Catalog No.
Product Name
Application
Product Information
Citations
-
NTPDase Inhibitor
h-NTPDase-IN-3 is a potent pan-inhibitor of NTPDase enzymes, demonstrating varying inhibitory activity with IC50 values of 34.13 μM for h-NTPDase1, 0.33 μM for h-NTPDase2, 23.21 μM for h-NTPDase3, and 2.48 μM for h-NTPDase8. This compound is valuable for research focused on purinergic signaling, offering insights into the regulation of extracellular nucleotide levels. Its ability to inhibit multiple NTPDase isoforms makes it suitable for studies exploring their roles in various physiological and pathological processes. -
NTPDase Inhibitor
NTPDase-IN-1 is a selective inhibitor targeting NTPDase enzymes, exhibiting IC50 values of 0.05, 0.23, and 0.54 µM for human NTPDase-1, -2, and -8 respectively. This compound acts as a non-competitive inhibitor for NTPDase-1 and -2, displaying a Km of 21 µM for NTPDase-1. NTPDase-IN-1 is applicable in research focused on cancer, immunological disorders, and bacterial infections. -
h-NTPDases 8 Inhibitor
h-NTPDase8-IN-1 is a selective inhibitor of human NTPDase8, exhibiting an IC50 value of 0.28 μM. This compound, classified as a sulfamoyl-benzamide, plays a crucial role in the modulation of physiological and pathological processes, including thrombosis, diabetes, inflammation, and cancer. Its potent inhibition of h-NTPDase8 makes it a valuable tool for research applications targeting these diverse biological functions. -
NTPDase Inhibitor
h-NTPDase-IN-4 is a potent pan-inhibitor of NTPDase, demonstrating IC50 values of 3.58 μM against h-NTPDase1, 10.21 μM against h-NTPDase2, 0.13 μM against h-NTPDase3, and 13.57 μM against h-NTPDase8. This compound selectively modulates nucleotide metabolism and purinergic signaling pathways, making it a valuable tool for research in cellular communication, inflammation, and cancer biology. Its broad activity across multiple NTPDase isoforms positions it as a significant reagent for studies investigating the role of purinergic receptors in various physiological and pathological processes. -
TcNTPDase1 Inhibitor
TcNTPDase1-IN-1 is a potent inhibitor of nucleoside triphosphate diphosphohydrolase 1 (TcNTPDase1) derived from Trypanosoma cruzi. This compound demonstrates key biological activities relevant to antibacterial, antitoxic, and antitumor research applications. By selectively targeting TcNTPDase1, TcNTPDase1-IN-1 provides valuable insights into its role in disease mechanisms and may aid in the development of therapeutic strategies against infections and cancer. -
Anti-osteoclastogenic Agent
NFATc1-IN-1 is a potent inhibitor of RANKL-induced osteoclast formation, exhibiting an IC50 of 1.57 μM. This compound exerts its anti-osteoclastogenic effects by disrupting the RANKL-mediated nuclear translocation of NFATc1. NFATc1-IN-1 is a valuable tool for research into osteoclastic diseases, providing insights into the regulation of osteoclastogenesis. -
Non-steroidal Anti-inflammatory Agent
Pirprofen is an orally active non-steroidal anti-inflammatory agent that functions as a reversible inhibitor of prostaglandin synthetase. Its key biological activities include anti-inflammatory, analgesic, and antipyretic effects, while also inhibiting leucocyte chemotaxis and the secondary phase of platelet aggregation triggered by collagen and arachidonic acid. This compound is of particular interest for research focused on inflammatory diseases and associated mechanisms. Note that pirprofen may also induce hepatotoxicity, warranting careful consideration in experimental applications. -
mPGES1 Inhibitor
CAY10526 is a selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES1), exerting its effects by specifically modulating mPGES1 expression without influencing cyclooxygenase-2 (COX-2). This compound effectively reduces PGE2 production, leading to significant suppression of tumor growth and enhanced apoptosis in melanoma xenografts. CAY10526 downregulates anti-apoptotic proteins BCL-2 and BCL-XL while elevating levels of pro-apoptotic proteins BAX and BAK, along with cleaved caspase-3, promoting cell death. It demonstrates potent cytotoxicity with an IC50 of less than 5 μM in melanoma cell lines expressing mPGES1, making it valuable for cancer research and therapeutic studies. -
mPGES-1 Inhibitor
Vipoglanstat is a potent and selective non-peptide inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1). As a carboxamide derivative, it demonstrates significant anti-inflammatory activity, making it a valuable tool in research focusing on inflammation-related diseases. Its oral bioavailability facilitates in vivo studies aimed at understanding the role of mPGES-1 in various pathological conditions. -
