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.

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.

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

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

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.

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.

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].

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].

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.

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

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.

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.

SN50 is a cell permeable NF-κB translocation inhibitor.

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