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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-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 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. -
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-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. -
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 Specific Inhibitor
SC-236 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 10 nM and also acts as a PPARγ agonist. It effectively suppresses activator protein-1 (AP-1) through the inhibition of c-Jun NH2-terminal kinase, demonstrating significant anti-inflammatory effects. SC-236 has been shown to reduce ERK phosphorylation in murine models, highlighting its potential for investigating inflammatory pathways and therapeutic interventions. -
COX-2 Inhibitor
Humulone, a prenylated phloroglucinol derivative, is a selective inhibitor of cyclooxygenase-2 (COX-2). It demonstrates significant anti-inflammatory properties and serves as a positive modulator of GABAA receptors at low micromolar concentrations. Additionally, Humulone is known to inhibit bone resorption and exhibits antioxidant, anti-angiogenic, and pro-apoptotic activities, making it valuable for various research applications in inflammation and cancer studies. -
COX-2 Inhibitor
DuP-697 is a potent, irreversible, and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 10 nM for human COX-2 and 800 nM for COX-1. This compound demonstrates significant antiproliferative effects on HT29 colorectal cancer cells with an IC50 of 42.8 nM, as well as antiangiogenic and pro-apoptotic activities. By inhibiting prostaglandin synthesis, DuP-697 offers potential applications in studies related to inflammation, cancer, and fever reduction. -
COX Inhibitor
Metamizole sodium is a potent cyclooxygenase (COX) inhibitor that exhibits significant anti-inflammatory, analgesic, and antipyretic properties. This compound not only inhibits cell proliferation but also promotes apoptosis in various cell types. Additionally, Metamizole sodium serves as a spasmolytic agent, making it a valuable tool for research applications aimed at pain relief and the study of inflammatory processes. Its multifunctional activities contribute to its utility in diverse areas of biomedical research. -
COX-2 Inhibitor
COX-2-IN-43 is a selective COX-2 inhibitor with an IC50 of 0.247 μM for COX-2 and 0.983 μM for COX-1. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and colonization while inducing apoptosis. It is valuable for research applications targeting inflammatory diseases and cancer therapeutics. -
COX Inhibitor
Metamizole hemimagnesium is a cyclooxygenase (COX) inhibitor with anti-inflammatory and antioxidant properties. This compound effectively reduces body temperature and has been shown to decrease levels of C-reactive protein (CRP) and interleukin 6 (IL-6). Metamizole hemimagnesium also inhibits cell proliferation and promotes apoptosis. It is utilized in research applications focused on inflammation and fever modulation. -
COX Inhibitor
Ketorolac hydrochloride is a non-steroidal anti-inflammatory drug (NSAID) that acts as a nonselective inhibitor of cyclooxygenase (COX), with IC50 values of 20 nM for COX-1 and 120 nM for COX-2. It is utilized in the study of various ophthalmic conditions, including allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Additionally, Ketorolac hydrochloride functions as a DDX3 inhibitor, making it relevant for cancer research applications. -
COX Inhibitor
Meloxicam sodium is a selective cyclooxygenase (COX) inhibitor, primarily targeting COX-2 with an IC50 of 0.49 μM while exhibiting a higher IC50 of 36.6 μM for COX-1. This non-steroidal anti-inflammatory agent is capable of crossing the blood-brain barrier, making it suitable for research applications involving central nervous system inflammation and pain management. Meloxicam sodium is widely utilized in studies assessing the efficacy of anti-inflammatory therapies. -
COX-1/2 Inhibitor
Taraxerol acetate is an inhibitor of COX-1 and COX-2, exhibiting IC50 values of 116.3 μM and 94.7 μM, respectively. This compound demonstrates notable anticancer properties and has been shown to induce apoptosis in cancer cells. Taraxerol acetate is valuable for research applications focusing on inflammation, pain relief, and cancer treatment mechanisms. -
COX-2/NLRP3 Inhibitor
COX-2/NLRP3-IN-1 is a selective inhibitor targeting both COX-2 and the NLRP3 inflammasome, with an IC50 of 1.53 μM for COX-2. This compound exhibits notable anti-inflammatory properties by disrupting the NF-κB/NLRP3 signaling pathway, making it a valuable tool for research into inflammatory diseases. It is suitable for studying the roles of COX-2 and NLRP3 in various biological processes and therapeutic interventions. -
COX Inhibitor
(±)-Aiphanol is a potent inhibitor of cyclooxygenase (COX) enzymes, specifically targeting COX-1 (IC50 = 1.9 μM) and COX-2 (IC50 = 9.9 μM). This compound displays significant anti-inflammatory properties and further inhibits vascular endothelial growth factor receptor 2 (VEGFR2) with an IC50 of 0.92 μM. By impeding both COX-2 and VEGFR2 pathways, (±)-Aiphanol effectively blocks angiogenesis and induces apoptosis, making it a valuable tool in the study of inflammatory diseases and cancer research. The compound demonstrates oral bioactivity, enhancing its potential for in vivo applications. -
COX Inhibitor
Indomethacin farnesil is a prodrug of indomethacin, primarily targeting cyclooxygenase (COX) enzymes. This potent, blood-brain barrier-permeable inhibitor exhibits nonselective activity against COX-1 and COX-2, with IC50 values of 18 nM and 26 nM, respectively. Indomethacin farnesil has been shown to disrupt autophagic flux by impairing lysosomal function, making it useful for investigating inflammatory pathways and autophagy-related processes in research applications. -
COX-2 Inhibitor/PPAR-γ Activator
Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury. -
COX-2 Inhibitor
Hexahydrocurcumin is a selective, orally active inhibitor of cyclooxygenase-2 (COX-2), demonstrating significant potential in anti-inflammatory applications. As one of the primary metabolites of curcumin, it exhibits antioxidant and anticancer properties, making it relevant for research in various therapeutic areas. Its selectivity towards COX-2 over COX-1 highlights its potential for minimizing gastrointestinal side effects often associated with non-steroidal anti-inflammatory drugs (NSAIDs). -
COX-2 Inhibitor
COX-2-IN-65 is a selective inhibitor of cyclooxygenase-2 (COX-2) with a reported IC50 of 10.24 μM. This compound exhibits antibacterial activity against Staphylococcus aureus and Escherichia coli, while also scavenging reactive oxygen species (ROS). COX-2-IN-65 is valuable for research applications focused on bacterial infections and inflammation pathways. -
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/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-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. -
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-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. -
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.

