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COX-2/15-LOX Inhibitor
COX-2/15-LOX-IN-5 is a potent dual inhibitor of cyclooxygenase-2 (COX-2) and 15-lipoxygenase (15-LOX). This compound effectively attenuates lipopolysaccharide-induced NF-κB activation in RAW 264.7 macrophages, highlighting its role in modulating inflammatory responses. COX-2/15-LOX-IN-5 exhibits significant anti-inflammatory and antioxidant properties, making it a valuable tool for research into inflammatory diseases and other related biological processes. -
COX-2 Inhibitor
COX-2-IN-16 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 102 µM. This compound effectively inhibits nitric oxide (NO) production and exhibits significant anti-inflammatory activity. COX-2-IN-16 is suitable for research applications focused on inflammation and pain pathways. -
COX Inhibitor
Florifenine is a selective cyclooxygenase (COX) inhibitor that demonstrates significant anti-inflammatory activity. It effectively inhibits thromboxane B2 (TXB2) production in human whole blood with an IC50 value of 32.5 nM. Florifenine has been shown to reduce neutrophil migration and lower prostaglandin E2 (PGE2) levels in inflamed tissues, including ear edema and air pouch inflammation induced by Zymosan. This compound serves as a valuable tool for investigations in anti-inflammatory research. -
Lipoxygenase/COX Inhibitor
SKF-105809 is a dual inhibitor of lipoxygenase and cyclooxygenase (COX), targeting key enzymes involved in the inflammatory pathway. This compound demonstrates a significant reduction in edema and inflammatory cell infiltration in murine models of ear, paw, and peritoneal inflammation. Additionally, SKF-105809 reduces the production of acute-phase reactive proteins in models of arthritis and exhibits analgesic effects in abdominal contraction assays while preventing ulceration. Its applications extend to the study of inflammatory and immune system disorders, including peritonitis and arthritis. -
COX-2 Inhibitor
COX-2-IN-14 is a highly selective inhibitor of cyclooxygenase-2 (COX-2). This compound demonstrates effective binding at the active site of COX-2, as confirmed by co-crystal studies. In vivo, COX-2-IN-14 exhibits significant anti-inflammatory properties, notably reducing ear edema and myeloperoxidase (MPO) activity in mouse models. It serves as a valuable tool for research into inflammatory processes and the development of treatments targeting COX-2-related conditions. -
COX-1/2 Inhibitor
K-80001 is a selective COX-1/2 inhibitor that demonstrates potent inhibition with IC50 values of 82.9 μM, 3.4 μM, and 1.2 μM against RXRα, COX-1, and COX-2, respectively. Its mechanism involves binding to the RXRα receptor, contributing to its pharmacological profile. K-80001 is primarily utilized in studies focusing on pain management and inflammatory processes, making it a valuable tool for researchers investigating the roles of cyclooxygenases in various biological contexts. -
COX-2 Inhibitor
Parameritannin A-1 is a tetrameric proanthocyanidin (PAC) that selectively inhibits cyclooxygenase-2 (COX-2). Isolated from the bark of Parameria laevigata Moldenke, this compound exhibits anti-inflammatory properties and is valuable for studies related to inflammatory diseases. Additionally, Parameritannin A-1 has been shown to inhibit phospholipase A2 (PLA2) activity, further supporting its potential applications in biochemical research involving inflammatory pathways and lipid metabolism. -
COX-2 Inhibitor
Lefucoxib is a selective inhibitor of cyclooxygenase-2 (COX-2), an enzyme involved in the inflammatory process. This compound demonstrates significant anti-inflammatory activity, making it valuable for research applications related to osteoarthritis and rheumatoid arthritis. Its selective targeting of COX-2 allows for a focus on the inflammatory pathways involved in these conditions. -
COX-1/2 Inhibitor
COX-1/2-IN-3 is an inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). This compound exhibits significant anti-inflammatory activity while maintaining a low toxicity profile. It serves as a valuable tool for research in inflammation and pain pathways, providing insights into therapeutic applications for inflammatory diseases. -
COX-2/TAK1-NF-κB Inhibitor
BPD is a selective inhibitor of COX-2 and TAK1-NF-κB, exhibiting an IC50 of 18.5 μM for COX-2. This compound effectively reduces the transcriptional expression of key pro-inflammatory cytokines, including iNOS, TNF-α, IL-6, and IL-1β, thereby demonstrating notable anti-inflammatory properties. BPD has been shown to inhibit carrageenan-induced paw edema and mitigate LPS-induced septic mortality, making it a valuable tool for research in inflammation and related pathways. -
