gpx

3-Deoxyglucosone(3-Deoxy-D-glucosone) is synthesized by the intermediate pathway of the melad and polyol reactions.3-Deoxyglucosone reacts rapidly with protein amino groups to form advanced glycosylated end proteins (AGEs).3-Deoxyglucosone inactivates glutathione peroxidase and synergizes with low glucose to enhance GLP-1 secretion.3-Deoxyglucosone is used as a biomarker for diabetes mellitus.3-Deoxyglucosone has been shown to be an inhibitor of GLP-1 secretion in the presence of low glucose. 3-Deoxyglucosone inactivates glutathione oxidase, synergizes with low glucose to enhance GLP-1 secretion, and can be used as a biologic marker for diabetes.

Misonidazole as a novel GPX inhibitors to cause oxidative stress in chemotherapy-resistant tumors.

GPX4-IN-19 is a highly effective small-molecule inhibitor of glutathione peroxidase 4 (GPX4) with an IC50 value of 0.311 μM, which exerts its pharmacological activity by covalently binding to the Sec46 active site of GPX4, thereby disrupting lipid peroxide detoxification, inducing intracellular Fe²⁺ accumulation, elevating lipid peroxide (LPO) and reactive oxygen species (ROS) levels, triggering ferroptosis-associated DNA damage, demonstrating strong anti-proliferative effects with high ferroptosis selectivity, and providing a robust experimental tool for mechanistic and therapeutic studies in Triple-Negative Breast Cancer (TNBC).

GPX4-IN-3 (26a) is a potent inhibitor of glutathione peroxidase 4 (GPX4), selectively inducing ferroptosis. It demonstrates a 71.7% inhibition rate of GPX4 at a concentration of 1 μM .

GPX4-IN-5 is a small molecule covalent GPX4 inhibitor (IC50: 0.12 μM) with antitumour activity.GPX4-IN-5 induces ferroptosis and can be used for the prevention and treatment of triple-negative breast cancer (TNBC).

GPX4-IN-6 is a small molecule covalent GPX4 inhibitor (IC50: 0.12 μM) with antitumour activity.GPX4-IN-6 induces ferroptosis and is used for the treatment= and prevention of triple negative breast cancer (TNBC).

GPX-100 (13-deoxydoxorubicin) is an analogue of the anthracycline antitumour antibiotic doxorubicin. GPX-100 inserts into DNA and interacts with topoisomerase II to inhibit DNA replication and repair as well as RNA and protein synthesis.

GPX-100 is a n analogue of the anthracycline antineoplastic antibiotic doxorubicin. GPX-100 intercalates DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. GPX-100 was designed to be a non-cardiotoxic anthracycline antibiotic. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

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.

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.

Gamma-Glutamylcysteine is a natural dipeptide containing cysteine and glutamic acid, serving as a precursor to glutathione (GSH) and a cofactor for glutathione peroxidase (GPx). Gamma-Glutamylcysteine exhibits anti-inflammatory effects by upregulating IL-10 whilst downregulating TNF-α, IL-6, and IL-1β.

Gamma-glutamylcysteine TFA (γ-glutamylcysteine TFA) is a precursor of glutathione (GSH) with antioxidant and anti-inflammatory properties. It alleviates oxidative stress and mitochondrial damage induced by ethanol in hepatocytes by increasing cellular GSH, SOD activity, and mitochondrial membrane potential, protecting cells from alcohol-induced liver disease (ALD) by inhibiting oxidative stress, reducing inflammation, and preventing cell apoptosis.

ZX703 (compound 5I) is a GPX4-targeting PROTAC that induces efficient, dose- and time-dependent degradation of GPX4 through both ubiquitin–proteasome and autophagy–lysosome pathways, ZX703 results in reactive oxygen species accumulation, ferroptosis induction, and strong mechanistic relevance for cancer biology and ferroptosis-focused therapeutic research.

ML162-yne is an effective GPX4 inhibitor and affinity probe containing an alkyne group capable of click chemistry reactions with azide-containing molecules.

PKUMDL-LC-101-D04 is a potent allosteric activator of glutathione peroxidase 4 (GPX4), a regulator of ferroptosis. GPX4 activity was increased to 150% of control levels when used at a concentration of 20 μM in a cell-free assay, and at a concentration of 61 μM in wild-type, but not Gpx4-/-, mouse embryonic fibroblast (MEF) extracts.PKUMDL-LC-101-D04 (200 μM) reduced cholesterol peroxide-induced MEF death.

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.

BCP-T.A is an ferroptosis inducer that acts by binding to GPX4.

N6F11 is a novel, selective and potent inducer of ferroptosis with anticancer and antitumour activity that promotes GPX4 degradation by binding to TRIM25 in cancer cells.N6F11 can be used to study pancreatic cancer.

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.

Ligustroside is a natural product of phenolic glycosides from olive plants, which has antioxidant and anti-inflammatory activities. Ligustroside can up-regulate the mRNA expression of SIRT1, CREB1 and GPx1 in SH-SY5Y-APP695 cells. At the same time, the production of nitric oxide (NO) was significantly inhibited in RAW264.7 macrophages stimulated by lipopolysaccharide (LPS). Ligustroside has potential application value in cardiovascular and metabolic diseases related research.

GPX4-IN-14 (compound 2c) acts as a GPX4 inhibitor, exhibiting both free radical scavenging activity (with a maximum scavenging rate of 72.52%) and anti-tumor proliferation activity in vitro. This compound targets GPX4 protein, elevating lipid peroxide and intracellular Reactive Oxygen Species (ROS) levels, which induces ferroptosis and contributes to its anti-tumor proliferation effects.

GPX4 Activator 2 (Compound C3) serves as an activator of GPX4 and exhibits cardioprotective effects by inhibiting cellular iron death (ferroptosis) with an efficacy concentration (EC50) of 7.8 μM. It is used in the study of myocardial damage.

GPX4-IN-13 (compound 16), a GPX4 inhibitor, exhibits anticancer properties by diminishing the expression of GPX4, thereby reducing thyroid cell proliferation and inducing ferroptosis. Additionally, this compound effectively inhibits the growth of three distinct thyroid cancer cell lines: N-thy-ori-3-1 (IC 50 =8.39 μM), MDA-T32 (IC 50 =10.28 μM), and MDA-T41 (IC 50 =8.18 μM).

GPX4-IN-15 (Compound C1) is an inhibitor of GPX4, demonstrating an inhibition rate of 19.8% at a concentration of 1 μM. This compound effectively inhibits the proliferation of cancer cell lines MDA-MB-468, BT-549, and MDA-MB-231, with IC50 values of 0.86 μM, 0.96 μM, and 0.48 μM respectively.