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 a specific PPARγ agonist and also inhibits P21-activated kinase 1(PAK1) and NF-Κb. 5-Aminosalicylic Acid has anti-cancer and anti-inflammatory activities. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

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.

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

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

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.

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

GSTO1-IN-1 is a potent glutathione S-transferase omega 1 inhibitor (GSTO1) with an IC₅₀ of 31 nM.

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

NBDHEX is a potent inhibitor of glutathione S-transferase P1-1 (GSTP1-1) .

4-Aminosalicylic acid (para-aminosalicylic acid) is an analog of para-aminobenzoic acid (PABA) with antitubercular activity.

AZD5904 is a potent and irreversible human Myeloperoxidase (MPO) inhibitor(IC₅₀ of 140 nM and has similar potency in mouse and rat).

ZX782 acts as a GPX4 protein degrader and an inducer of ferroptosis (Ferroptosis), targeting GPX4 for destruction via both the ubiquitin-proteasome system and the autophagy-lysosome pathway. Following the degradation of GPX4 induced by ZX782, there is a significant increase in the accumulation of lipid reactive oxygen species (ROS) in HT1080 cells.

Ezatiostat hydrochloride (TLK199 HCl) is an effective inhibitor of glutathione S-transferase. Ezatiostat hydrochloride is a novel glutathione analog and the potential treatment of cytopenias. In addition, Ezatiostat hydrochloride has been revealed to selectively bind to and thus inhibit GSTP1-1.

PF-1355 (PF 06281355) is a selective 2-thiouracil mechanism-based MPO inhibitor. PF-1355 is used for treatment of vasculitic diseases.

JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor and the active metabolite of ML-210, which is converted to butyronitrile oxide JKE-1777. JKE-1674 kills LOX-IMVI cells in the same manner as ML-210 and is completely rescued by ferroptosis inhibitors.

N-Acetyl lysyltyrosylcysteine amide is a non-toxic, potent, reversible, and specific myeloperoxidase (MPO) tripeptide inhibitor that effectively inhibits MPO production in vivo, attenuates neuronal damage, preserves brain tissue and neurological function post-stroke, and inhibits MPO-dependent hypochlorite (HOCl) production, protein nitration, and LDL oxidation. It is also used in the study of bronchial dysplasia.

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.

Tinoridine hydrochloride (Y-3642 hydrochloride) is a non-steroidal anti-inflammatory drug. Tinoridine hydrochloride (5-100 μM), produced a concentration-dependent inhibition on the simultaneous increases in lipid peroxide formation and renin release induced by 50 μM ascorbic acid in the renin granule fraction. On the other hand, indomethacin, hydrocortisone, and prednisolone, which had no ability to inhibit the lipid peroxidation in the renin granule fraction, did not influence the release of renin from the granules. These results suggest that tinoridine suppresses renin release by inhibiting the oxidative disintegration of membranes of renin granules.

Ezatiostat (TER199(free base)) is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity.

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

Verdiperstat (AZD 3241) is a selective, irreversible and orally active myeloperoxidase inhibitor, with an IC₅₀ of 630 nM, and can be used in the research of neurodegenerative brain disorders.