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

Glutathione Peroxidase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-181656
    GPX4 degrader-2
    Inhibitor
    GPX4 degrader-2 is a GPX4 molecular glue degrader and ferroptosis inducer. GPX4 degrader-2 suppresses GPX4 enzyme activity, promotes ubiquitination-dependent proteasomal degradation of GPX4 protein. GPX4 degrader-2 indues ferroptosis, increases lipid ROS and MDA levels, suppresses glutathione levels in cancer cells. GPX4 degrader-2 inhibits cancer cells proliferation and colony formation. GPX4 degrader-2 can be used for the research of colorectal cancer.
    GPX4 degrader-2
  • HY-182072
    GPX4-IN-23
    Inhibitor
    GPX4-IN-23 (Compound 3e) is a GPX4 inhibitor with an IC50 of 0.27 μM. GPX4-IN-23 induces Ferroptosis by enhancing lipid peroxidation, ROS production, and intracellular GSH depletion. GPX4-IN-23 exhibits antiproliferative activity against central nervous system cancer cells. GPX4-IN-23 can be used in studies related to central nervous system cancers.
    GPX4-IN-23
  • HY-181598
    GPX4 degrader-1
    Degrader
    GPX4 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated GPX4 degrader (DC50: 8.9 nM in HT1080 cells) GPX4 degrader-1 induces GPX4 degradation. GPX4 degrader-1 induces Ferroptosis. GPX4 degrader-1 increases lipid ROS. GPX4 degrader-1 demonstrates potent antitumor efficacy in a murine mammary carcinoma model.
    GPX4 degrader-1
  • HY-168958
    Ferroptosis-IN-18
    Activator
    Ferroptosis-IN-18 (51), a promethazine derivative, shows strong anti-ferroptosis and anti-oxidant properties. Ferroptosis-IN-18 (51) can be used in the research for intracerebral hemorrhage (ICH).
    Ferroptosis-IN-18
  • HY-163272
    GPX4/CDK-IN-1
    Inhibitor
    GPX4/CDK-IN-1 (Compound B9) is a dual inhibitor of GPX4 and CDK, with IC50 values of 542.5 nM, 191.2 nM and 68.1 nM for GPX4, CDK4 and CDK6, reapectively. GPX4/CDK-IN-1 shows strong cancer cell growth inhibition in vivo.
    GPX4/CDK-IN-1
  • HY-183554
    Fa-Au
    Inhibitor
    Fa-Au is a TrxR inhibitor. Fa-Au downregulates GPX4, induces oxidative stress, mitochondria-associated ferroptosis (ferroptosis) and immunogenic cell death. Fa-Au induces ROS production in hepatoma cells. Fa-Au remodels the tumor immune microenvironment via M1 macrophage polarization, dendritic cell maturation, CD8+ T cell activation and reduction of regulatory T cells. Fa-Au induces an anti-tumor immune feedback loop through the IFNγ/STAT1/SLC7A11 axis. Fa-Au inhibits tumor growth. Fa-Au is applicable to hepatocellular carcinoma-related research.
    Fa-Au
  • HY-179299
    POI ligand-2-NH-C10H20-NH-Boc
    Ligand
    POI ligand-2-NH-C10H20-NH-Boc is a target protein ligand linker conjugate that contains a GPX4 ligand (HY-179294) and a PROTAC linker (HY-W047688), which can recruit E3 ligases. POI ligand-2-NH-C10H20-NH-Boc can be used for synthesis of PROTAC GPX4 degrader-5 (HY-178925).
    POI ligand-2-NH-C10H20-NH-Boc
  • HY-P2818B
    Alkaline phosphatase, Chicken Intestine
    Inhibitor
    Alkaline Phosphatase (Apase), Chicken Intestine is an alkaline phosphatase from Chicken Intestine, and is one of the most active alkaline phosphatases. Alkaline phosphatase, Chicken Intestine is an orally active membrane-bound glycoprotein that catalyzes the hydrolysis of phosphate monoesters at alkaline pH. Alkaline phosphatase, Chicken Intestine reduces myeloperoxidase activity and bacterial translocation. Alkaline phosphatase, Chicken Intestine improves survival rate of mice infected with E. coli. Alkaline phosphatase, Chicken Intestine improves TNBS-induced colon inflammation.
    Alkaline phosphatase, Chicken Intestine
  • HY-182052
    anti-NSCLC agent-2
    Inhibitor
    anti-NSCLC agent-2 exhibits nanomolar anti-proliferative activity and acts on wild-type and drug-resistant non-small cell lung cancer (NSCLC) cells. anti-NSCLC agent-2 downregulates ferroptosis-related factors SLC7A11 and GPX4, disrupts cellular redox homeostasis, depletes glutathione, accumulates lipid peroxides, and simultaneously elevates mitochondrial nitric oxide and ROS levels to induce ferroptosis in tumor cells. anti-NSCLC agent-2 is applicable to research related to non-small cell lung cancer.
    anti-NSCLC agent-2
  • HY-181447
    GPX4 (S)-9i
    Inhibitor
    GPX4 (S)-9i is a GPX4 inhibitor and ferroptosis inducer, with its (R) enantiomer exhibiting stronger activity. GPX4 (S)-9i can be used for the study of fibrosarcoma.
    GPX4 (S)-9i
  • HY-N16658
    Asperilin
    Activator
    Asperilin (NSC 85238) is an orally active sesquiterpene lactone. Asperilin is an effective hydroxyl radical scavenger. Asperilin significantly enhance the lipid peroxidation levels of liver microsomes in various systems. Asperilin leads to a significant decrease in liver glutathione (GSH) levels and an increase in glutathione peroxidase (GPx) activity. Asperilin can be used for research on inflammatory conditions.
    Asperilin
  • HY-183791A
    Ferroptosis/apoptosis inducer-5
    Inhibitor
    Ferroptosis/apoptosis inducer-5 (Compound 14) is an orally active inducer of Ferroptosis and Apoptosis. Ferroptosis/apoptosis inducer-5 downregulates GPX4, upregulates ACSL4, promotes ROS production, activates the Caspase cascade, induces Mitochondrial dysfunction, and alters the Bcl-2/Bax balance. Ferroptosis/apoptosis inducer-5 significantly inhibits tumor growth in a pancreatic cancer xenograft mouse model. Ferroptosis/apoptosis inducer-5 can be used for the research of pancreatic cancer.
    Ferroptosis/apoptosis inducer-5
  • HY-170509
    Ferroptosis-IN-17
    Activator
    Ferroptosis-IN-17 (Compound 18) is a ferroptosis (Ferroptosis) inhibitor with an EC50 value of 0.57 μM. Ferroptosis-IN-17 reduces intracellular ferrous ion accumulation, lipid peroxidation, and effectively restores the levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4). Ferroptosis-IN-17 shows good solubility and significant metabolic stability in rat plasma. Ferroptosis-IN-17 is promising for research in tumor suppression, neurodegenerative diseases, and cardiovascular diseases.
    Ferroptosis-IN-17
  • HY-W018161S
    Hexadecanedioic acid-d28
    99.21%
    Hexadecanedioic acid-d28 is the deuterium labeled Hexadecanedioic acid (HY-W018161). Hexadecanedioic acid (Thapsic acid) is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits IRE1α-XBP1s-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease.
    Hexadecanedioic acid-d<sub>28</sub>
  • HY-126017
    Aminopyridine 2
    Inhibitor
    Aminopyridine 2 is an irreversible, selective, and orally active myeloperoxidase (MPO) inhibitor, with an IC50 of 0.16 μM and a Ki of 24 μM against human MPO. Aminopyridine 2 is applicable to research on chronic inflammatory diseases.
    Aminopyridine 2
  • HY-176274
    FASN/SCD-IN-1
    Agonist
    FASN/SCD-IN-1 is a Silybin (HY-N0779A) derivative, an orally active inhibitor of Fatty Acid Synthase (FASN)/Stearoyl-CoA Desaturase (SCD). FASN/SCD-IN-1 has shown in vitro activity in inhibiting lipid deposition, reducing FASN and SCD transcriptional levels, and exhibiting antioxidant, anti-inflammatory, and anti-fibrotic activities. FASN/SCD-IN-1 has demonstrated significant hepatoprotective effects in a rat model of acute liver injury. FASN/SCD-IN-1 ameliorates the pathological features of MASH liver, including steatosis, inflammation, and fibrosis in a mouse model of myeloproliferative steatohepatitis (MASH). FASN/SCD-IN-1 can be used to study MASH.
    FASN/SCD-IN-1
  • HY-178447
    PPARγ agonist 20
    Agonist
    PPARγ agonist 20 is a potent, orally active PPAR-γ agonist. PPARγ agonist 20 effectively increases antioxidant defenses (SOD, GSH) and reduces lipid peroxidation. PPARγ agonist 20 can upregulate of Pparg, Glut4, and AdipoQ, suppresses of TNF-α, IL-6, and NF-κB p65. PPARγ agonist 20 significantly lowers fasting blood glucose, improving glucose tolerance, and restoring metabolic balance in Streptozotocin (HY-13753)-Nicotinamide (HY-B0150)-induced diabetic rats. PPARγ agonist 20 can be used for the study of type 2 diabetes.
    PPARγ agonist 20
  • HY-175852
    Ferroptosis inducer-11
    Inhibitor
    Ferroptosis inducer-11 is a ferroptosis inducer. Ferroptosis inducer-11 exhibits potent cytotoxicity against HCT-116, NCM-60 and HT-29 cells with IC50 values of 0.43 μM, 3.14 μM and 0.48 μM, respectively. Ferroptosis inducer-11 strongly suppresses GPX4 enzymatic activity with an IC50 of 1.86 μM. Ferroptosis inducer-11 induces ferroptosis, as well as increases intracellular lipid ROS, malondialdehyde (MDA), and Fe2+ levels, while decreasing glutathione (GSH) levels in colon cancer cells. Ferroptosis inducer-11 can be used for the study of colon cancer.
    Ferroptosis inducer-11
  • HY-147691
    MPO-IN-5
    Inhibitor
    MPO-IN-5 (compound 1) is a potent, irreversible MPO (myeloperoxidase) inhibitor. MPO-IN-5 inhibits MPO peroxidation and hERG binding, with IC50 values of 0.22 and 2.8 μM, respectively. MPO-IN-5 shows rapid kinetics of inhibition, with enzyme inactivation rate (kinact/Ki) of 23000 M−1s−1.
    MPO-IN-5
  • HY-N17850
    5-Hydroxy-6,7-dimethoxyflavone
    Activator
    5-Hydroxy-6,7-dimethoxyflavone is an orally active inhibitor of ferroptosis (Ferroptosis). 5-Hydroxy-6,7-dimethoxyflavone inhibits H1N1 virus-induced ferroptosis by upregulating the expression of SLC7A11 and GPX4. 5-Hydroxy-6,7-dimethoxyflavone alleviates inflammatory responses and inhibits apoptosis by suppressing the activation of the NF-κB and p38 MAPK signaling pathways. 5-Hydroxy-6,7-dimethoxyflavone can be used in studies related to H1N1 influenza virus infection.
    5-Hydroxy-6,7-dimethoxyflavone
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