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COX activator
Beta-Elemonic acid (3-Oxotirucallenoic Acid), a known triterpene isolated from Boswellia (Burseraceae), exhibits anti?inflammatory effects. -
COX2 Inhibitor
Iminostilbene is a well-characterized inhibitor of COX2 (Cyclooxygenase-2) with additional activity against PKM2 (Pyruvate Kinase M2). This compound effectively reduces the expression of COX2 and iNOS, as well as the release of pro-inflammatory cytokines such as IL-1β, IL-6, TNF-α, and MCP-1 in macrophages. Its ability to mitigate macrophage-mediated inflammatory responses makes iminostilbene a valuable reagent for investigating mechanisms of inflammation regulation, cardiovascular disease, including myocardial ischemia/reperfusion injury, and immune-related disorders. -
COX Inhibitor
Aspirin lithium is a potent, orally active, irreversible inhibitor of cyclooxygenase COX-1 and COX-2, exhibiting IC50 values of 5 and 210 μg/mL, respectively. This compound promotes apoptosis and inhibits the activation of NF-κB, making it valuable for studies on inflammation and cell death. Additionally, Aspirin lithium effectively inhibits platelet prostaglandin synthetase, providing potential protective effects against coronary artery and cerebrovascular thrombosis. -
COX Inhibitor
(E)-Ethyl p-methoxycinnamate is a COX inhibitor that exhibits significant anti-inflammatory properties. Isolated from Kaempferia galangal, this compound demonstrates both anti-neoplastic and anti-microbial activities. In vitro studies reveal that (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 with IC50 values of 1.12 μM and 0.83 μM, respectively, making it a valuable reagent for research in inflammatory and cancer-related studies. -
COX Inhibitor
Ketorolac hemicalcium is a non-steroidal anti-inflammatory drug (NSAID) that functions as a nonselective cyclooxygenase (COX) inhibitor, exhibiting IC50 values of 20 nM for COX-1 and 120 nM for COX-2. This compound is utilized in research related to allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain, as well as for its potential applications in cancer research due to its role as a DDX3 inhibitor. -
COX Inhibitor
Metamizole magnesium is an orally active cyclooxygenase (COX) inhibitor known for its key roles in reducing inflammation and pain. It exhibits significant anti-inflammatory and antioxidant activities, along with the ability to inhibit cell proliferation and promote apoptosis. Due to its antipyretic and analgesic properties, Metamizole magnesium is commonly utilized in various research applications aimed at investigating pain mechanisms and inflammatory responses. -
Topo I/COX-2 Inhibitor
Topo I/COX-2-IN-1 is an inhibitor of both Topoisomerase I and Cyclooxygenase-2 (COX-2). It demonstrates significant biological activity, with IC50 values of 0.24 μM for COX-2 and 4.42 μM for Topo I. This compound effectively induces apoptosis and inhibits the migration of cancer cells, showcasing potential applications in cancer research and therapy. -
Topo I/COX-2 Inhibitor
Topo I/COX-2-IN-2 is a potent dual-target inhibitor of Topoisomerase I (Topo I) and Cyclooxygenase-2 (COX-2), exhibiting inhibitory concentrations (IC50) of 0.90 μM and 2.31 μM, respectively. This compound induces apoptosis in cancer cells via the mitochondrial pathway, making it a valuable agent for research in cancer therapeutics and cell death mechanisms. Its dual activity supports investigations into the interplay between topoisomerase inhibition and inflammatory pathways in cancer progression. -
Celecoxib Analog
OSU-03013 is a Celecoxib analog that targets multiple pathways involved in cancer progression. It promotes apoptosis while enhancing E-cadherin expression and reduces β-catenin, c-myc, Wnt1, and N-cadherin levels. By inhibiting cell migration and invasion, OSU-03013 effectively regulates Wnt and mTOR signaling, leading to decreased proliferation of colon cancer cells. This compound is suitable for research focused on colon cancer and its underlying mechanisms. -
COX-1 Inhibitor
Ibuprofen sodium is a selective inhibitor of cyclooxygenase-1 (COX-1), exhibiting an IC50 value of 13 μM. This compound demonstrates significant biological activities, including inhibition of cell proliferation, angiogenesis, and induction of apoptosis. As a nonsteroidal anti-inflammatory agent and nitric oxide (NO) donor, ibuprofen sodium is valuable in research areas such as pain, inflammation, infection, immunology, and oncology. -
COX-2/MMP-7/TLR4 Inhibitor
