COX Inhibitor

Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 25.8 μM; is a widely used antipyretic and analgesic agent.. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor. Acetaminophen induces ferroptosis and leads to acute liver injury in mice model.

EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA also enhances autophagy by inhibiting Na⁺/H⁺-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.

Leupeptin hemisulfate is a broad-spectrum protease inhibitor. Leupeptin hemisulfate inhibits serine, cysteine and threonine proteases, and regulates autophagy. Leupeptin hemisulfate reduces the expression levels of LC3B, iNOS, Cox-2, Beclin-1 and the level of endopeptidases; increases the levels of p62, Arg 1, Msr 1 and Mrc⁻1; and blocks the upregulation of p-PTEN, p-NF-κB, p-PI3K, p-Akt, p-p38 and ERK1/2. Leupeptin hemisulfate inhibits NO, ROS, proinflammatory cytokines, the IFN-γ/IL-10 ratio, phagolysosome fusion, mammalian lysosomal hydrolase activity and SARS-CoV-2 replication; and reverses impaired autophagic flux. Leupeptin hemisulfate is applicable to research related to chronic inflammatory diseases, edema, skin tumorigenesis, COVID-19 and respiratory infections.

Indomethacin (Indometacin) is a potent, orally active COX1/2 inhibitor with IC₅₀ values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin has anticancer activity and anti-infective activity. Indomethacin can be used for cancer, inflammation and viral infection research.

2,2'-Biphenol (o,o'-Biphenol) is an anti-inflammatory agent and the major non-protein-bound phenolic metabolite activated by rat bone marrow homogenate and hydrogen peroxide. 2,2'-Biphenol inhibits lipopolysaccharide (LPS) (HY-D1056)-induced COX-2 mRNA and protein expression. 2,2'-Biphenol suppresses the binding of AP-1 and NF-κB to their respective consensus sequences. 2,2'-Biphenol is applicable to research related to inflammation.

Moracin G is a plant-derived kinase modulator and receptor ligand that forms stable bindings with multiple key proteins (AKT1, COX2 and Estrogen receptor 1) and competitively inhibits the activity of specific kinases. By binding to MELK to disrupt cell cycle regulation, Moracin G impairs the survival and proliferation of cancer cells, induces cancer cell apoptosis, and thereby exerts anti-tumor potential. Moracin G can be used in research related to periodontitis and breast cancer.

COX-2-IN-67 is an orally active, blood-brain barrier permeable multi-target inhibitor that potently targets COX-2 (IC₅₀=0.07 μM), hCA IX (K_i=62.7 nM) and hBuChE (IC₅₀=0.47 μM). COX-2-IN-67 alleviates oxidative stress and liver stress, improves glucose homeostasis and insulin sensitivity, and optimizes lipid profiles. Meanwhile, COX-2-IN-67 effectively reduces the levels of neuroinflammatory markers and improves hippocampus-dependent cognitive function in a high-fat diet-induced rat model. COX-2-IN-67 can be used for the research of metabolic dysfunction-associated mild cognitive impairment.

Celecoxib,a selective and BBB-permeable non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC₅₀ of 40 nM.

Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.

GY4137 is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GY4137 can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity.

Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study.

Gallic acid (3,4,5-Trihydroxybenzoic acid) is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2). Gallic acid has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities.

Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC₅₀s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selective COX-1 inhibitor with an IC₅₀ value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers.

Sodium propionate is an orally active short-chain fatty acid. Sodium propionate can be produced by intestinal bacteria from the metabolism of dietary fiber. Sodium propionate increases PPAR-γ, inhibits NF-κB activation, and reduces COX-2 expression and NO production. Sodium propionate also induces Apoptosis and Autophagy. Sodium propionate reduces HSV-1-induced keratitis. Sodium propionate has anticancer effects against glioblastoma. Sodium propionate exhibits neuroprotective, antioxidant, and anti-inflammatory activities. Sodium propionate can be used in the research of spinal cord injury and Alzheimer's disease.

Catechin ((+)-Catechin) inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 1.4 μM.

20(S)-Ginsenoside Rg3 is the main component of Panax ginseng C. A. Meyer. Ginsenoside Rg3 inhibits Na⁺ and hKv1.4 channel with IC₅₀s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.

(-)-Epicatechin inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.

Meloxicam is a non-steroidal antiinflammatory agent that can pass through the blood-brain barrier, inhibits COX activity, with IC₅₀s of 0.49 μM and 36.6 μM for COX-2 and COX-1, respectively.

Naproxen is a COX-1 and COX-2 inhibitor with IC₅₀s of 8.72 and 5.15 μM, respectively in cell assay.