Catalog No.
Product Name
Application
Product Information
Citations
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HPGDS inhibitor
HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.- Beixian Zhou, .et al. , Chin Med, 2023, Oct 27;18(1):139 PMID: 37891648
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hPGDS inhibitor
SAR191801 is a hPGDS inhibitor ,with IC50 of 12 nM in the Fluorescence Polarization Assay or the EIA assay. -
H-PGDS inhibitor
HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM. -
mPGES-1 inhibitor
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM). -
PGE2 agonist
Evatanepag (CP-533536) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM. -
anti-inflammatory agent
Sinensetin is a methylated flavone found in certain citrus fruits. pocess potent antiangiogenesis and anti-inflammatory, sinensetin enhances adipogenesis and lipolysis. -
PGE2 Antagonist
EP4 receptor antagonist 7 is a selective antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, demonstrating an IC50 value of 1.1 nM. This compound effectively inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM and downregulates the expression of several important mRNAs, including IL-4 and Arg1, in RAW 264.7 macrophages. Additionally, EP4 receptor antagonist 7 shows potential in combination with anti-PD-1 antibodies to inhibit tumor growth and enhance CD8+ T cell infiltration in a CT26 murine colon cancer model, making it a valuable tool for cancer immunotherapy research. -
PGE2 Metabolite
15-keto-Prostaglandin E2 is a metabolite of prostaglandin E2 that primarily targets and inhibits STAT3 activation through binding to the Cys259 residue. This compound has been shown to inhibit the growth and progression of breast cancer cells while activating PPAR-γ, promoting fungal growth. Additionally, 15-keto-Prostaglandin E2 disrupts glomerular vascularization during zebrafish development, resulting in a decreased surface area of the glomerular filtration barrier, highlighting its importance in developmental biology and cancer research. -
mPGES-2 Inhibitor
SZ0232 is a selective inhibitor of microsomal prostaglandin E synthase-2 (mPGES-2), effectively reducing the production of prostaglandin E2 (PGE2) and downregulating the PGE2-EP4 signaling pathway. This inhibition disrupts the β-catenin/STAT3/c-Myc proliferation cascade, demonstrating significant effects on the abnormal proliferation of cyst epithelial cells. SZ0232 serves as a valuable tool for investigating autosomal dominant polycystic kidney disease (ADPKD) in both in vitro and in vivo research models. -
mPGES-1/5-LOX Inhibitor
YS121 is a dual inhibitor targeting microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LOX), with IC50 values of 3.4 μM and 6.5 μM, respectively. It demonstrates specific, reversible binding to mPGES-1, indicated by a KD of 10-14 μM. YS121 reduces PGE2 production in IL-1β-stimulated A549 cells with an EC50 of 12 μM and activates PPAR-α and PPAR-γ, with EC50 values of 1 μM and 3.6 μM, respectively. Additionally, YS121 exhibits significant anti-inflammatory effects in human whole blood and in vivo, making it a valuable tool for pleurisy research. -
PGE2 Inhibitor
N1-Acetyl-5-methoxykynuramine hydrochloride is a potent inhibitor of prostaglandin E2 (PGE2) production, acting as an active metabolite of melatonin. This compound effectively scavenges reactive oxygen species and suppresses COX-2 expression in RAW 264.7 macrophages in a dose- and time-dependent manner. Additionally, in a mouse model of Parkinson's disease induced by MPTP, it diminishes lipid peroxidation in key brain regions. N1-Acetyl-5-methoxykynuramine hydrochloride is relevant for research focused on metabolic and neurological disorders. -
mPGES-1 Inhibitor
Zaloglanstat is a selective microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor, demonstrating an IC50 of 5 nM for human mPGES-1 while sparing COX-1 and COX-2 with IC50 values greater than 10 μM. It effectively inhibits the conversion of prostaglandin PGH2 to prostaglandin PGE2, thereby mitigating inflammation-related overproduction of PGE2 and alleviating pain. In vitro studies show that Zaloglanstat reduces IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts. It is applicable in research exploring asthma, osteoarthritis, and neurodegenerative diseases, and exhibits effective inhibition of PGE2 release in whole blood from pig and dog models with IC50 values of 161 nM and 154 nM, respectively. -
NO/mPGES-1 Inhibitor
Shanciol B is a selective inhibitor of nitric oxide (NO) production and microsomal prostaglandin E synthase-1 (mPGES-1). Isolated from the ethyl acetate extract of Pholidota imbricate, Shanciol B exhibits notable anti-inflammatory properties and demonstrates effective 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity. This compound is valuable for research applications focused on inflammation and oxidative stress. -
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. -
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.