PGE synthase Inhibitor
Zomepirac sodium salt is a potent inhibitor of prostaglandin E synthase, exhibiting significant anti-inflammatory properties. As a non-steroidal anti-inflammatory drug (NSAID), Zomepirac sodium salt is primarily utilized in research to study prostaglandin biosynthesis and related inflammatory processes. It is noteworthy that this compound has been associated with immune-mediated liver injury, highlighting its importance in pharmacological safety assessments. -
mPGES-1 Inhibitor
mPGES1-IN-7 is a benzimidazole-derived inhibitor targeting microsomal prostaglandin E synthase-1 (mPGES-1). It significantly reduces prostaglandin E2 (PGE2) production and exhibits inhibitory effects on other prostaglandins. mPGES1-IN-7 has demonstrated effectiveness in mitigating acute inflammation, as evidenced in a Carrageenan-induced air sac model in mice, making it a valuable tool for research in inflammation and related biological pathways. -
mPGES-1 Inhibitor
UK4b is a selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1). This compound exhibits anti-inflammatory and analgesic properties, making it a valuable tool for research on pain and inflammation. Additionally, UK4b has demonstrated the ability to inhibit the growth of abdominal aortic aneurysms in murine models, highlighting its potential applications in cardiovascular research. -
mPGES-1 Inhibitor
PF-4693627 is a potent and selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 3 nM. This compound exhibits oral bioavailability and is designed for research into inflammatory conditions, particularly those related to osteoarthritis and rheumatoid arthritis. Its ability to inhibit mPGES-1 makes it a valuable tool for investigating pathways involved in inflammation. -
mPGES-1 Inhibitor
PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), exhibiting an IC50 of 16.5 nM. It effectively inhibits IL-1β-induced prostaglandin E2 (PGE2) synthesis in vitro, making it a valuable tool for studying inflammatory processes. This compound is applicable in research focused on pain, inflammation, and other related pathways. -
mPGES-1 Inhibitor
CAY10589 is a selective inhibitor of the enzyme mPGES-1, which plays a critical role in inflammatory responses. This compound is primarily utilized in research to study the mechanisms of inflammation and its associated pathways. Importantly, CAY10589 does not significantly influence the differentiation of bone marrow myeloid precursor cells into M2-like tumor-associated macrophages (TAMs), making it a valuable tool for dissecting inflammatory processes without altering macrophage polarization. -
mPGES1 Inhibitor
mPGES1-IN-9 is a selective inhibitor of the microsomal prostaglandin E synthase-1 (mPGES1) enzyme, exhibiting an IC50 value of 0.5 μM. This compound is utilized in anti-inflammatory research, facilitating studies aimed at understanding the role of mPGES1 in various inflammatory processes. Its effective inhibition makes it a valuable tool for investigating potential therapeutic strategies in inflammatory diseases. -
PGE synthase Inhibitor
mPGES1-IN-4 is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), effectively reducing PGE2 production at submicromolar concentrations. This compound demonstrates notable anti-inflammatory activity, particularly in in vivo models of acute inflammation, by selectively targeting the mPGES-1 pathway. Its application in research includes investigating the role of PGE2 in inflammatory processes and potential therapeutic interventions. -
PGE2 Inhibitior
(+)–ε-Viniferin is a stilbene compound that acts as a PGE2 inhibitor, demonstrating significant anti-inflammatory properties. This compound is orally active and has been shown to reduce fat accumulation, making it a valuable tool for research focused on inflammation and obesity. -
mPGES-1 Inhibitor
AF3442 is a selective inhibitor of mPGES-1, exhibiting an IC50 value of 0.06 μM. This compound effectively reduces PGE2 generation from monocytes, even in the presence of plasma proteins, demonstrating its practical application in biological systems. AF3442's selectivity for mPGES-1 over other prostanoids such as TXB2, PGF2α, and 6-keto-PGF1α supports its use in research focused on analgesia and inflammation pathways. -
PGE Inhibitor
