2. Signaling Pathways
  3. Apoptosis
    Metabolic Enzyme/Protease
  4. Glutathione Peroxidase

Glutathione Peroxidase

Glutathione Peroxidase

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Glutathione peroxidases (GPx) are a family of enzymes with the ability to reduce organic and inorganic hydroperoxides to the corresponding alcohols using glutathione or thioredoxin as an electron donor. These enzymes promote hydrogen peroxide metabolism and protect cell membrane structure and function from oxidative damage. Dysregulated GPx expression is connected with severe pathologies, including obesity and diabetes. GPx1 has been reported to be involved in both pro- and anticancer effects in different tumor models.

In mammals, the GPxs family consists of eight members (GPx1-GPx8) identified so far; five of them (GPx1-GPx4 and GPx6) contain selenocysteine in the catalytic center and the other three are cysteine-containing proteins. GPx1 is one of the most critical members of the GPxs family that catalytically reduces hydrogen peroxide to produce water. The function of GPx3 is to scavenge H2O2 and lipoperoxides in the plasma to reduce systematic oxidative stress and to maintain the bioavailability of vascular nitric oxide. Gpx4 is an essential mammalian glutathione peroxidase, which protects cells against detrimental lipid peroxidation and governs a novel form of regulated necrotic cell death, called ferroptosis.

Glutathione Peroxidase Isoform Specific Products:

