PGE synthase
Prostaglandin E synthase
PGE synthase (Prostaglandin E synthase), which converts cyclooxygenase (COX)-derived prostaglandin H2 (PGH2) to PGE2, is known to comprise a group of at least three structurally and biologically distinct enzymes. There are membrane-associated PGES (mPGES)-1, mPGES-2, and cytosolic PGES (cPGES).
mPGES-1 is a perinuclear protein that is markedly induced by proinflammatory stimuli and downregulated by anti-inflammatory glucocorticoids as in the case of COX-2. It is functionally coupled with COX-2 in marked preference to COX-1. mPGES-2 is synthesized as a Golgi membrane-associated protein, and the proteolytic removal of the N-terminal hydrophobic domain leads to the formation of a mature cytosolic enzyme. This enzyme is rather constitutively expressed in various cells and tissues and is functionally coupled with both COX-1 and COX-2. cPGES is constitutively expressed in a wide variety of cells and is functionally linked to COX-1 to promote immediate PGE2 production.
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PGE synthase Related Products (127)
Related Products (127)
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Antibodies (2)
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Desoxo-narchinol A
0 ImagesDesoxo-narchinol A is an orally active and potent anti-inflammatory agent. Desoxo-narchinol A can be isolated from the roots and rhizomes of Nardostachys jatamansi. Desoxo-narchinol A can be used for septic shock and inflammatory diseases research.
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YS121
0 ImagesYS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50 = 3.4 μM) and 5-lipoxygenase (5-LOX; IC50 = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (KD = 10-14 μM). YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells. YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively). YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research.
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PF-4693627
0 ImagesPF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
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Pirprofen
0 ImagesCat. No.: HY-W870794CAS No.: 31793-07-4Synonyms: SU 21524Pirprofen (SU 21524) is an orally active non-steroidal anti-inflammatory agent. pirprofen is a reversible prostaglandin synthetase inhibitor. Pirprofen inhibits leucocyte chemotaxis. Pirprofen shows anti-inflammatory, analgesic, antipyretic, ulcerogenic activities. Pirprofen inhibits the secondary phase of platelet aggregation induced by Collagen and Arachidonic acid (HY-109590). Pirprofen induces hepatitis.
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PF-9184
0 ImagesPF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro.
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Friluglanstat
0 ImagesFriluglanstat is a prostaglandin E synthase (mPGES-1) inhibitor, with anti-inflammatory activity.
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HPGDS inhibitor 2
0 ImagesHPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM.
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Yangambin
0 ImagesYangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases.
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Hydralazine-d4 (hydrochloride)
0 ImagesCat. No.: HY-B0464SCAS No.: 2749234-32-8Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain.
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Withaphysalin A
0 ImagesWithaphysalin A is a withanolide compound with anti-inflammatory and antioxidant activities. Withaphysalin A inhibits LPS (HY-D1056)-induced nuclear translocation of NF-κB p65, as well as phosphorylation of STAT3, ERK, JNK and p38 MAPK. Withaphysalin A upregulates the expression of HO-1. Withaphysalin A inhibits LPS-induced production of NO, PGE2, IL-1β, IL-6 and TNF-α. Withaphysalin A downregulates LPS-induced expression of iNOS and COX-2. Withaphysalin A interacts with B-cell activating factor protein (BAFF) to exert inhibitory effects. Withaphysalin A exhibits ELOVL6 inhibitory activity. Withaphysalin A can be used in the research of inflammatory diseases, nephrotic syndrome and chronic myeloid leukemia.
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Prostaglandin E2 Inhibitor 3
0 ImagesCat. No.: HY-169858CAS No.: 3054217-03-4Prostaglandin E2 Inhibitor 3 (Compound 3) is a selectivity microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50 = 0.2 µM). Prostaglandin E2 Inhibitor 3 has higher selectivity for mPGES-1 than cyclooxygenases (COX)-1/2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH). Prostaglandin E2 Inhibitor 3 has anti-inflammatory activity and can attenuate zymosan-induced peritoneal leukocyte migration in mice.
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4-Acetylaminoantipyrine
0 Images4-Acetylaminoantipyrine (4-AA) is a derivative of antipyrine (HY-B0171). 4-Acetylaminoantipyrine acts as a PGE2-dependent blocker and inhibitor of cyclooxygenase (COX). 4-Acetylaminoantipyrine can inhibit Cu/ZnSOD. 4-Acetylaminoantipyrine can spontaneously bind with bovine serum albumin (BSA) and alter its conformation.
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6,9,12,15,18-Heneicosapentaenoic acid
0 ImagesSynonyms: HPA; Heneicosapentaenoic acid methyl ester6,9,12,15,18-Heneicosapentaenoic acid (HPA) is a ∆5 desaturase inhibitor. 6,9,12,15,18-Heneicosapentaenoic acid serves as a weak substrate for Prostaglandin H synthase and 5-lipoxygenase, yet it inactivates Prostaglandin H synthase at a rate comparable to that of AA, EPA and DHA. 6,9,12,15,18-Heneicosapentaenoic acid is a weak inducer of Aacyl-CoA oxidase. 6,9,12,15,18-Heneicosapentaenoic acid incorporates into phospholipids and triacylglycerols in cell culture. 6,9,12,15,18-Heneicosapentaenoic acid can be used in research related to liver cancer.
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(E)-KME-4
0 ImagesSynonyms: PGS-IN-1(E)-KME-4 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.
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AT-56 (Standard)
0 ImagesAT-56 (Standard) is the analytical standard of AT-56. This product is intended for research and analytical applications. AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2.
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mPGES1-IN-3
0 ImagesCat. No.: HY-100864CAS No.: 1469976-70-2mPGES1-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).
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HPGDS inhibitor 3
0 ImagesCat. No.: HY-146662CAS No.: 2255311-93-2HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity.
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Sargachromanol E
0 ImagesCat. No.: HY-123364CAS No.: 856414-54-5Sargachromanol E is an apoptosis inducer, anti-inflammatory agent, and anti-aging agent. Sargachromanol E activates caspase-3, mediates PARP cleavage, downregulates Bcl-xL and upregulates Bax levels, and drives sub-G1 phase cell cycle arrest, inhibits LPS-induced COX-2 and iNOS transcription and expression (NO: IC50 = 6.99 μg/mL), reduces p38 MAPK and ERK1/2 phosphorylation levels, and suppresses the release of pro-inflammatory mediators such as TNF-α, IL-1β, and prostaglandin E2 (PGE2). Sargachromanol E can be used for research on skin aging, leukemia, oral squamous cell carcinoma, and inflammation-related studies.