Isofraxidin is a coumarin compound derived from *Acanthopanax senticosus* that exhibits anti-invasive and anti-inflammatory properties. It inhibits MMP-7 expression and suppresses cell invasion in human hepatoma cells by reducing ERK1/2 phosphorylation. Isofraxidin also downregulates the expression of iNOS and COX-2 and inhibits the formation of the TLR4/myeloid differentiation protein-2 (MD-2) complex. -
COX/LOX inhibitor
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. -
COX-1/COX-2 inhibitor
Glafenine is a non-selective, non-steroidal anti-inflammatory drug (NSAID) that inhibits both COX-1 and COX-2 enzymes. It exerts anti-inflammatory, anti-proliferative, and anti-migratory effects by suppressing the arachidonic acid metabolic pathway, thereby reducing prostaglandin production. Additionally, glafenine induces cell cycle arrest in vascular smooth muscle cells and endothelial cells and decreases the synthesis of the extracellular matrix protein tenascin. It is utilized in research related to inflammatory disorders, vascular restenosis, and cystic fibrosis. -
COX inhibitor
Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active, non-selective cyclooxygenase (COX) inhibitor. It exhibits analgesic, anti-inflammatory, and anti-cancer effects. As the active enantiomer of ketoprofen, Dexketoprofen trometamol is commonly used for the management of pain and inflammation, and it is also under investigation for its potential anticancer properties. -
COX-2 inhibitor
SC-58125 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.04 μM. It demonstrates antitumor activity both in vitro and in vivo and is effective in reducing inflammation-related edema. Additionally, SC-58125 possesses analgesic properties, making it a valuable compound for research in cancer, inflammation, and pain management. -
PPAR agonist
Lobeglitazone sulfate is a novel thiazolidinedione and an orally active agonist of peroxisome proliferator-activated receptors (PPARs), with EC50 values of 137.4 nM for PPARγ and 546.3 nM for PPARα. It also acts as an inhibitor of the ERK/JNK/Smad/NF-κB signaling pathways. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic activities, supporting its potential in the treatment of metabolic and inflammatory diseases. - 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.
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NSAID/COX inhibitor
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory drug (NSAID) that functions primarily by inhibiting cyclooxygenase (COX) enzymes, thereby reducing the synthesis of pro-inflammatory prostaglandins. In addition to its classical NSAID activity, Fenoprofen has been identified as a positive allosteric modulator (PAM) of melanocortin receptors (MCRs), enhancing MCR-mediated signaling. Fenoprofen also promotes ERK1/2 activation in HEK293T cells, suggesting additional modulation of intracellular signaling pathways involved in inflammation and cellular proliferation. -
PPAR agonist
Lobeglitazone is a novel thiazolidinedione-class compound and an orally active dual agonist of peroxisome proliferator-activated receptors (PPARs), with EC₅₀ values of 137.4 nM for PPARγ and 546.3 nM for PPARα. In addition to its metabolic effects, Lobeglitazone functions as an inhibitor of multiple pro-inflammatory and pro-fibrotic signaling pathways, including ERK, JNK, Smad, and NF-κB. Lobeglitazone exhibits a broad range of pharmacological activities, including anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic effects. These properties make it a promising candidate for therapeutic research in metabolic syndrome, type 2 diabetes, cardiovascular disease, and fibrosis-related conditions. -
COX-1/HDAC/Tyrosinase Inhibitor
Gnetol is a bioactive phenolic compound isolated from the root of *Gnetum montanum* with diverse pharmacological properties. It potently inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 0.78 μM and exhibits histone deacetylase (HDAC) inhibitory activity. Gnetol is also a strong tyrosinase inhibitor, with an IC₅₀ of 4.5 μM against murine tyrosinase, leading to suppression of melanin biosynthesis. In addition to its antioxidant, antiproliferative, anticancer, and hepatoprotective effects, Gnetol modulates metabolic enzymes in a concentration-dependent manner, including α-amylase, α-glucosidase, and adipogenesis pathways, making it a promising candidate for research in oncology, dermatology, and metabolic disorders. -
COX-1/2 Inhibitor