COX-1 Inhibitor
Parsalmide is a COX-1 inhibitor that exhibits oral activity as a non-steroidal anti-inflammatory and gastroprotective agent, demonstrating an IC50 value of 9.92 μM for COX-1 and 155 μM for COX-2. This compound effectively prevents gastric injury and reduces edema, making it valuable for studies related to arthritis and inflammation. Its dual-action profile positions Parsalmide as a promising candidate for research focused on gastrointestinal protection alongside anti-inflammatory applications. -
COX-2/PI3K Inhibitor
COX-2/PI3K-IN-2 is a potent inhibitor targeting both COX-2 and PI3K pathways, exhibiting an IC50 value of 2.78 nM for PI3K and a Ki value of 3.02 nM for COX-2. This compound demonstrates significant anti-inflammatory and anti-cancer activities, making it valuable for research in oncology and inflammatory disease studies. Its dual-target mechanism provides insights into the therapeutic potential of modulating these critical pathways. -
COX-2 inhibitor
Lixadesiran is an siRNA designed to inhibit cyclooxygenase-2 (COX-2) by targeting its mRNA. This compound is part of the STP705 formulation, which includes two siRNA oligonucleotides, with Pixofisiran targeting TGF-β1. Lixadesiran's mechanism of action contributes to the modulation of inflammatory pathways, making it relevant for research in cancer and fibrosis studies. -
COX Inhibitor
Murraol is a coumarin compound that acts as a cyclooxygenase (COX) inhibitor. It exhibits inhibitory effects on both COX and lipoxygenase enzymatic activities, contributing to its potential anti-inflammatory properties. Additionally, Murraol demonstrates an inhibitory effect on the growth of cancer cells, making it a valuable tool for cancer research and therapeutic investigations. -
COX Inhibitor
4-Methylamino antipyrine hydrochloride is a COX inhibitor and an active metabolite of Metamizole, a pyrazolone non-steroidal anti-inflammatory drug (NSAID). It exhibits analgesic and antipyretic properties, making it useful in the management of pain and fever. While its anti-inflammatory effects are relatively weak, this compound serves as an important tool in research applications focusing on pain relief and inflammatory pathways. -
COX Inhibitor
Pifoxime is a potent inhibitor of cyclooxygenase (COX-1 and COX-2), classified as a non-steroidal anti-inflammatory drug (NSAID). It demonstrates significant anti-inflammatory properties, making it suitable for various research applications, including neuropsychiatric studies. Pifoxime's ability to modulate inflammation can provide valuable insights into the underlying mechanisms of inflammatory processes in different biological contexts. -
COX-2 Inhibitor
Esculentic acid is a selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting significant anti-inflammatory properties. As a pentacyclic triterpenoid derived from the Chinese herb Phytolacca esculenta, it is valuable in research focused on inflammation and related pathways. This compound is applicable in studies targeting the modulation of COX-2 activity and its implications in various inflammatory conditions. -
COX Inhibitor
SC-75416 is a selective inhibitor of cyclooxygenase-2 (COX-2), primarily designed to mitigate pain and inflammation. Its pharmacokinetic/pharmacodynamic (PK/PD) model has been utilized to develop clinical trial simulations that support its analgesic efficacy, demonstrated to exceed that of ibuprofen in post-oral surgery pain models. The results from these simulations and subsequent clinical trials indicate that SC-75416 offers superior pain relief, underscoring its potential as a valuable therapeutic agent for managing postoperative pain. -
COX-1/2 Inhibitor
Diclofenac amide is a prodrug that functions as an oral inhibitor of cyclooxygenase-1 and -2 (COX-1/2), effectively reducing the synthesis of prostaglandins and thromboxanes. This compound demonstrates significant anti-inflammatory activity in the carrageenan-induced rat paw edema model while preserving gastric integrity, making it a valuable tool for studying inflammation and pain mechanisms. Its favorable safety profile and effectiveness position it as a promising candidate in pharmacological research. -
COX Inhibitor
Bromfenac is a potent and orally active inhibitor of cyclooxygenases (COX-1 and COX-2), exhibiting IC50 values of 5.56 nM and 7.45 nM, respectively. This selective COX inhibition makes Bromfenac valuable in the study of ocular inflammation and pain management. Its effectiveness in reducing inflammation positions it as a useful tool for researchers investigating inflammatory pathways in various biological contexts. -
