gpx4

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.

FIN56, a specific inducer of ferroptosis, is identified by its IUPAC name [1,3,8-trihydroxy-6-methylanthracen-9(10H)-one].

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.

PROTAC GPX4 degrader-3 is a potent GPX4-targeting PROTAC degrader, exhibiting a DC50 of 0.019 μM (24 h) and an IC50 of 0.024 μM in HT1080 cells.

GPX4-IN-4 (Compound 24) is a potent inhibitor of GPX4, employed in cancer research [1].

GPX4-IN-16 ((R)-9i) is a potent inhibitor of GPX4 with a KD value of 20.4 nM, exhibiting cytotoxic properties and anticancer activity.

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-IN-7 (Compound 31), an indirubin derivative, serves as a ferroptosis inducer in colon cancer treatment. Exhibiting potent antitumor properties, it inhibits HCT-116 cell growth with an IC50 of 0.49 μM. This compound also facilitates GPX4 degradation, leading to lipid ROS accumulation, thereby inducing ferroptosis [1].

GPX4-IN-10 (compound I20) is a non-covalent inhibitor of GPX4. It induces ferroptosis and inhibits the growth of HT1080 cells.

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.

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

PROTAC GPX4 Degrader-1 (DC-2) is a PROTAC-based compound that efficiently degrades GPX4, demonstrating a degradation concentration (DC 50) of 0.03 μM in HT1080 cells [1].

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 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-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).

GPX4-IN-11 (compound I14) serves as an effective inhibitor of GPX4, exhibiting a dissociation constant (KD) of 45.7 μM. This compound plays a crucial role in the study of ferroptosis (ferroptosis).

GPX4 24, a derivative of (1S,3R)-RSL3, acts as a potent inhibitor of glutathione peroxidase 4 (GPX4) through covalent binding in a concentration-dependent manner within 4T1 murine mammary carcinoma cells. This compound effectively induces ferroptosis in GPX4-dependent HT-1080 fibrosarcoma cells with an EC50 value of 0.16 µM. Additionally, at a dose of 200 mg/kg, GPX4 24 elevates malondialdehyde (MDA) levels in both kidney and plasma of mice, highlighting its impact on lipid peroxidation.

GPX4-IN-2 is a potent inhibitor of GPX4, exhibiting antiproliferative activity and holding potential for cancer research applications.

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 activator 1 (Compound A9) is a GPX4 allosteric activator (Kd= 5.86 μM, EC50= 19.19 μM) that selectively targets ferroptosis, preventing the accumulation of intracellular lipid peroxides induced by ferroptosis inducers.

GPX4-IN-12 (compound I22) is a non-covalent inhibitor of GPX4. It induces ferroptosis and inhibits the growth of HT1080 cells.

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.

FINO2 is a potent ferroptosis-inducing compound that inhibits GPX4 activity. It functions as a stable oxidant, effectively oxidizing ferrous iron and demonstrating stability across varying pH levels. Furthermore, FINO2 induces widespread lipid peroxidation.

iFSP1, a potent, selective, and glutathione-independent ferroptosis suppressor protein 1 (FSP1) (AIFM2) inhibitor with an EC50 of 103 nM, sensitizes diverse human cancer cell lines to ferroptosis inducers like (1S,3R)-RSL3. It uniquely triggers ferroptosis in GPX4-knockout cells overexpressing FSP1.