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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. -
p300/CBP Inhibitor
KB528 is a selective inhibitor of the histone acetyltransferases p300 and CBP, demonstrating low nM IC50 values against these targets while sparing other members of the KAT family. This compound modulates the IRF4 transcriptional network, leading to decreased expression of key oncogenes such as IRF4, MYC, CAV2, and IGLL5, as well as reduced levels of IKZF3 protein. KB528 has been shown to effectively induce apoptosis in multiple myeloma cells, making it a valuable tool for research in multiple myeloma and related oncological studies. -
Inflammatory Pathway Inhibitor, Oxidative Stress Inhibitor, Cancer Pathway Inhibitor
Matairesinol is an orally active bioactive compound that functions as an inflammatory pathway, oxidative stress, and cancer pathway inhibitor. It effectively inhibits the phosphorylation of MAPK, JNK, and NF-κB, while downregulating RANKL-induced NFATc1 expression and activity, and suppressing the activation of the PI3K/AKT/FOXO1 pathway. Matairesinol is applicable in research on sepsis-mediated brain injury, osteoporosis, heart failure, atopic dermatitis, and various cancer models. -
RAS/RAS-RAF Inhibitor
RAS/RAS-RAF-IN-1 is a potent inhibitor targeting the RAS and RAS-RAF signaling pathways. With a dissociation constant (KD) in the range of 5.0 μM to 15 μM for cyclophilin A (CYPA), this compound demonstrates significant binding affinity. RAS/RAS-RAF-IN-1 exhibits notable antitumor activity, making it a valuable tool for cancer research and therapeutic development. -
WNT7A Inhibitor/Photosensitizer
WNT7A-IN-1 is a WNT7A inhibitor that disrupts the interaction between WNT7A and its receptor FZD5, leading to the upregulation of MHC-I expression. This compound enhances the expression of MHC-I and phosphorylated p65 while decreasing the levels of active β-catenin. Additionally, WNT7A-IN-1 serves as a photosensitizer in the green spectral region, making it valuable for research in cancer immunotherapy and photodynamic therapy applications. -
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. -
Arginase Inhibitor
nor-NOHA monoacetate is a selective and reversible inhibitor of arginase. It induces apoptosis in cells expressing arginase 2 under hypoxic conditions and demonstrates anti-leukemic activity. This compound is valuable for investigating endothelial dysfunction, immunosuppression, and metabolic processes in various biological contexts. -
Arginase Inhibitor
ABH hydrochloride is a potent arginase inhibitor with a Ki value of 8.5 nM. This compound enhances nitric oxide production and downregulates inflammatory mediators, including ICAM-1, VCAM-1, and MCP-1. ABH hydrochloride is utilized in research focused on erectile dysfunction, lung protection, wound healing, blood pressure regulation, and vascular fibrosis. Its dual role in promoting vasodilation and reducing inflammation makes it a valuable reagent for studying cardiovascular and inflammatory diseases. -
Arginase Inhibitor
OATD-02 is a competitive, reversible, noncovalent inhibitor that targets arginase 1 and 2. It exhibits slow offset kinetics with IC50 values of 20 nM for human arginase 1, 39 nM for human arginase 2, 39 nM for mouse arginase 1, and 28 nM for rat arginase 1. OATD-02 effectively disrupts tumor immunosuppression mediated by arginases, making it a valuable tool for research in melanoma and other cancer immunotherapy studies. -
Arginase Inhibitor
ARG1-IN-1 is a potent arginase inhibitor with an IC50 value of 29 nM. This compound effectively inhibits serum arginase activity, leading to increased levels of arginine in various mouse tumor models. ARG1-IN-1 is particularly useful for research applications focused on tumor biology and arginine metabolism in cancer. -
Arginase Inhibitor
NED-3238 is a potent inhibitor of arginase I and II, exhibiting IC50 values of 1.3 nM and 8.1 nM, respectively. This compound is valuable in research focused on metabolic regulation and immune modulation, facilitating studies related to cancer, cardiovascular diseases, and inflammation. Its high specificity and potency make it a suitable tool for investigating arginine metabolism and its implications in various biological processes. -
