of Prunus domestica, with xanthine oxidase (XO) inhibitory activity with IC50 of 6 µM.

Xanthine oxidase-IN-1 is an effective inhibitor of xanthine oxidase with an IC50 value of 6.5 nM. It plays a central role in purine catabolism through the degradation of bioactive nucleotides facilitated by nucleic acid and nucleotide intermediates.

Xanthine oxidoreductase-IN-5 is an orally active inhibitor of xanthine oxidoreductase (XOR) with an IC50 of 55 nM. Xanthine oxidoreductase-IN-5 may be used in studies of acute hyperuricemia.

Xanthine oxidoreductase-IN-4 is an orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 29.3 nM, useful for studying hyperuricemia.

Xanthine oxidoreductase-IN-3 is an orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 of 26.3 nM, suitable for use in acute hyperuricemia studies.

Tetrahydroamentoflavone is a potent XO inhibitor (IC50 = 92 nM, Ki = 982 nM) with anti-inflammatory effects. Tetrahydroamentoflavone can be used for studies about inflammation and gout.

HDAC-IN-79 (compound 4) is an orally active dual inhibitor of xanthine oxidase and HDAC, exhibiting potent anti-hyperuricemia and antitumor activities in vivo (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM). Among leukemia cells, it is most effective in inhibiting the growth of HL60 cells (IC50=0.706 μM) and induces both apoptosis and autophagy. HDAC-IN-79 also modulates the expression levels of biomarkers associated with intracellular HDAC inhibition.

Blumeatin shows XO inhibitory activity.

Compound BDEO (URAT1&XO inhibitor 2) serves as a dual-action inhibitor targeting both xanthine oxidase (XO) and URAT1, demonstrating an IC50 value of 3.3 μM for XO inhibition. It effectively impedes uric acid uptake in HEK293 cells with URAT1 expression, evidenced by a Ki of 0.145 μM. In hyperuricemic mice models, the compound has been shown to reduce serum urate levels and uric acid excretion, indicating potential utility for hyperuricemia research [1].

Compound 5f (Antioxidant agent-13) is an antioxidant that demonstrates inhibition of DPPH and FRAP with half maximal inhibitory concentrations (IC50s) of 80.33 µM and 85.69 µM, respectively. Additionally, it inhibits the enzymes lipoxygenase (LOX) and xanthine oxidase (XO) with IC50s of 16.85 µM and 23.01 µM, respectively [1].

CC15009 is a potent inhibitor of xanthine oxidoreductase (XOR), demonstrating an IC50 value of 0.237 nM. It effectively inhibits the oxidative subtype of XOR, thereby reducing the generation of the byproduct ROS and exhibiting antioxidant activity. CC15009 has shown a favorable dose-dependent uric acid-lowering effect in two different XOR substrate-induced hyperuricemia mouse models.

Fraxamoside is a xanthine oxidase inhibitor (XOI) comparable in potency in vitro to the standard antigout drug allopurinol. It shows significant free radical scavenging effect against DPPH(EC50=62.6 uM).

URAT1&XO Inhibitor 1 (compound 29) serves as a dual inhibitor with IC50 values of approximately 10 μM for URAT1 and 1.01 μM for Xanthine Oxidase. It induces a hypouricemic effect in the potassium oxonate-induced hyperuricemic rat model and is utilized in research pertaining to hyperuricemia [1].

Xanthine Oxidase-IN-11, an analog of XO8, is an inhibitor of xanthine oxidase (XO) [1].

Xanthine oxidase-IN-12 (Compound 11), an inhibitor of xanthine oxidase (XO), has an IC50 value of 91 nM and exhibits antioxidant properties, also reducing intracellular reactive oxygen species (ROS) [1].

Xanthine oxidase-IN-16 is an effective orally active inhibitor of xanthine oxidase (XO), demonstrating significant therapeutic efficacy in rats with hyperuricemia and an IC50 of 102 nM.