COX
C2 Ceramide (d14:1/2:0) is a lipid molecule that selectively targets cyclooxygenase-2 (COX-2). This compound demonstrates a robust binding affinity for the COX-2 protein, making it a valuable tool for studying COX-2 overexpression in various disease contexts. C2 Ceramide (d14:1/2:0) can be utilized in research focused on inflammatory pathways and potential therapeutic interventions involving COX-2 modulation. -
COX Inhibitor
Naproxen ethyl ester is a nonsteroidal anti-inflammatory drug that functions primarily as a cyclooxygenase (COX) inhibitor. This compound effectively alleviates pain, fever, swelling, and stiffness by obstructing the actions of COX enzymes. The R-(-)-isomer of Naproxen ethyl ester is noted for its enhanced immunogenicity, demonstrating a Michaelis-Menten constant (K(M)) of 6.67 mM and exhibiting a catalytic efficiency that is 5.8 x 10^4 times greater than that of non-catalytic reactions. This compound is useful in pain management and inflammation research. -
COX-1 Inhibitor
COX-1-IN-5 is a highly selective COX-1 inhibitor, demonstrating an IC50 of 1 nM for COX-1 and greater than 0.1 μM for COX-2, thereby showing over 1000-fold selectivity for COX-1. This compound exhibits significant anti-inflammatory, antipyretic, analgesic, antithrombotic, and potential anti-cancer properties. COX-1-IN-5 is suitable for investigating COX-mediated diseases, including inflammatory conditions and pain. Additionally, when radiolabeled with 11C, it serves as a selective PET tracer for in vivo imaging of COX-1 distribution and target engagement. -
COX Inhibitor
Flunoxaprofen is an orally active cyclooxygenase (COX) inhibitor that exhibits significant anti-inflammatory properties. In preclinical models, such as rat paw edema assays, Flunoxaprofen has demonstrated efficacy in reducing inflammation. This compound may be utilized in research focused on immune system disorders, including arthritis and related inflammatory conditions. -
COX-2 Inhibitor
COX-2-IN-19 is a potent inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 value of 1.76 μM. This compound demonstrates significant in vivo anti-inflammatory activity, making it a valuable tool for research in inflammation and pain pathways. COX-2-IN-19 is suitable for studies focused on the modulation of COX-2-related biological processes in various disease models. -
COX Inhibitor
COX-1/2-IN-4 is a dual inhibitor of cyclooxygenase enzymes COX-1 and COX-2, exhibiting IC50 values of 0.239 μM and 0.191 μM, respectively. This compound demonstrates moderate anticancer activity against COLO205 and B16F1 cancer cell lines, with IC50 values of 30.79 μM and 74.15 μM. It serves as a valuable tool for research into the roles of COX enzymes in inflammation and cancer. -
COX-2/15-LOX Inhibitor
COX-2/15-LOX-IN-1 is a dual inhibitor of cyclooxygenase-2 (COX-2) and 15-lipoxygenase (15-LOX), exhibiting IC50 values of 10.65 μM for COX-1, 0.075 μM for COX-2, and 2.98 μM for 15-LOX. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research into inflammatory pathways and related diseases. Its ability to modulate key enzymes involved in arachidonic acid metabolism positions COX-2/15-LOX-IN-1 as a promising candidate for therapeutic investigation in inflammatory conditions. -
COX-2 Inhibitor
COX-2-IN-34 is a selective and orally active inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 0.42 μM. This compound demonstrates anti-inflammatory properties without the associated gastric ulcer toxicity often seen with non-selective COX inhibitors. COX-2-IN-34 is suitable for research applications focused on inflammation and related pathways. -
COX Inhibitor
ZXX2-77 is a selective inhibitor of cyclooxygenase-1 (COX-1) from the benzenesulfonylanilide compound class. It demonstrates significant COX-1 inhibitory activity in vitro, making it a candidate for pain management without the gastrointestinal side effects commonly associated with traditional analgesics. While its low oral absorption contributes to a reduced analgesic effect in vivo, its unique profile highlights the potential for developing effective COX-1 selective inhibitors that mitigate gastric damage. Further exploration of ZXX2-77 and its derivatives may lead to new therapeutic options for pain relief. -
COX-2 Inhibitor
