PGE Synthase

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.

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.

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.

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.

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.

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.

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.

13,14-Dihydro-15-keto-prostaglandin A2 is a derivative of 13,14-dihydro-15-keto PGE2, resulting from the non-enzymatic dehydration process. This compound is primarily involved in the metabolic pathway leading to the formation of bicyclo PGE2, which serves as a critical biomarker for PGE2 synthesis. Its significant role in prostaglandin metabolism makes it valuable for research in inflammation, pain, and various physiological processes associated with prostaglandins.

13,14-Dihydro PGE1 is a significant metabolite of Prostaglandin E1 (PGE1) that functions as a potent inhibitor of ADP-induced platelet aggregation, with an ID50 of 10.8 ng/mL in platelet-rich plasma. This compound is primarily utilized in research regarding cardiovascular health and platelet function. Its mechanism of action makes it valuable for studies focused on thrombotic disorders and the modulation of vascular responses.

AT-56 is am orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS) (Ki = 75 μM, IC50 = 95 μM).

MF63 is a selective mPGES-1 inhibitor with an IC50 of 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively.

SAR191801 is a hPGDS inhibitor ,with IC50 of 12 nM in the Fluorescence Polarization Assay or the EIA assay.

Limaprost(OP1206) is a PGE1 analog and potent platelet adhesion inhibitor.

HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM.

Sinensetin is a methylated flavone found in certain citrus fruits. pocess potent antiangiogenesis and anti-inflammatory, sinensetin enhances adipogenesis and lipolysis.

Evatanepag (CP-533536) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.

Furprofen is an non-steroidal anti-inflammatory drug (NSAID) with analgesic properties. Furprofen acts via the inhibition of prostaglandin (PGE) synthesis. Furprofen can be treated orally for the relief of pain.

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).

PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM.

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.

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.

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.

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.

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.