PGE synthesis (prostaglandin E synthase, PGES), which converts cyclooxygenase (COX)-derived prostaglandin (PG) H2 to PGE2, occurs in multiple forms with distinct enzymatic properties, modes of expression, cellular and subcellular localizations and intracellular functions. Cytosolic PGES (cPGES) is a cytosolic protein that is constitutively expressed in a wide variety of cells and tissues and is associated with heat shock protein 90 (Hsp90). Membrane-associated PGES (mPGES), the expression of which is stimulus-inducible and is downregulated by anti-inflammatory glucocorticoids, is a perinuclear protein belonging to the microsomal glutathione S-transferase (GST) family.
|Zomepirac sodium salt
|Zomepirac sodium is a pyrrole-acetic acid structurally related to tolmetin sodium and a prostaglandin synthetase inhibitor.
|Suprofen is a COX1/2 inhibitor and a non-steroidal anti-inflammatory drug (NSAID).
|Pranoprofen is a non-steroidal COX inhibitor with anti-inflammatory effects, used in treatment of ophthalmology.
|Pizuglanstat is a hematopoietic prostaglandin synthase inhibitor.
|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.
|KW-8232 free base
|KW-8232 free base is an anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.
|HQL-79 is a selective inhibtor of hematopoietic prostaglandin D (PGD) synthase, one of two synthases involved in the production of prostaglandin D2 (PGD2) from arachidonic acid.
|hPGDS-IN-1 is a hPGDS inhibitor ,with IC50 of 12 nM in the Fluorescence Polarization Assay or the EIA assay.
|HPGDS inhibitor 1
|HPGDS inhibitor 1 is a selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.
|HPGDS inhibitor 2
|GSK-2894631A is a highly potent and selective HPGDS inhibitor with IC50 value of 9.9nM.
|Flurbiprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity.
|Bismuth subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.
|AT 56 is an orally active L-PGDS inhibitor with IC50 value of 95μM. It inhibits the production of PGD2 from PGH2 in vitro, with no effect on PGE2 or PGF2α production.