glutathione peroxidase

Glutathione Peroxidase (GSH-Px; EC 1.11.1.9), a member of the peroxidase family, catalyzes the oxidation of reduced glutathione (GSH) to oxidized glutathione (GSSG) by forming a disulfide bridge, while concurrently reducing hydrogen peroxide or lipid peroxides to water, serving as a potent antioxidant and protecting against oxidative stress [1].

5-Aminosalicylic Acid (5-ASA) is an anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE.

RSL3 (RSL3 1S) is an inhibitor of GPX4, and inhibits system xc- that blocks GSH synthesis (IC50=100 nM). RSL3 is a VDAC-independent activator of ferroptosis that is selective for tumor cells carrying oncogenic RAS.

AZD8309 is a potent, orally available antagonist of the chemokine receptor CXCR2 that regulates neutrophil transport, significantly reduces MPO in the pancreas and lung, and decreases trypsin and elastase activity in the pancreas.AZD8309 can be used to study a range of inflammatory diseases.

GPX4-IN-4 (Compound 24) is a potent inhibitor of GPX4, employed in cancer research [1].

NC-R17, an RSL3-based noncovalent GPX4 degrader implicated in ferroptosis, demonstrates anti-tumor activity and is utilized in the design of noncovalent GPX4-targeted proteolysis targeting chimeras (PROTACs) [1].

LAS17 is a selective and highly effective inhibitor of glutathione S-transferase Pi (GSTP1), which inhibits GSTP1 activity in vitro in a concentration-dependent manner. LAS17 has anti-tumor activity and inhibits breast cancer cell growth.

Lepadin E, a notably cytotoxic compound, effectively stimulates ferroptosis via the canonical p53-SLC7A11-GPX4 pathway. By elevating p53 and repressing SLC7A11 and GPX4 expression, it heightens ROS and lipid peroxidation while also augmenting ACSL4 expression, culminating in cell death. This compound exhibits a considerable antitumor effect [1].

Moracin N, a ferroptosis inhibitor derived from mulberry leaves, exhibits neuroprotective activity by mitigating oxidative stress [1].

Mitiperstat is a potent myeloperoxidase (MPO) inhibitor that is effective in preventing cardiovascular diseases such as heart failure and coronary artery disease.

Ferroptosis-IN-17 (Compound 18) is an inhibitor of ferroptosis with an EC50 value of 0.57 μM. It effectively reduces the accumulation of intracellular ferrous ions and lipid peroxidation while restoring levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4). In rat plasma, Ferroptosis-IN-17 demonstrates good solubility and notable metabolic stability. This compound holds potential for research in tumor suppression, neurodegenerative diseases, and cardiovascular disorders.

GPX4-IN-16 ((R)-9i) is a potent inhibitor of GPX4 with a KD value of 20.4 nM, exhibiting cytotoxic properties and anticancer activity.

Monoamine OxidaseB inhibitor 6 (Compound BT5) is a highly selective, reversible, and competitive MAO-B inhibitor capable of crossing the blood-brain barrier, with an IC50 of 0.11 μM. It exhibits antioxidant and neuroprotective properties, making it suitable for research into neurodegenerative diseases.

LOC1886 is a covalent inhibitor of GPX4, with slightly lower potency compared to RSL3 and ML162.

ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor that induces ferroptosis. ML162 has antitumor activity and selectively inhibits cell lines expressing mutant RAS oncogenes.

MPO-IN-1 is an orally active myeloperoxidase (MPO) inhibitor, inhibiting MPO and thyroid peroxidase (TPO). It is useful in inflammation research.

Nabumetone (BRL14777)(BRL14777) is a non-steroidal anti-inflammatory drug and its active metabolite 6MNA inhibits the enzymes cyclo-oxygenase I and II.

4-Methylesculetin (Methylesculetin) is one of the coumarin derivatives with great anti-oxidant and anti-inflammatory activities.

Melatonin (Melatonine) is a natural hormone secreted by the pineal gland that activates melatonin receptors. Melatonin is a hormone that regulates the biological clock and also has antioxidant and anti-inflammatory activities.

4-POBN (Myeloperoxidase Inhibitor 1) is a potent and irreversible inhibitor of myeloperoxidase (IC50 = 0.3 µM). 4-POBN can be used in studies about subacute stroke.

Cefdinir (FK-482) is a third-generation, semi-synthetic cephalosporin antibiotic effective against common bacterial infections of the ear, sinus, throat, and skin.

ML-210 (CID 49766530) is a glutathione peroxidase 4 (GPX4) inhibitor (EC50=30 nM) that is covalent and selective. ML-210 has antitumor activity and induces ferroptosis.

PF-06282999, a potent and selective myeloperoxidase inhibitor, is potentially useful for the treatment of cardiovascular diseases.

MPO-IN-28 is a novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM.