2. Signaling Pathways
  3. Immunology/Inflammation
  4. PGE synthase

PGE synthase

Prostaglandin E synthase

PGE synthase

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-111140
    YS121
    		Inhibitor 99.74%
    YS121 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.
    YS121
  • HY-N0297R
    Sinensetin (Standard)
    		Inhibitor
    Sinensetin (Standard) is the analytical standard of Sinensetin. This product is intended for research and analytical applications.
    Sinensetin (Standard)
  • HY-B0464S1
    Hydralazine-d5 (hydrochloride)
    		Inhibitor 99.9%
    Hydralazine-d5 (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464). 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.
    Hydralazine-d<sub>5</sub> (hydrochloride)
  • HY-125415
    PF-4693627
    		Inhibitor 99.63%
    PF-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).
    PF-4693627
  • HY-106907
    Furprofen
    		Inhibitor 98.90%
    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.
    Furprofen
  • HY-19622
    PF-9184
    		Inhibitor 98.10%
    PF-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.
    PF-9184
  • HY-156612
    Friluglanstat
    		Inhibitor
    Friluglanstat is a prostaglandin E synthase (mPGES-1) inhibitor, with anti-inflammatory activity.
    Friluglanstat
  • HY-126134
    HPGDS inhibitor 2
    		Inhibitor 99.72%
    HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM.
    HPGDS inhibitor 2
  • HY-N4267
    Yangambin
    		Inhibitor 98.27%
    Yangambin 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.
    Yangambin
  • HY-B0464S
    Hydralazine-d4 (hydrochloride)
    		Inhibitor
    Hydralazine-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.
    Hydralazine-d<sub>4</sub> (hydrochloride)
  • HY-N11011
    Withaphysalin A
    		Inhibitor 98%
    Withaphysalin 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.
    Withaphysalin A
  • HY-W268542
    4-Acetylaminoantipyrine
    		Inhibitor 99.60%
    4-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.
    4-Acetylaminoantipyrine
  • HY-141469
    6,9,12,15,18-Heneicosapentaenoic acid
    		99.4%
    6,9,12,15,18-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.
    6,9,12,15,18-Heneicosapentaenoic acid
  • HY-101587
    (E)-KME-4
    		Inhibitor 99.51%
    (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.
    (E)-KME-4
  • HY-13988R
    AT-56 (Standard)
    		Inhibitor
    AT-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.
    AT-56 (Standard)
  • HY-100864
    mPGES1-IN-3
    		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).
    mPGES1-IN-3
  • HY-146662
    HPGDS inhibitor 3
    		Inhibitor
    HPGDS 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.
    HPGDS inhibitor 3
  • HY-N7878
    Tectorigenin sodium sulfonate
    		Inhibitor
    Tectorigenin sodium sulfonate is the product of tectorigenin sulfonated with sulfuric acid and mixed with saturated salt water. Tectorigenin sodium sulfonate has high water-solubility and good antioxidant properties.
    Tectorigenin sodium sulfonate
  • HY-129199
    U-51605
    		Inhibitor
    U-51605 is a platelet aggregation inhibitor and inhibits thromboxane synthesis. U-51605 is also a prostaglandin I2 synthase inhibitor and can inhibit the retinal vasodilation response induced by NO donors (such as NOR3).
    U-51605
  • HY-N3380
    Linderaspirone A
    		Inhibitor
    Linderaspirone A is a natural compound that can be isolated from the roots of Lindera aggregate. Linderaspirone A shows significant inhibitory effects on the production of prostaglandin E2 (PGE2),TNF-α, and IL-6 .
    Linderaspirone A
Cat. No. Product Name / Synonyms Application Reactivity