COX-2-IN-40 is a selective COX-2 inhibitor with an IC50 value of 14.86 μM. This compound is primarily utilized in the investigation of chronic pain mechanisms and related therapeutic approaches. Its inhibition of COX-2 activity makes it a valuable tool for research into inflammatory processes and pain management strategies. -
COX-2 Inhibitor
COX-2-IN-29 is a selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 0.005 μM. This compound demonstrates significant anti-inflammatory activity, making it valuable in research focusing on pain modulation and inflammatory disease models. Its oral bioavailability further supports its potential utility in pharmacological studies and therapeutic applications targeting COX-2-related pathways. -
COX-2 Inhibitor
Mefenamic acid-d4 is a deuterated form of Mefenamic acid, which acts as a selective competitive inhibitor of cyclooxygenase-2 (COX-2). This NSAID exhibits significant anti-inflammatory properties, with a notable ability to penetrate the blood-brain barrier. Mefenamic acid-d4 is primarily utilized in pharmacokinetic studies and metabolic research, aiding in the exploration of inflammatory responses and mechanisms of pain relief through its interaction with COX-1 and COX-2 enzymes. -
COX Inhibitor
Ibuprofen Impurity K is a chemical impurity associated with Ibuprofen, a well-known nonsteroidal anti-inflammatory drug (NSAID) that functions as a cyclooxygenase (COX) inhibitor. It selectively inhibits COX-1 with an IC50 of 13 μM and COX-2 with an IC50 of 370 μM, contributing to its anti-inflammatory effects. This compound is relevant for studies focused on the metabolism and safety of Ibuprofen, as well as for research into the pharmacological profiles of COX inhibitors. -
COX Inhibitor
Thiazolinobutazone is a selective cyclooxygenase (COX) inhibitor that exhibits anti-inflammatory properties. This compound is recognized for its reduced toxicity compared to Phenylbutazone, making it a safer alternative in pharmacological research. Thiazolinobutazone is primarily utilized in the investigation of various immunological diseases, providing insights into COX-related pathways and inflammation mechanisms. -
COX Inhibitor
LY150310 free base is a potent COX inhibitor that effectively inhibits thromboxane synthase and cyclooxygenase, as well as thrombin activation. This compound demonstrates a dose-dependent ability to inhibit spontaneous lung metastasis, making it valuable for research applications aimed at understanding metastatic processes and developing anti-cancer therapies. -
COX-2 Inhibitor
COX-2-IN-12 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 19.98 μM, demonstrating potent anti-inflammatory properties. This compound is suitable for various biological research applications related to inflammation and pain management. In vivo acute toxicity studies indicate a favorable safety profile for COX-2-IN-12, supporting its potential for therapeutic exploration. -
COX-1 Inhibitor
(+)-Catechin pentaacetate serves as a precursor for the synthesis of (+)-catechin, a natural compound with herbicidal and antimicrobial properties. This compound functions as a selective inhibitor of cyclooxygenase-1 (COX-1), exhibiting an IC50 value of 1.4 μM. Its ability to modulate COX-1 activity makes it valuable for research in inflammation and pain response pathways. -
COX-2 Inhibitor
COX-2-IN-23 is a selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting IC50 values of 0.28 μM for COX-2 and 20.14 μM for COX-1. This compound demonstrates significant anti-inflammatory activity while maintaining a low ulcerogenic profile, making it suitable for research applications focused on inflammation and pain modulation. Its selectivity and efficacy position it as a valuable tool in the study of inflammatory pathways. -
COX Inhibitor
COX-2-IN-50 is a highly soluble COX-2 inhibitor, exhibiting notable analgesic activity. With a water solubility of 20.3 mg/mL, it surpasses its precursor compound, PC407, which has a solubility of 1.6 μg/mL. This compound demonstrates excellent biocompatibility, making it suitable for the formulation of injectable dosage forms. COX-2-IN-50 has shown significant analgesic effects in vivo, indicating its potential in pain management research and therapeutic applications. -
COX Inhibitor
Diclofenac deanol is a potent cyclooxygenase (COX) inhibitor, particularly exhibiting enhanced selectivity for COX-2 over COX-1. This compound possesses anti-inflammatory, analgesic, and antipyretic properties, making it valuable in pain management and inflammation-related research. Its superior water solubility compared to traditional diflunisal salts facilitates its application in various biological assays and medical research, expanding its potential therapeutic uses. -
COX-2 Inhibitor
COX-2-IN-20 is a selective COX-2 inhibitor with a measured IC50 of 17.9 nM. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research in inflammation and pain management. Its oral bioavailability allows for convenient administration in various studies aimed at understanding COX-2's role in inflammatory diseases. -
COX Inhibitor
Flunixin is a cyclooxygenase (COX) inhibitor that exhibits IC50 values of 0.55 μM for COX-1 and 3.24 μM for COX-2. It is known for its anti-inflammatory properties, making it valuable in studies aimed at understanding inflammatory pathways. Flunixin is commonly utilized in research focused on pain management and related therapeutic applications. -
COX-2 Inhibitor
COX-2-IN-22 is a selective inhibitor of Cyclooxygenase-2 (COX-2) with an IC50 of 8.6 µM. In addition to its primary activity, COX-2-IN-22 also exhibits inhibitory effects on Acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), β-Secretase, Lipoxygenase-5 (LOX-5), and DPPH, with IC50 values of 2.8 µM, 6.3 µM, 15.3 µM, 13.9 µM, and 6.8 µM, respectively. This compound is capable of crossing the blood-brain barrier, making it a valuable tool for research in neuroinflammatory and neurodegenerative disease models. -
COX Inhibitor
2-Hydroxy Ibuprofen is a metabolic derivative of Ibuprofen, functioning primarily as a cyclooxygenase (COX) inhibitor. It demonstrates significant anti-inflammatory activity, targeting COX-1 and COX-2 enzymes with inhibitory concentrations (IC50) of 13 μM and 370 μM, respectively. This compound is valuable for studying the mechanisms of inflammation and pain in various research applications, particularly in pharmacology and toxicology. -
COX-2 Inhibitor
Etoricoxib hydrochloride is a selective COX-2 inhibitor that effectively reduces inflammation and alleviates pain by blocking the conversion of arachidonic acid to prostaglandins. This compound is primarily utilized in research related to osteoarthritis and demonstrates significant anti-inflammatory properties. Additionally, etoricoxib hydrochloride has been shown to promote bone remodeling through enhanced alkaline phosphatase activity. Its formulation, developed using emulsion solvent evaporation technology, ensures good cell compatibility for various biological applications. -
COX-2 Inhibitor
Indomethacin heptyl ester is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 0.04 μM. This compound demonstrates significant anti-inflammatory activity, making it valuable for studying inflammatory processes and discovering potential therapeutic interventions in diseases characterized by COX-2 overexpression. Its specificity for COX-2 provides insights into the mechanism of action and the development of novel anti-inflammatory agents. -
COX Inhibitor
Indobufen sodium is a reversible inhibitor of cyclooxygenase (COX) activity, primarily targeting platelet aggregation. By suppressing the synthesis of thromboxane A2 (TxA2), it effectively modulates platelet function. Additionally, Indobufen sodium down-regulates the expression of tissue factor (TF) in monocytes, making it a valuable tool for research involving cardiovascular and inflammatory processes. -
COX-2/Aromatase Inhibitor
COX-2/Aromatase-IN-2 is a potent dual inhibitor targeting cyclooxygenase-2 (COX-2) and aromatase. It effectively suppresses inflammation and inhibits cell proliferation in breast cancer models, demonstrating significant anti-cancer and anti-inflammatory activities. Proven efficacy in the MCF-7 breast cancer cell line and carrageenan-induced rat paw edema model makes COX-2/Aromatase-IN-2 a valuable tool for researching inflammation and breast cancer pathways. -
5-LOX/COX-1 Inhibitor
Atractylochromene is a dual inhibitor targeting 5-lipoxygenase (5-LOX) and cyclooxygenase-1 (COX-1), exhibiting IC50 values of 0.6 μM and 3.3 μM, respectively. This compound serves as a valuable tool in research related to inflammatory pathways and can facilitate the study of related conditions influenced by leukotrienes and prostaglandins. Its inhibitory effects position Atractylochromene as a potential candidate for therapeutic exploration in inflammatory diseases. -
XO/COX/LOX Inhibitor
XO/COX/LOX-IN-1 is a potent inhibitor of xanthine oxidase, cyclooxygenases, and lipoxygenases. This compound exhibits significant anti-inflammatory activity, making it valuable for research in inflammation, cancer, and metabolic diseases. Its multifaceted inhibition profile positions XO/COX/LOX-IN-1 as a critical tool for exploring pathways involved in these pathological conditions.