mPGES1-IN-6 is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 value of 0.03 μM. By effectively blocking mPGES-1, this compound plays a crucial role in reducing prostaglandin E2 synthesis, making it valuable for studies related to inflammation and pain modulation. mPGES1-IN-6 is suitable for research applications focused on anti-inflammatory drug discovery and the investigation of related signaling pathways. -
PGE2 Synthase Inhibitor
5-trans U-44069 is a selective inhibitor of prostaglandin E2 synthase, effectively modulating the synthesis of this key inflammatory mediator. Its primary mechanism of action involves the blockade of prostaglandin E2 formation, making it a valuable tool for investigating the role of PGE2 in various biological processes. This compound is suitable for research applications related to inflammation, pain, and cardiovascular studies. -
PGE synthase Inhibitor
Friluglanstat is a selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), targeting the synthesis of prostaglandin E2. This compound exhibits anti-inflammatory activity by reducing prostaglandin levels, making it a valuable tool for investigating inflammatory pathways. It is applicable in research focused on inflammation, pain relief, and related diseases. -
mPGES-1Inhibitor
AGU661 is a potent inhibitor of Microsomal Prostaglandin E2 Synthase 1 (mPGES-1) with an IC50 of 0.22 nM. It effectively reduces PGE2 production in human pro-inflammatory M1 macrophages and activated monocytes, while sparing other lipid mediator pathways. Although AGU661 exhibits poor metabolic stability and high plasma protein binding, its incorporation into PLGA-based nanoparticles significantly enhances its bioactivity. This compound is suited for research related to inflammatory disorders. -
PGE synthase Inhibitor
mPGES1-IN-5 is a polysubstituted pyrimidine compound that serves as a selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). This compound demonstrates potent submicromolar inhibition of PGE2 production, primarily exerting its anti-inflammatory effects through mPGES-1 blockade. It is particularly useful in research related to inflammation and can be applied in various acute inflammation models in vivo to study its therapeutic potential. -
PGE Inhibitor
BRP-201 is a selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), demonstrating an IC50 value of 0.42 μM. This compound exhibits potent anti-inflammatory properties, making it a valuable tool for research in inflammatory diseases. Its specificity for mPGES-1 supports its potential application in the development of next-generation anti-inflammatory therapeutics. -
5-LO/mPGES-1 Inhibitor
5-LO/mPGES1-IN-1 is a dual inhibitor of 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1), exhibiting IC50 values of 0.3 μM and 0.4 μM, respectively. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research in inflammatory pathways. Applications include studies focused on the modulation of inflammatory responses, providing insights into potential therapeutic strategies for related diseases. -
mPGES-1 Inhibitor
AGU654 is a selective mPGES-1 inhibitor with an IC50 of 2.9 nM, acting primarily on the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme. By inhibiting this enzyme, AGU654 disrupts the conversion of arachidonic acid to prostaglandin E2 (PGE2), thereby reducing inflammatory responses, pain, and fever. In cellular models, AGU654 effectively suppresses PGE2 production in response to bacterial exotoxins while maintaining the synthesis of other prostaglandins. Furthermore, in guinea pig models, it demonstrates significant anti-inflammatory, analgesic, and antipyretic properties, highlighting its potential for research in inflammatory diseases and pain management. -
PGE synthase Inhibitor
Fagaramide is a potent inhibitor of prostaglandin E synthase, demonstrating significant anti-inflammatory properties. Extracted from Zanthoxylum bungeanum, it effectively reduces carrageenan-induced foot swelling in rat models. This compound serves as a valuable tool for research into inflammation mechanisms and potential therapeutic applications targeting prostaglandin synthesis. Its biological activity is approximately 1/20 that of indomethacin, making it a noteworthy candidate for further exploration in inflammatory studies. -
PGE synthase Inhibitor
Cryogenine is an alkaloid that functions as a selective inhibitor of prostaglandin E synthase, exhibiting significant anti-inflammatory properties. With an IC50 value of 424 μM, Cryogenine effectively attenuates inflammatory responses. In experimental models, administration at doses of 100 mg/kg per day has shown a reduction in paw edema and a decreased mean arthritic index in rats with adjuvant-induced polyarthritis. This makes Cryogenine a valuable reagent for researching inflammation and related disorders. -
