mpges 1 inhibitor 1

mPGES-1 Inhibitor-1 is a novel selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with anti-inflammatory and analgesic activity for the study of acute liver injury.

PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.

Zaloglanstat (ISC-27864) is a selective, orally active mPGES-1 inhibitor with an IC50 of 5 nM against human mPGES-1, demonstrating analgesic effects in osteoarthritis and inflammatory arthritis.

mPGES1-IN-3 is a potent and selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) .

MF63 is a selective mPGES-1 inhibitor (IC50: 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively).

HPGDS inhibitor 1 is a novel and selective inhibitor for Hematopoietic Prostaglandin D Synthase (HPGDS) with an IC50 Value of 0.7 nM.

α-Gracinoic acid acts as an inhibitor of mPGES-1, exhibiting anti-inflammatory properties.

mPGES1-IN-4 (compound 32) is a multi-substituted pyrimidine compound acting as a submicromolar inhibitor of PGE2 production. It primarily exerts its anti-inflammatory effects by inhibiting mPGES-1 and significantly suppresses acute inflammation models in vivo.

mPGES1-IN-5 (compound 18) is a multi-substituted pyrimidine compound that acts as a submicromolar inhibitor of PGE2 production. It primarily exerts its anti-inflammatory effects by inhibiting mPGES-1 and demonstrates significant inhibitory activity in vivo against acute inflammation models.

KH176m serves as a selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), effectively suppressing mPGES-1 expression. It inhibits the growth of DU145-derived spheroids, but does not affect cells with low mPGES-1 expression such as LNCaP. As an antioxidant and redox modulator, KH176m demonstrates high efficacy in combating cardiac oxidative stress, with its impact varying according to the duration of ischemia. It holds potential therapeutic value in alleviating acute cardiac ischemia-reperfusion injury (IRI).

AGU654 (Compound 44) is a selective mPGES-1 inhibitor with an IC50 value of 2.9 nM against mPGES-1. By inhibiting mPGES-1, AGU654 interrupts the pathway where COX-1/2 converts arachidonic acid to prostaglandin E2 (PGE2), effectively reducing inflammatory responses, pain, and fever symptoms. In models using activated human monocyte-derived macrophages and whole blood, AGU654 selectively inhibits PGE2 production induced by bacterial endotoxins, while preserving the production of other prostaglandins. In guinea pig models, AGU654 significantly alleviates fever, inflammation, and inflammatory pain, demonstrating excellent anti-inflammatory, analgesic, and antipyretic effects. AGU654 holds promise as a new approach for researching inflammatory diseases and pain.

mPGES-1/sEH-IN-1 (compound 1f) is an sEH inhibitor with an IC50 value of 5 μM. It also exhibits antitumor activity by inhibiting mPGES-1, with an IC50 value of 25 µM.

mPGES-1/5-LOX-IN-1 (compound 3j) is a potent, orally active dual inhibitor of mPGES-1 and 5-LOX, with IC50 values of 0.92 and 1.89 µM, respectively. Additionally, mPGES-1/5-LOX-IN-1 exhibits anti-inflammatory properties.

AGU661 is an inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) with an IC50 of 0.22 nM. It effectively reduces PGE2 production in human pro-inflammatory M1 macrophages and activated monocytes without affecting other lipid mediator pathways. Despite its poor physicochemical properties, low metabolic stability, and high plasma protein binding rate, encapsulating AGU661 in PLGA-based nanoparticles significantly enhances its bioactivity. AGU661 is applicable for research on inflammatory diseases.

mPGES1-IN-10 (Compound 7d) is a potent inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) with an IC50 value of 1.0 μM. It holds potential for research into chronic inflammation-related diseases and malignant tumors, such as colorectal cancer.

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 dose-dependently reduces the production of PGE2 with EC50=12 μM in IL-1β-stimulated A549 cells [1].

CAY10526 (BTH) is a selective mPGES-1 inhibitor that acts as an inhibitor of the NF-κB signaling pathway.

CAY10589 is an mPGES-1 inhibitor.

FR20 is a human microsomal prostaglandin synthase 1 (mPGES 1) inhibitor.