Glutathione Peroxidase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-139008
    RC363
    		Activator
    RC363 is a novel probucol analog with the activity to protect mouse hippocampal cells and primary cortical neurons from glutamate-induced oxidative cell death (ferroptosis) and increase glutathione peroxidase (GPx) 1 levels and activity.
    RC363
  • HY-168879
    GPX4-IN-16
    		Inhibitor
    GPX4-IN-16 ((R)-9i) is a potent GPX4 inhibitor with an Kd value of 20.4 nM. GPX4-IN-16 shows cytotoxicity. GPX4-IN-16 shows anticancer activity.
    GPX4-IN-16
  • HY-139012
    RC574
    RC574 is a novel probucol analog with the activity to protect mouse hippocampal cells and primary cortical neurons from glutamate-induced oxidative cell death (ferroptosis) and increase glutathione peroxidase (GPx) 1 levels and activity.
    RC574
  • HY-133931
    Bimakalim
    		Inhibitor
    Bimakalim (EMD-52692) is an ATP-sensitive potassium channel opener. Bimakalim reduces transmural MPO activity. Bimakalim mimics the effects of ischemic preconditioning to reduce infarct size, adenosine release, and neutrophil function in dogs.
    Bimakalim
  • HY-179502
    Anti-inflammatory agent 107
    		Activator
    Anti-inflammatory agent 107 is an orally active anti-inflammatory agent. Anti-inflammatory agent 107 inhibits and NF-κB with a superior binding affinity of -9.4578 kcal/mol. Anti-inflammatory agent 107 reduces levels of inflammatory biomarkers (TNF-α, IL-6, INF-γ, NF-κβ, C-reactive protein and Erythrocyte Sedimentation Rate) and enhances the endogenous antioxidant defense system by elevating SOD (Superoxide Dismutase), CAT (Catalase) and GSH (Glutathione) activities. Anti-inflammatory agent 107 not induces liver toxicity and demonstrates hepatoprotective effects. Anti-inflammatory agent 107 dose-dependently ameliorates leukocyte infiltration and tissue edema. Anti-inflammatory agent 107 can be used for anti-inflammatory research.
    Anti-inflammatory agent 107
  • HY-162717
    GPX4-IN-11
    		Inhibitor
    GPX4-IN-11 (compound I14) is a potent inhibitor of GPX4, with the KD of 45.7 μM. GPX4-IN-11 plays an important role in ferroptosis research.
    GPX4-IN-11
  • HY-183294
    GPX4-IN-24
    		Inhibitor
    GPX4-IN-24 is an orally active glutathione peroxidase 4 (GPX4) inhibitor with a human IC50 of 10.90 μM, human Kd of 10.04 μM. GPX4-IN-24 suppresses GPX4 enzymatic activity, disrupts redox homeostasis, drives lipid peroxidation, promotes lipid peroxidation, and induces ferroptosis. GPX4-IN-24 can be used for the research of triple-negative breast cancer.
    GPX4-IN-24
  • HY-175811
    Ferroptosis inducer-10
    		Inhibitor
    Ferroptosis inducer-10 is a ferroptosis inducer. Ferroptosis inducer-10 can inhibit A549 cells growth with an IC50 of 0.76 μM. Ferroptosis inducer-10 can deplete GSH, elevate ROS and MDA, and downregulate GPX4 expression. Ferroptosis inducer-10 can induce cell G2/M phase and inhibit migration. Ferroptosis inducer-10 can be used for the research of cancer, such as non-small lung cancer.
    Ferroptosis inducer-10
  • HY-175041
    GPX4-IN-18
    		Inhibitor
    GPX4-IN-18 (Compound 17) is a ferrocene-containing inhibitor of glutathione peroxidase 4 (GPX4). GPX4-IN-18 is also an inducer of ferroptosis. GPX4-IN-18 can increase the production of ROS and malondialdehyde (MDA) levels in OS-RC-2 clear cell renal cell carcinoma cells. GPX4-IN-18 induces ferroptosis in HT-1080 cells with IC50s of 0.007 μM (absence of ferrostatin-1) and 1.486 μM (presence of ferrostatin-1). GPX4-IN-18 reduces in vivo tumor volume and intratumoral GPX4 levels in OS-RC-2 xenograft murine model.
    GPX4-IN-18
  • HY-182802
    Ferroptosis inducer-15
    		Inhibitor
    Ferroptosis inducer-15 is a ferroptosis inducer. Ferroptosis inducer-15 downregulates GPX4 expression, triggers lipid peroxidation via ROS accumulation, and disrupts mitochondrial membrane potential to drive ferroptosis. Ferroptosis inducer-15 increases splenic CD4+ T cell proportion, promotes CD8+ cytotoxic T cell tumor infiltration, and activates antitumor immune responses. Ferroptosis inducer-15 exerts antiproliferative activity against colorectal cancer cells and inhibits tumor growth in xenograft mice models without significant body weight loss. Ferroptosis inducer-15 can be used for the research of cancer, such as colorectal cancer.
    Ferroptosis inducer-15
  • HY-W001083S2
    3-Hydroxyphenylacetic acid-d6
    3-Hydroxyphenylacetic acid-d6 is the deuterium labeled 3-Hydroxyphenylacetic acid (HY-W001083). 3-Hydroxyphenylacetic acid is an orally active flavonoid metabolite produced by intestinal flora, with blood pressure-lowering activity. 3-Hydroxyphenylacetic acid can also inhibit ferroptosis by upregulating the expression of GPX4, thereby improving spermatogenic dysfunction in aged mice. In addition, abnormal levels of 3-Hydroxyphenylacetic acid are closely related to certain diseases, such as autism spectrum disorders.
    3-Hydroxyphenylacetic acid-d<sub>6</sub>
  • HY-179003
    mTOR/GLS1-IN-1
    		Inhibitor
    mTOR/GLS1-IN-1 (Compoud 9d) is a potent dual targeted mTOR/GLS1 inhibitor. Has anti proliferative activity against various tumor cells. mTOR/GLS1-IN-1 dose dependently induces ROS accumulation, induces autophagosome formation, and induces apoptosis. mTOR/GLS1-IN-1 can increase Fe2+, decrease GPX4, and induce ferroptosis. mTOR/GLS1-IN-1 can inhibit cell migration, invasion, and angiogenesis. mTOR/GLS1-IN-1 can be used in the research of cancer, such as breast cancer.
    mTOR/GLS1-IN-1
  • HY-W879508
    ALT-2074
    ALT-2074 (BXT-51071) is an orally active catalytic analogue of glutathione peroxidase. ALT-2074 is an inhibitor of human CYP3A, with its IC50 value ranging from 2.0 to 2.6 μM. ALT-2074 shows only a weak inhibitory effect on CYP3A in vivo, suggesting that it may not significantly affect the metabolism of CYP3A substrate drugs. ALT-2074 can be used to study inflammatory diseases characterized by reactive oxygen species, such as acute coronary syndrome.
    ALT-2074
  • HY-186143
    KY0418
    		Inhibitor
    KY0418 is a selective GPX4 inhibitor. KY0418 selectively and covalently modifies the selenocysteine residue of GPX4 and inhibits GPX4 activity. KY0418 induces ferroptosis and suppresses cell proliferation. KY0418 can be used for the study of ferroptosis and cancer.
    KY0418
  • HY-179384
    PROTAC FSP1 degrader 1
    		Activator
    PROTAC FSP1 degrader 1 is a highly efficient and selective PROTAC degrader targeting FSP1. PROTAC FSP1 degrader 1 significantly induces the accumulation of intracellular lipid peroxides. PROTAC FSP1 degrader 1 exhibits synergistic induction of ferroptosis with GPX4 inhibitors. PROTAC FSP1 degrader 1 can induce ROS production. PROTAC FSP1 degrader 1 upregulates the mRNA expression of ferroptosis-related proteins (GPX4, FTH1, ACSL4, TfR1, FSP1). PROTAC FSP1 degrader 1 can be used for the study of triple-negative breast cancer.
    PROTAC FSP1 degrader 1
  • HY-161972
    ZX782
    		Degrader
    ZX782 is a HyT GPX4 degrader and a ferroptosis inducer, which induces GPX4 degradation and significantly increases lipid ROS accumulation in HT1080 cells. ZX782 can be used to treat AD by reducing the size and/or number of brain amyloid plaques and by inhibiting the spread of IL-1beta-positive microglial-like cells around amyloid plaques. ZX782 is labeled with hydrophobic benzyl alcohol (HBA) and appears bright blue under acidic conditions, which can be used for quantitative determination. ZX782 is composed of target protein ligand (red part) ML-210 (HY-100003), PROTAC linker (black part) Bromo-PEG2-CH2-Boc (HY-141371) and Hty molecule (blue part) Adamantan-1-ylmethanamine (HY-W037848). The conjugate consisting of Hyt and linker parts is Adamantan-C-amide-PEG2-C-Br (HY-161974), and the activity control of the target protein ligand is Hydroxyl-ML-210 (HY-161973).
    ZX782
  • HY-100218AR
    RSL3 (Standard)
    		Inhibitor
    RSL3 (Standard) is the analytical standard of RSL3 (HY-100218A). This product is intended for research and analytical applications. RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.
    RSL3 (Standard)
  • HY-17355BS
    Dexpramipexole-d3 dihydrochloride
    		Activator
    Dexpramipexole-d3 ((R)-Pramipexole-d3) dihydrochloride is the deuterium labeled Dexpramipexole. Dexpramipexole ((R)-Pramipexole) dihydrochloride is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole dihydrochloride upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole dihydrochloride induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole dihydrochloride is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.
    Dexpramipexole-d<sub>3</sub> dihydrochloride
  • HY-100002R
    ML162 (Standard)
    		Inhibitor
    ML162 (Standard) is the analytical standard of ML162 (HY-100002). This product is intended for research and analytical applications. ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor. ML162 has a selective lethal effect on mutant RAS oncogene-expressing cell lines
    ML162 (Standard)
  • HY-19321R
    PF-06282999 (Standard)
    		Inhibitor
    PF-06282999 (Standard) is the analytical standard of PF-06282999. This product is intended for research and analytical applications. PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases.
    PF-06282999 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Glutathione Peroxidase Isoform Comparison

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