Arginase Inhibitor
(-)-3-O-Acetylcatechin is an arginase inhibitor that demonstrates significant activity against Leishmania amazonensis, with an IC50 value of 3.7 μM. This compound serves as a valuable tool for investigating leishmaniasis and studying arginase-related metabolic pathways in parasitic infections. Its application in biochemical research may contribute to the development of therapeutic strategies for managing leishmaniasis. -
Arginase Inhibitor
BEC is a competitive inhibitor of the binuclear manganese metalloenzyme arginase, functioning as an arginine analogue with slow-binding characteristics. This compound promotes the increased availability of arginine for nitric oxide synthase, thereby facilitating nitric oxide-dependent smooth muscle relaxation in the corpus cavernosum. As a result, BEC is significant in studies related to penile erection and vascular health. -
Arginase Inhibitor
NG-Hydroxy-L-arginine acetate is a selective arginase inhibitor that participates in modulating the nitric oxide pathway. By interfering with the conversion of arginine to citrulline, it facilitates increased nitric oxide production via nitric oxide synthase. This compound is valuable in research related to cardiovascular health, neurobiology, and inflammation, where nitric oxide signaling plays a critical role. -
Inhibitor Of The Binding Of DQ8 Peptide To MHC Class II Molecule
D-α-Methyl DOPA is an inhibitor of the binding of DQ8 peptide to MHC class II molecules. By occupying a pocket in the DQ8 peptide binding groove, D-α-Methyl DOPA disrupts the presentation of DQ8 peptides to CD4+ T cells. This inhibition may play a role in modulating the immune response, potentially slowing the development or progression of type 1 diabetes and celiac disease. This compound is valuable in immunological research focused on T cell activation and autoimmune disease mechanisms. -
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. -
iNOS Inhibitor
S-Methylisothiourea sulfate serves as a potent, selective, and competitive inhibitor of inducible nitric oxide synthase (iNOS). This compound has demonstrated significant biological activity in reducing nitric oxide production and exhibits protective effects in rodent models of septic shock. Its role in modulating iNOS activity makes it a valuable reagent for research focused on inflammation and immune response mechanisms. -
Nonimmunosuppressive Cyclophilin Inhibitor
NIM258 is a potent nonimmunosuppressive cyclophilin inhibitor, specifically targeting cyclophilin A with a Kd of 1.2 nM. It exhibits significant anti-HCV activity, with an EC50 of 40 nM. This compound serves as a valuable tool for research into HCV infection and its associated pathways. -
CCR5 Inhibitor
DAPTA is a synthetic peptide that acts as a selective inhibitor of the CCR5 receptor. By blocking CCR5, DAPTA interferes with viral entry into host cells, exhibiting significant anti-HIV activity. This compound is valuable for research in virology and the development of therapeutic strategies against HIV. -
HIV-1 Entry Inhibitor
RPR103611 is a derivative of betulinic acid that functions as a potent HIV-1 entry inhibitor. It displays IC50 values of 80 nM for CCR5-tropic virus YU2, 0.27 nM for CXCR4-tropic virus NL4-3, and 0.17 nM for dual tropic virus 89.6. This compound is valuable for research focused on the mechanisms of HIV-1 entry and the development of antiviral therapies. -
CXCR Inhibitor
AMD 3329 octahydrobromide is a potent CXCR4 inhibitor that effectively reduces HIV-1 and HIV-2 viral replication. It demonstrates exceptional antiviral activity with EC50 values of 0.8 nM and 1.6 nM, surpassing the efficacy of related compounds. Additionally, AMD 3329 significantly obstructs the binding of specific CXCR4 monoclonal antibodies and inhibits SDF-1 alpha-induced Ca(2+) influx. This compound also disrupts virus-induced syncytium formation, with an EC50 of 12 nM, making it a valuable tool for HIV research and therapeutic development. -