Pge Synthase Inhibitor
5-trans U-46619 is an inhibitor of prostaglandin E synthase, which plays a critical role in the biosynthesis of prostaglandins. At a concentration of 10 μM, 5-trans U-46619 demonstrates an inhibition of less than 20% on PGE synthase activity. This compound is suitable for research applications investigating the modulation of inflammatory pathways and the role of prostaglandins in various biological processes. -
PGE synthase Inhibitor
Suprofen L-lysine is a non-steroidal anti-inflammatory drug (NSAID) that functions primarily as a prostaglandin E synthase inhibitor. This compound exhibits significant anti-inflammatory activity, making it suitable for research applications aimed at understanding inflammation pathways and evaluating potential therapeutic strategies for inflammatory diseases. Its mechanistic insights can contribute to the development of new anti-inflammatory agents in pharmaceutical research. -
mPGES-1 Inhibitor
α-Gracinoic acid is a selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), which plays a crucial role in the synthesis of pro-inflammatory prostaglandins. This compound exhibits significant anti-inflammatory activity, making it a valuable tool in research focused on chronic inflammatory diseases. It can be utilized to explore the molecular mechanisms underlying inflammation and the potential therapeutic strategies targeting the mPGES-1 pathway. -
PGE synthase Inhibitor
FR20 is a potent inhibitor of human microsomal prostaglandin synthase 1 (mPGES-1). By selectively targeting this enzyme, FR20 effectively reduces the synthesis of pro-inflammatory prostaglandins, making it valuable in research focused on inflammation and pain pathways. This reagent is ideal for studies exploring the role of mPGES-1 in various biochemical and cellular contexts. -
PGE synthase Inhibitor
AF3485 is an inhibitor of the human microsomal prostaglandin E synthase-1 (mPGES-1), demonstrating significant antitumor activity both in vitro and in vivo. This compound effectively targets tumor-associated angiogenesis by lowering prostaglandin E2 (PGE2) levels, inhibiting epidermal growth factor receptor (EGFR) signaling, and decreasing the expression of vascular endothelial growth factor (VEGF) and fibroblast growth factor-2 (FGF-2). Subchronic administration of AF3485 has been shown to reduce tumor growth in mice with human A431 xenograft tumors, making it a valuable tool for cancer research. -
PGE synthase Inhibitor
mPGES1-IN-8 is a selective inhibitor of microsomal prostaglandin E synthase 1 (mPGES1), which plays a crucial role in the biosynthesis of prostaglandin E2. This compound exhibits significant anti-inflammatory properties by inhibiting the production of pro-inflammatory mediators. It is useful in research applications focused on inflammation, pain, and related pathological conditions. -
PGE synthase Inhibitor
Gingerdione is a selective inhibitor of prostaglandin E synthase, a key enzyme in the inflammatory pathway. This compound, extracted from ginger rhizomes, has demonstrated anti-inflammatory properties and can be utilized in research focused on the modulation of pain and inflammation. Its ability to inhibit prostaglandin synthesis makes it a valuable tool for studying the therapeutic potential in various inflammatory conditions. -
PGE synthase Inhibitor
Zomepirac is a potent inhibitor of prostaglandin E synthase, acting as a non-steroidal anti-inflammatory drug (NSAID). It effectively suppresses prostaglandin biosynthesis, which is integral to inflammatory processes. Zomepirac has been used in research to explore its anti-inflammatory properties and may be relevant in studies assessing immune-mediated liver injury. -
PSMA Inhibitor
Zadavotide guraxetan is a potent inhibitor of prostate-specific membrane antigen (PSMA). This compound is utilized in SPECT/CT imaging, providing valuable insights into the cellular profiles of triple-negative breast cancer and prostate cancer. Its application in radionuclide studies underscores its significance in cancer research and therapeutic development. -
PSMA Inhibitor
Tert-Butyl-DCL is a potent inhibitor of Prostate-Specific Membrane Antigen (PSMA), a crucial target in prostate cancer research. Its inhibition of PSMA activity makes Tert-Butyl-DCL a valuable tool for studying the molecular mechanisms of prostate cancer progression and therapeutic interventions. This compound is ideal for applications in cancer biology and the development of PSMA-targeted therapies. -