Cudraflavone B is a prenylated flavonoid that functions as a dual inhibitor of COX-1 and COX-2, demonstrating significant anti-inflammatory and anti-tumor activity. This compound inhibits the translocation of nuclear factor κB (NF-κB) in macrophages, leading to decreased tumor necrosis factor α (TNFα) gene expression and secretion. Additionally, Cudraflavone B induces the mitochondrial apoptotic pathway while activating MAPK signaling pathways, including p38 and ERK, and upregulating SIRT1 expression. These mechanisms contribute to its efficacy in attenuating the growth of human oral squamous cell carcinoma cells, making it a valuable tool for cancer research. -
COX Inhibitor
Oxaprozin is a potent, orally active cyclooxygenase (COX) inhibitor, demonstrating IC50 values of 2.2 μM for human platelet COX-1 and 36 μM for IL-1-stimulated human synovial cell COX-2. This compound exhibits significant anti-inflammatory activity and is known to inhibit the activation of NF-κB, promoting cell apoptosis. The inhibition of the Akt/IKK/NF-κB signaling pathway is a key mechanism underlying its anti-inflammatory properties, making Oxaprozin valuable for research in inflammation and related disorders. -
Dual COX-2/EGFR Inhibitor
Melafolone is a potent dual inhibitor of COX-2 and EGFR, displaying IC50 values of 13.2 μM for COX-2 and 17.4 μM for EGFR. This compound enhances the efficacy of anti-PD-1 therapy by promoting vascular normalization and downregulating PD-L1 through the PI3K/Akt signaling pathway in Lewis lung carcinoma (LLC) and CMT167 models. Melafolone is suitable for applications in lung cancer research. -
COX Inhibitor
Oxaprozin potassium is a potent cyclooxygenase (COX) inhibitor, demonstrating IC50 values of 2.2 μM for human platelet COX-1 and 36 μM for IL-1-stimulated human synovial cell COX-2. It not only exhibits anti-inflammatory activity but also inhibits the activation of NF-κB, inducing cell apoptosis. The inhibition of the Akt/IKK/NF-κB pathway is a key mechanism contributing to its anti-inflammatory effects, making it a valuable tool for research in inflammation and related cellular processes. -
COX-2 Inhibitor
Withangulatin A is a selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating significant potential in the modulation of inflammatory and tumorigenic processes. This compound also interferes with the MAPK, NF-κB, and Akt/mTOR/p70S6K signaling pathways, thereby exhibiting notable antitumor and anti-inflammatory activities. Additionally, Withangulatin A has been shown to possess trypanocidal effects, making it useful for research in cancer, inflammation, and parasitic diseases. -
COX-2 Inhibitor
Ataquimast is a selective COX-2 inhibitor that effectively suppresses the release of leukotrienes, TNF-α, and GM-CSF. Its mechanism supports research into inflammatory responses and has potential applications in the study of advanced estrogen receptor-positive breast cancer. This compound may aid in elucidating the role of COX-2 in tumor progression and therapeutic resistance. -
COX-2 Inhibitor
COX-2-IN-60 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating an IC50 of 0.06 μM and approximately 100-fold selectivity over COX-1. This compound significantly reduces oxidative stress and neuroinflammatory cytokines, effectively counteracting epileptogenesis. In preclinical studies utilizing a pilocarpine-induced seizure mouse model, COX-2-IN-60 exhibited substantial anticonvulsant effects while protecting against hippocampal injury. Its application in research relates to neuroinflammatory pathways and epilepsy mechanisms. -
ROS/iNOS/TNF-α/COX-2 Inhibitor
Callistephin chloride is an anthocyanin that functions as an inhibitor of reactive oxygen species (ROS) and nitric oxide synthase (iNOS), as well as tumor necrosis factor-alpha (TNF-α) and cyclooxygenase-2 (COX-2). This compound regulates the expression of inflammatory and apoptosis-related proteins by inhibiting p38 phosphorylation, thereby enhancing the protective effects against microglial cell damage. Callistephin chloride also significantly reduces ROS levels, mitigates glutamate excitotoxicity, and provides neuroprotection to cerebellar granule neurons. Additionally, it inhibits the proliferation and metastasis of breast cancer cells through the induction of apoptosis. -
COX-2/HDAC Inhibitor
Andrographidine E is an inhibitor of cyclooxygenase-2 (COX-2) and histone deacetylases (HDAC), with an IC50 of 19 μM for COX-2 and a strong affinity for HDAC1 and HDAC3. This compound selectively binds to macrophages, suggesting its potential as an immunotargeting agent. Andrographidine E is valuable for research applications focused on inflammation and immune modulation. -
COX-1/cAMP Phosphodiesterase Inhibitor