COX Inhibitor
Ibuprofen Impurity F is a specific impurity of Ibuprofen, a well-known anti-inflammatory compound that inhibits cyclooxygenase enzymes COX-1 and COX-2. It exhibits inhibitory activity with IC50 values of 13 μM for COX-1 and 370 μM for COX-2. This reagent is valuable for quality control and analytical characterization in pharmaceutical research and development, particularly in the study of non-steroidal anti-inflammatory drugs (NSAIDs). -
COX Inhibitor
Piroxicam cinnamate is a cyclooxygenase (COX) inhibitor with demonstrated anti-inflammatory properties. It is stable under gastric conditions, making it suitable for research applications focused on inflammatory-degenerative osteoarticular diseases, rheumatic disorders, and varicocele-associated oligoasthenospermia. This compound offers significant potential for investigating therapeutic approaches to various inflammatory conditions. -
COX-1 Inhibitor
Valeryl salicylate is a potent and irreversible inhibitor of cyclooxygenase-1 (COX-1). This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research into inflammatory processes. Its mechanism offers insights into the modulation of COX-1 enzyme activity and potential therapeutic applications in inflammatory conditions. -
COX1/2 Inhibitor
4,4'-Dihydroxy-2,6-dimethoxydihydrochalcone is a selective inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). This compound demonstrates significant anti-inflammatory properties and is valuable in research aimed at understanding the role of COX enzymes in various disease models. Its application extends to pharmacological studies focused on pain, inflammation, and potential therapeutic interventions. -
COX Inhibitor
Ibuprofen impurity 1 is an impurity of the widely used anti-inflammatory agent ibuprofen, which acts as a dual inhibitor of cyclooxygenase enzymes COX-1 and COX-2, exhibiting IC50 values of 13 μM and 370 μM, respectively. This compound is essential for evaluating the purity and quality of ibuprofen formulations in research. It serves as a valuable tool for studying the pharmacological effects and potential side effects of ibuprofen in various biological assays. -
COX-2 Inhibitor
Robenacoxib is a selective cyclooxygenase-2 (COX-2) inhibitor with potent anti-inflammatory and analgesic properties. It primarily reduces the production of prostaglandins associated with inflammation and pain, making it valuable for research related to inflammatory diseases and pain management. This compound is utilized in studies aiming to elucidate the role of COX-2 in various biological processes and to develop therapeutic strategies targeting inflammation. -
COX-2 Inhibitor
3-Carene is a bicyclic monoterpene that functions as a cyclooxygenase-2 (COX-2) inhibitor. It demonstrates significant anti-inflammatory properties by reducing nociceptive stimulus-induced inflammatory infiltrates and decreasing COX-2 overexpression. Additionally, 3-Carene enhances both the activity and expression of alkaline phosphatase, a crucial early marker of osteoblastic differentiation, making it a valuable compound for research in pain management and bone health. -
COX-2 Inhibitor
Mavacoxib is a selective, oral cyclooxygenase-2 (COX-2) inhibitor, functioning as a long-acting non-steroidal anti-inflammatory drug (NSAID). This compound effectively alleviates pain and inflammation related to degenerative joint disease, particularly in canine subjects. Research applications include studies on inflammation and pain management in veterinary medicine. -
COX-2 Inhibitor
Desmethyl Celecoxib is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 32 nM, demonstrating significant anti-inflammatory activity. As an analog of Celecoxib, this compound serves as a valuable tool in research applications focusing on inflammation and pain pathways. Its potency and specificity make it suitable for studies related to COX-2 mediated processes. -
5-LO/COX Inhibitor
BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) enzymes, exhibiting an IC50 of 5 μM for 5-LO. It also demonstrates inhibitory activity against COX-1 and COX-2, with IC50 values of 0.65 and 1.2 μg/mL, respectively. This compound is valuable for research applications involving inflammation and other related pathways. Its ability to concurrently inhibit key lipid mediators makes BW 755C a useful tool in studies focused on arachidonic acid metabolism and signaling pathways. -
COX-2 Inhibitor
Enflicoxib is a selective inhibitor of cyclooxygenase-2 (COX-2), a key enzyme in the inflammatory pathway. This nonsteroidal anti-inflammatory compound exhibits notable anti-inflammatory, analgesic, and antipyretic effects in various animal models. Enflicoxib is valuable for research investigating COX-2-mediated processes and potential therapeutic applications in pain management and inflammation. -
COX-1 Inhibitor
CP-74006 is a selective inhibitor of Cyclooxygenase-1 (COX-1). This compound demonstrates significant anti-inflammatory activity by blocking the conversion of arachidonic acid to prostaglandins, key mediators in the inflammatory response. CP-74006 is utilized in research focusing on inflammation, pain management, and cardiovascular disease, providing valuable insights into COX-1 related biological processes. -
COX inhibitor
2-Chloro-N-(2,6-dimethylphenyl)acetamide is a cyclooxygenase (COX) inhibitor that modulates inflammatory responses by inhibiting the conversion of arachidonic acid to prostaglandins. Its biological activity makes it a valuable tool in research focused on inflammation and pain pathways. This compound is utilized for studying COX-related mechanisms in various biological contexts, potentially aiding in the development of anti-inflammatory therapies. -
COX- 2 Inhibitor
Ocarocoxib is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 value of 1.4 μM. By inhibiting COX-2, Ocarocoxib effectively reduces the synthesis of prostaglandins, thereby imparting significant anti-inflammatory effects. This compound is useful for research on inflammation and associated pathological conditions. -
COX-2/5-LOX Inhibitor
Tebufelone is a selective dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LO). It exhibits significant anti-inflammatory, analgesic, and antipyretic properties, making it useful for research into inflammatory pathways. This compound is valuable for studying the roles of COX-2 and 5-LO in various biological processes and assessing novel therapeutic strategies for inflammatory diseases. -
COX-1 Inhibitor
Teriflunomide impurity 3, also known as 4-Amino-N-(4-trifluoromethylphenyl)benzamide, acts as a selective inhibitor of cyclooxygenase-1 (COX-1) with an IC50 of 30 µM. This compound exhibits significantly lower activity against COX-2, with an IC50 greater than 100 µM. Teriflunomide impurity 3 is valuable for research applications exploring inflammatory pathways and the role of COX-1 in various biological processes. -
iNOS/COX-2 Inhibitor
Rehmapicrogenin is a selective inhibitor of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). This compound, derived from the root of Rehmannia glutinosa, demonstrates significant anti-inflammatory properties, making it a valuable tool for research focused on inflammation pathways. Its ability to inhibit pro-inflammatory mediators such as IL-6 further underscores its relevance in studies aimed at understanding and treating inflammatory diseases. -
COX-1/COX-2 Inhibitor
(S)-(+)-Ibuprofen-d3 is a deuterated analog of (S)-(+)-Ibuprofen, targeting the COX-1 and COX-2 enzymes. With IC50 values of 2.1 μM and 1.6 μM, respectively, this compound exhibits significant analgesic, anti-inflammatory, and antipyretic properties. It serves as a valuable tool for studying the pharmacodynamics and mechanisms of nonsteroidal anti-inflammatory drugs (NSAIDs) in various biological research applications. -
COX Inhibitor
Isoxicam is a non-steroidal anti-inflammatory drug (NSAID) that functions as a nonselective inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). Its primary mechanism involves the inhibition of prostaglandin synthesis, making it effective in reducing inflammation and pain. Isoxicam is commonly utilized in research related to arthritis and other inflammatory conditions, providing valuable insights into the role of COX enzymes in various biological processes. -