Crisdesalazine (AAD 2004) is an inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1). Crisdesalazine reduces autophagosome formation, axonopathy, and motor neuron degeneration, improving motor function and increasing life span.

2,5-dimethyl Celecoxib is a derivative of celecoxib that does not inhibit COX-2 (IC50 = >100 μM).1 It does inhibit microsomal prostaglandin E synthase-1 (mPGES-1) in HeLa cells (IC50 = 15.6 μM) and reduces prostaglandin E2 production in HeLa, A549, and HCA-7 cells (IC50s = 0.64, 0.83, and 3.08 μM, respectively).2 It inhibits proliferation of drug-sensitive RPMI8226 and multidrug-resistant 8226/Dox40 multiple myeloma cells, as well as increases the rate of apoptosis when used at concentrations of 20 and 30 μM.3 2,5-dimethyl Celecoxib reduces the expression of survivin, cyclin A, cyclin B, MEK1, and MEK2 in 8226/Dox40 cells. The antiproliferative effect of 2,5-dimethyl celecoxib is independent of mPGES-1 inhibition.2References1. Zhu, J., Song, X., Lin, H.-P., et al. Using cyclooxygenase-2 inhibitors as molecular platforms to develop a new class of apoptosis-inducing agents. J. Natl. Cancer Inst. 94(23), 1745-1757 (2002).2. Wobst, I., Schiffmann, S., Birod, K., et al. Dimethylcelecoxib inhibits prostaglandin E2 production. Biochem. Pharmacol. 76(1), 62-69 (2008).3. Kardosh, A., Soriano, N., Liu, Y.-T., et al. Multitarget inhibition of drug-resistant multiple myeloma cell lines by dimethyl-celecoxib (DMC), a non-COX-2 inhibitory analog of celecoxib. Blood 106(13), 4330-4338 (2005). 2,5-dimethyl Celecoxib is a derivative of celecoxib that does not inhibit COX-2 (IC50 = >100 μM).1 It does inhibit microsomal prostaglandin E synthase-1 (mPGES-1) in HeLa cells (IC50 = 15.6 μM) and reduces prostaglandin E2 production in HeLa, A549, and HCA-7 cells (IC50s = 0.64, 0.83, and 3.08 μM, respectively).2 It inhibits proliferation of drug-sensitive RPMI8226 and multidrug-resistant 8226/Dox40 multiple myeloma cells, as well as increases the rate of apoptosis when used at concentrations of 20 and 30 μM.3 2,5-dimethyl Celecoxib reduces the expression of survivin, cyclin A, cyclin B, MEK1, and MEK2 in 8226/Dox40 cells. The antiproliferative effect of 2,5-dimethyl celecoxib is independent of mPGES-1 inhibition.2 References1. Zhu, J., Song, X., Lin, H.-P., et al. Using cyclooxygenase-2 inhibitors as molecular platforms to develop a new class of apoptosis-inducing agents. J. Natl. Cancer Inst. 94(23), 1745-1757 (2002).2. Wobst, I., Schiffmann, S., Birod, K., et al. Dimethylcelecoxib inhibits prostaglandin E2 production. Biochem. Pharmacol. 76(1), 62-69 (2008).3. Kardosh, A., Soriano, N., Liu, Y.-T., et al. Multitarget inhibition of drug-resistant multiple myeloma cell lines by dimethyl-celecoxib (DMC), a non-COX-2 inhibitory analog of celecoxib. Blood 106(13), 4330-4338 (2005).

CAY10678 is an mPGES-1 inhibitor that inhibits PD-1.CAY10678 reduces collagen deposition and T-cell depletion, and may be used to study melanoma.CASHIPS

BRP-201 is a selective, novel, and potent inhibitor of mPGES-1 (IC50: 0.42 μM) and is considered a promising therapeutic target for the next generation of anti-inflammatory drugs for the treatment of inflammatory diseases.

Embelin (Embelic acid), isolated from the Japanese Ardisia herb, is an inhibitor of the X-linked inhibitor of apoptosis (IC50: 4.1 uM).