PSMA Imaging Agent
EC0652 is a potent PSMA imaging agent designed for SPECT imaging applications. It enables the detection and visualization of prostate-specific membrane antigen (PSMA) expression, making it a valuable tool in research focused on metastatic castration-resistant prostate cancer. This compound enhances the understanding of tumor biology and may aid in the development of targeted therapeutic strategies. -
PSMA Modulator
Flotufolastat is a prostate-specific membrane antigen (PSMA) modulator that serves as a radiodiagnostic agent for imaging prostate cancer. This compound is instrumental in enhancing the detection and characterization of prostate cancer lesions. Flotufolastat is valuable for research applications focused on prostate cancer and other malignancies associated with PSMA expression. -
PSMA Ligand
PSMA binder-1 is a potent ligand targeting Prostate-Specific Membrane Antigen (PSMA). It facilitates the synthesis of PSMA-targeting molecules, such as Ac-PSMA-trillium, providing a valuable tool for research in prostate cancer diagnosis and therapy. This compound is essential for studies focused on imaging and targeted treatment strategies aimed at PSMA-expressing tumors. -
Contrast Agent
Piflufolastat is a positron emission tomography (PET) imaging agent that specifically targets prostate-specific membrane antigen (PSMA). Labeled with fluorine-18, Piflufolastat F-18 serves as a diagnostic tool for the visualization of prostate cancer. Its application in molecular imaging enables enhanced detection and monitoring of prostate malignancies, supporting research and clinical decision-making in oncology. -
PSMA Ligand
PSMA-azide is a ligand targeting prostate-specific membrane antigen (PSMA). It effectively inhibits PSMA-dependent hydrolysis of N-acetylaspartylglutamic acid (NAAG) with an IC50 of 9 nM and a Ki of 1 nM, making it a valuable tool for studying PSMA-related pathways. Additionally, PSMA-azide features an azide moiety, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with alkynyl-containing molecules, facilitating various biochemical labeling and conjugation applications in research. -
Active Intermediate
Glu-urea-Glu-NHS ester is an activated N-hydroxysuccinamide (NHS) ester of the Glu-urea-Glu compound. It serves as a versatile active intermediate in the synthesis of small-molecule inhibitors targeting prostate-specific membrane antigen (PSMA). This reagent is valuable for developing imaging agents, such as PSMAi-PEG conjugates, and enhancing the efficacy of targeted drug delivery systems in research applications. -
GCPII Inhibitor
GCPII-IN-1 is a potent inhibitor of the gene carboxypeptidase II (GCPII), also recognized as prostate-specific membrane antigen (PSMA), with a Ki value of 44.3 nM. This compound is primarily utilized in the research of prostate cancer, facilitating studies aimed at understanding tumor biology and developing potential therapeutic strategies. Its mechanism of action makes it a valuable tool for elucidating the role of GCPII in cancer progression. -
GCPII Inhibitor
GCPII-IN-1 TFA is a selective inhibitor of GCPII (glutamate carboxypeptidase II), also known as prostate-specific membrane antigen (PSMA), exhibiting a Ki value of 44.3 nM. This compound is instrumental in the investigation of prostate cancer, facilitating studies on the modulation of GCPII activity and its potential therapeutic applications in oncology. Researchers can utilize GCPII-IN-1 TFA to explore mechanisms of tumor growth and treatment resistance in prostate cancer models. -
PSA Substrate
Prostate Specific Antigen Substrate is a fluorescent substrate utilized for the detection of enzymatic activity associated with prostate specific antigen (PSA). This reagent enables researchers to effectively measure PSA activity, aiding in the study of prostate cancer and other related conditions. Its application in various assays facilitates enhanced understanding of PSA's role in oncology research. -
PSMA-Targeted Maytansinoid
EC1169 is a PSMA-targeted maytansinoid conjugate that selectively binds to prostate-specific membrane antigen (PSMA). This compound delivers the cytotoxic maytansinoid B hydrazide payload directly to PSMA-positive tumor cells, demonstrating significant antitumor activity while sparing PSMA-negative cells. In preclinical models, EC1169 promotes complete recovery in mice with PSMA-positive tumors, exhibiting a favorable safety profile without inducing body weight loss or major organ damage. This reagent is valuable for research focused on prostate cancer and other PSMA-expressing malignancies.