COX-2 Inhibitor
Cimicoxib is a selective COX-2 inhibitor that effectively penetrates the blood-brain barrier. It displays significant anti-inflammatory, analgesic, and antipyretic properties by inhibiting the production of thromboxane B2 and prostaglandin E2, with an IC50 of 66 nM against human COX-2. Additionally, Cimicoxib targets CYP2D15, exhibiting an IC50 of 1.6 μM in canines and 0.056 μM in felines. This compound is utilized in research involving inflammatory diseases, osteoarthritis, and perioperative pain management in orthopedic and soft tissue surgeries. -
COX Inhibitor
Naproxen glucuronide, a metabolite of naproxen, functions as a non-selective cyclooxygenase (COX) inhibitor. This compound exhibits significant anti-inflammatory, analgesic, and antipyretic activity, making it useful in the study of pain relief and inflammation pathways. Research applications include examining its metabolic pathways, assessing its efficacy in various inflammatory conditions, and exploring its pharmacokinetic properties in biological systems. -
Dual COX/5-LOX Inhibitor
ER-34122 is a dual inhibitor of cyclooxygenase (COX) and 5-lipoxygenase (5-LO). This compound exhibits significant anti-inflammatory activity, making it valuable for research into inflammation-related pathways. ER-34122 is particularly relevant for studies investigating the interplay between COX and 5-LO pathways in various disease models and therapeutic contexts. -
mPGES-1 Inhibitor
Crisdesalazine is a selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1). It demonstrates significant biological activity as a free radical scavenger, effectively neutralizing reactive oxygen species (ROS) such as hydrogen peroxide, thereby providing neuroprotective benefits against apoptosis and axonal damage. By inhibiting PGE2 production, Crisdesalazine also modulates inflammatory responses and facilitates the conversion of macrophages from the pro-inflammatory M1 to the anti-inflammatory M2 phenotype. This compound is particularly valuable for research focused on neuroprotection in conditions such as multiple sclerosis and spinal cord injury. -
NO/PGE2 Inhibitor
Epibetulinic acid is an inhibitor of nitric oxide (NO) and prostaglandin E2 (PGE2) production. It demonstrates significant anti-inflammatory activity, exhibiting IC50 values of 0.7 μM for NO and 0.6 μM for PGE2 in mouse macrophages (RAW 264.7) stimulated with bacterial endotoxin. This compound is valuable for research applications focused on inflammation and immune response modulation. -
5-LO/PGE2 Inhibitor
Canniprene is a potent inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase/microsomal prostaglandin E2 synthase (PGE2), with IC50 values of 0.4 μM and 10 μM, respectively. Derived from Cannabis sativa, Canniprene modifies the biosynthesis of inflammatory eicosanoids and prostaglandins, making it a valuable tool for researching inflammation and related pathways. Its unique mechanism of action positions Canniprene as a potential candidate for studying inflammatory diseases and therapeutic interventions targeting lipid mediators. -
PGE2 Inhibitor
Saikogenin D is an effective PGE2 inhibitor isolated from Bupleurum chinense. This compound exhibits significant anti-inflammatory properties by activating epoxygenases, leading to the conversion of arachidonic acid into epoxyeicosanoids and dihydroxyeicosatrienoic acids, which subsequently suppress PGE2 production. Saikogenin D also induces an increase in intracellular calcium levels ([Ca2+]i) through the release of Ca2+ from intracellular stores, making it a valuable tool for studying inflammatory pathways. -
COX-2 Inhibitor
Apricoxib is a selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating a potent inhibitory effect on PGE2 production with an IC50 of 1.5 nM. This compound exhibits notable biological activities, including anticancer, analgesic, and anti-inflammatory properties. Apricoxib is a valuable tool for research applications focused on inflammation, pain management, and cancer therapeutics.