Triflusal is a dual inhibitor of Cyclooxygenase-1 (COX-1) and cAMP phosphodiesterase, which penetrates the blood-brain barrier. It effectively inhibits platelet aggregation, nuclear factor kappa B (NF-κB) activation, inducible nitric oxide synthase (iNOS) activity, and prostaglandin synthesis in ischemic tissues. Additionally, Triflusal enhances neutrophil nitric oxide production, endothelial nitric oxide synthase (eNOS) expression, and constitutive nitric oxide synthase (cNOS) activity. This compound is valuable for investigating thromboembolic and ischemic diseases of the cardiovascular and cerebrovascular systems, as well as Alzheimer's disease pathology. -
COX Inhibitor
Pentagamavunon-1 (PGV-1) is a COX-2 inhibitor that modulates multiple molecular pathways to induce apoptosis. This Curcumin analog exhibits notable oral bioactivity and suppresses key angiogenic factors, including vascular endothelial growth factor (VEGF). Additionally, PGV-1 inhibits NF-κB activation, highlighting its potential in cancer research and therapeutic applications targeting inflammation and tumor progression. -
EGFR/HER2/CDK9/COX-2 Inhibitor
CDK9-IN-41 is a potent inhibitor of CDK9, EGFR, HER2, and COX-2, exhibiting IC50 values of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM respectively. This compound demonstrates significant antitumor activity across various cancer cell lines, including leukemia, colon, melanoma, ovarian, and breast cancer. It serves as a valuable tool for exploring the role of these kinases in cancer biology and therapeutic applications. -
COX Inhibitor
[8]-Shogaol is a potent inhibitor of cyclooxygenase (COX), specifically targeting COX-2 with an IC50 of 17.5 μM. This compound exhibits significant antiplatelet properties (IC50=5 μM) and demonstrates anti-cancer and anti-inflammatory activities. Additionally, [8]-Shogaol modulates key signaling pathways by inhibiting TAK1, IKK, and Akt, thereby influencing MAPK signaling and alleviating synovitis. Its unique pharmacological profile makes it a valuable reagent for research in cancer, inflammation, and cardiovascular diseases. -
COX Inhibitor
Diclofenac potassium is a potent nonselective inhibitor of cyclooxygenase (COX) enzymes, demonstrating IC50 values of 4 nM for human COX-1 and 1.3 nM for human COX-2 in CHO cells, along with 5.1 μM and 0.84 μM for ovine COX-1 and COX-2, respectively. This reagent exhibits significant anti-inflammatory properties and is particularly effective in inducing apoptosis in neural stem cells through the activation of the caspase cascade. It is widely used in research studies focusing on inflammatory pathways and neural stem cell biology. -
iNOS/COX-2 Inhibitor
Ermanin is a flavonoid extracted from Tanacetum microphyllum, known for its potent inhibitory effects on inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Its biological activities include anti-inflammatory, anti-tuberculous, and anti-viral/bacterial properties, making it a valuable reagent in research related to inflammation and infectious diseases. Ermanin is useful for exploring the pathways associated with nitric oxide production and prostaglandin synthesis in various biological contexts. -
COX Inhibitor
α-Spinasterol is a selective inhibitor of cyclooxygenase enzymes COX-1 and COX-2, exhibiting IC50 values of 16.17 μM and 7.76 μM, respectively. This compound demonstrates a range of biological activities, including antibacterial, anti-inflammatory, antidepressant, and antioxidant effects. Furthermore, it can effectively cross the blood-brain barrier and has shown potential in improving diabetes in murine models, making it a valuable tool for research in inflammatory disorders and neurological conditions. -
COX-1/2 Inhibitor
2-(p-Tolyl)propanoic acid is a selective inhibitor of COX-1 and COX-2 enzymes, displaying IC50 values of 38.23 μM and 64.30 μM, respectively. This compound exhibits antimicrobial properties and is relevant for research on bacterial pathogens such as Escherichia coli, Enterococcus faecalis, Listeria monocytogenes, and Staphylococcus aureus. Its mechanism of action positions it as a valuable tool for investigating inflammatory processes and antimicrobial resistance in various biological studies. -
COX1/2 Inhibitor
Indomethacin sodium is a potent inhibitor of cyclooxygenase enzymes COX-1 and COX-2, exhibiting IC50 values of 18 nM and 26 nM, respectively. This compound demonstrates significant anticancer and anti-infective properties, making it valuable in various biological research applications. Indomethacin sodium is essential for investigating mechanisms related to cancer treatment, inflammation, and viral infections. -
COX-2/Carbonic Anhydrase Inhibitor
