PGE synthase Inhibitor

Pheophytin a is a multi-target inhibitor, anticancer agent, antioxidant and antiviral agent. Pheophytin a directly binds to and inhibits HCV-NS3/4A protease (IC₅₀=0.89 μM) to block viral replication. Pheophytin a also scavenges free radicals, reduces ferric ions, and exhibits cytotoxic activity against breast cancer cells. Pheophytin a effectively inhibits LPS-induced production of nitric oxide, prostaglandin E2, NOS2 and COX-2, as well as various pro-inflammatory cytokines, by downregulating the transcription levels of inflammatory mediators and blocking the ERK1/2 and STAT-1 pathways. In a low nerve growth factor environment, Pheophytin a also enhances ERK1/2 phosphorylation and synergistically promotes neurite outgrowth through MAPK pathway. Pheophytin a can be used to investigate the pathogenic mechanisms of diseases including chronic hepatitis C, sepsis, breast cancer and Alzheimer's disease.

Cannflavin B is a flavonoid compound that can be isolated from Cannabis sativa L. Cannflavin B is inhibitors of PGE₂ release (IC₅₀: 0.7 μM), mPGES-1 (IC₅₀: 3.7 μM), and 5-lipoxygenase. Cannflavin B has multiple activities such as anti-inflammatory, antioxidant, anti-glycation, anti-ferroptosis, anti-tumor, and anti-Leishmania (IC₅₀: 14 μM). Cannflavin B can also inhibit the TrkB-BDNF signaling pathway.

Crisdesalazine (AAD-2004) is a microsomal prostaglandin E₂ synthase-1 (mPGES-1) inhibitor. Crisdesalazine acts as a potent free radical scavenger that directly neutralizes reactive oxygen species (ROS) including hydrogen peroxide, exerting neuroprotective effects against apoptosis and axonal damage. Crisdesalazine inhibits PGE₂ production, mediates inflammatory responses, and promotes the conversion of macrophages from the pro-inflammatory M1 phenotype to the anti-inflammatory M2 phenotype. Crisdesalazine is applicable to neuroprotection research in multiple sclerosis and spinal cord injury.

UK4b is a highly selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor. UK4b possesses anti-inflammatory and analgesic effects. UK4b can block the growth of abdominal aortic aneurysms in mice.

SZ0232 is a selective mPGES-2 inhibitor. SZ0232 binds to the active site of mPGES-2 via hydrogen bonds and π-π stacking, reduces the production of prostaglandin E₂ (PGE₂) and blocks the PGE₂-EP3 pathway. SZ0232 regulates Ferroptosis by activating the heme-dependent p53/SLC7A11/GPX4 axis, inhibits lipid peroxidation, and protects renal tubules. SZ0232 enhances glucose-stimulated insulin secretion, inhibits β-cell senescence, and improves glucose homeostasis. SZ0232 reduces renal lipid accumulation, alleviates fibrosis, and ameliorates renal dysfunction in diabetic mice. SZ0232 inhibits renal cyst growth in polycystic kidney disease models. SZ0232 exhibits an insulinotropic effect that strengthens with the increase of animal age. SZ0232 can be used in studies related to type 2 diabetes, acute kidney injury, diabetic kidney disease, and autosomal dominant polycystic kidney disease.

mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice.

1-O-Hexadecylglycerol can up-regulate PPAR-γ expression, inhibit pGE2, and exhibit anti-inflammatory properties. 1-O-Hexadecylglycerol is effective in oral administration.

UT-11 is a potent and blood-brain barrier-permeable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with IC₅₀s of 0.10 μM and 2.00 μM for inhibiting PGE₂ production in human (SK-N-AS) and murine (BV2) cells, respectively.

hPGDS-IN-1 (Compound 2) is an hPGDS inhibitor with an IC₅₀ of 12 nM (as measured by fluorescence polarization assay or EIA). hPGDS-IN-1 can be used in the research of allergic rhinitis and spinal cord neurons.

Suprofen (TN-762) is a non-steroidal anti-inflammatory drug (NSAID).

(S)-Flurbiprofen (Standard) is the analytical standard of (S)-Flurbiprofen. This product is intended for research and analytical applications. (S)-Flurbiprofen is an active enantiomer of Flurbiprofen, with IC₅₀ values of 0.48 μM and 0.47 μM for COX-1 and COX-2, respectively.

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 PGE_E2; 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.

TFC-007 is a selective and orally effective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, with an IC₅₀ of 71 nM for H-PGDS. TFC-007 shows weak effects on L-PGDS and various arachidonic acid-related enzymes and receptors. TFC-007 inhibits PGD2 production in KU812 cells without decreasing H-PGDS protein levels. TFC-007 can be used for research on H-PGDS/PGD2 signaling and allergic rhinitis.

Desoxo-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.

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 (K_D = 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.

Sinensetin (Standard) is the analytical standard of Sinensetin. This product is intended for research and analytical applications.

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).

Pirprofen (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.

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.

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.