Polmacoxib is a novel, orally active nonsteroidal anti-inflammatory drug (NSAID) that acts as a dual inhibitor of cyclooxygenase-2 (COX-2) and carbonic anhydrase, with an IC50 value of approximately 0.1 μg/ml for COX-2. It exhibits significant biological activity by inhibiting the growth of colorectal adenomas and tumors in mouse models, making it a promising tool for cancer research. Polmacoxib is valuable for studying the roles of COX-2 and carbonic anhydrase in cancer biology and inflammation. -
COX-2 Inhibitor
COX-2-IN-30 is a benzenesulfonamide derivative that functions as a potent selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 49 nM and also inhibits 5-lipoxygenase (5-LOX) with an IC50 of 2.4 μM. Additionally, it affects human carbonic anhydrase isoforms IX and XII, displaying nanomolar Ki values. This compound demonstrates significant analgesic and anti-inflammatory properties while maintaining a favorable gastrointestinal safety profile, making it useful for research in inflammation, pain relief, and related gastrointestinal studies. -
COX Inhibitor
Aspirin DL-lysine is a lysine-conjugated derivative of aspirin that functions primarily as a cyclooxygenase (COX) inhibitor. This compound effectively inhibits the synthesis of thromboxane A2 (TXA2) in platelets, leading to a reduction in platelet activation and aggregation. Aspirin DL-lysine is valuable for research applications focused on thrombin generation, particularly in clinical studies involving unstable angina pectoris. -
COX-2 Inhibitor
APHS is a selective and covalent inhibitor of cyclooxygenase-2 (COX-2) that exerts neuroprotective effects. By acetylating serine 516 in the active site of COX-2, APHS effectively inhibits prostaglandin production, which is often upregulated in colorectal cancer. In addition to its role as a COX-2 inhibitor, APHS also co-inhibits the WNT signaling pathway, contributing to its anti-tumor mechanisms. This compound is valuable for research into cancer biology and neuroprotection. -
5-LO/COX-2/DPP-4 Inhibitor
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. -
COX-2 Inhibitor
Thymohydroquinone is a selective inhibitor of cyclooxygenase-2 (COX-2) with noted anti-SARS-CoV-2 activity. It exhibits cytotoxic properties, antiproliferative effects, and the ability to suppress tumor growth in various cancer models. This compound is applicable in research focused on squamous cell carcinoma, fibrosarcoma, and the pathogenesis and treatment of COVID-19 caused by SARS-CoV-2. -
COX-1 Inhibitor
NCX 466 is a selective inhibitor of COX-1 and COX-2, demonstrating notable anti-inflammatory and analgesic properties. It functions as a nitric oxide (NO) donor, enhancing microcirculation while exerting antioxidant effects. NCX 466 effectively reduces levels of transforming growth factor-β (TGF-β) and oxidative stress markers, including thiobarbituric acid reactive substances (TBARS) and 8-hydroxy-2'-deoxyguanosine (8-OHdG). Furthermore, it mitigates leukocyte recruitment during inflammatory responses by decreasing myeloperoxidase (MPO) activity, contributing to the prevention of bleomycin-induced pulmonary fibrosis in murine models. -
COX-2 Inhibitor
Hirsutanonol, a diarylheptanoid derived from the bark of Alnus hirsute var. sibirica, functions primarily as an inhibitor of cyclooxygenase-2 (COX-2). This compound exhibits significant anti-filarial activity, demonstrated by an IC50 value of 44.11 μg/mL against microfilariae. Hirsutanonol is valuable in research focused on inflammation reduction and parasitic disease interventions. -
COX-1 Inhibitor
Dihydroflavokawin B is a selective COX-1 inhibitor, exhibiting an IC50 of 1.22 μM, with moderate effects on COX-2 and 5-LOX. This compound demonstrates significant activity against the promastigote forms of Leishmania panamensis and Leishmania braziliensis, making it a valuable tool for leishmaniasis research. Additionally, Dihydroflavokawin B inhibits rabbit platelet aggregation induced by arachidonic acid, platelet-activating factor, and adenosine diphosphate, highlighting its potential for in vitro anti-inflammatory studies. -
COX Inhibitor
Serratiopeptidase is a zinc-containing metalloprotease that primarily acts as a cyclooxygenase (COX) inhibitor. It effectively reduces the release of inflammatory mediators such as prostaglandins and interleukins, alleviating pain and swelling. In addition to its anti-inflammatory properties, Serratiopeptidase exhibits mucolytic, antibiofilm, and wound-healing activities. Its enzymatic action allows it to dissolve fibrin and blood clots, while also demonstrating potential anti-Alzheimer's effects by degrading amyloid fibrils. Furthermore, Serratiopeptidase shows cytotoxicity against colon cancer cells, making it a versatile reagent for research applications in inflammation and oncology.

