Ferroptosis Activator

FIN56 is a specific inducer of ferroptosis. FIN56 induces ferroptosis by inducing degradation of GPX4. FIN56 also binds to and activates squalene synthase.

Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.

ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor. ML162 has a selective lethal effect on mutant RAS oncogene-expressing cell lines

L-Glutamic acid monosodium salt is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid monosodium salt has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid monosodium salt can be used in the study of neurological diseases. L-Glutamic acid monosodium salt acts at ionotropic and metabotropic glutamate receptors.

Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.

BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.

Piperlongumine is a alkaloid, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome.

(-)-Epicatechin inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.

Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC₅₀ of 5.6 μM.

BAY 11-7085 (BAY 11-7083) is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC₅₀ of 10 μM.

Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).

Atorvastatin hemicalcium salt (CI-981) is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, with blood-brain barrier permeability. Atorvastatin hemicalcium salt has the ability to effectively decrease blood lipids. Atorvastatin hemicalcium salt inhibits human SV-SMC proliferation and invasion with IC₅₀s of 0.39 μM and 2.39 μM, respectively.

FINO2 is a potent ferroptosis inducer. FINO2 inhibits GPX4 activity. FINO2 is a stable oxidant that oxidizes ferrous iron and stable at varying pH levels. FINO2 causes widespread lipid peroxidation.

Trigonelline is an alkaloid with potential antidiabetic activity that can be isolated from Trigonella foenum-graecum L or Leonurus artemisia. Trigonelline is a potent Nrf2 inhibitor that blocks Nrf2-dependent proteasome activity, thereby enhancing apoptosis in pancreatic cancer cells. Trigonelline also has anti-HSV-1, antibacterial, and antifungal activity and induces ferroptosis.

L-Cystine is an orally active extracellular form of L-Cysteine (HY-Y0337), occurring in proteins of plants and animals. L-Cystine elevates Nrf2 protein expression and activates Nrf2 transcription factor. L-cystine reduces ROS generation and protects against oxidant- or Doxorubicin (HY-15142A)-induced apoptosis. L-Cystine combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine is promising for research of cystinuria and kidney stones

Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC₅₀ of 8 nM. Fluvastatin sodium protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.

Gingerenone A is an Nrf2-Gpx4 activator that can induce Ferroptosis in liver damage with oral activity. Gingerenone A has anti-inflammatory, anti-diabetic, anti-tumor, and pro-aging effects in mice.

CDDO-Im (RTA-403) is an activator of Nrf2 and PPAR, with K_is of 232 and 344 nM for PPARα and PPARγ.

PD146176 (NSC168807), a 15-Lipoxygenase (15-LO) inhibitor, inhibits rabbit reticulocyte 15-LO (K_i=197 nM, IC₅₀=0.54 μM). PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.

DL-Buthionine-(S,R)-sulfoximine hydrochloride (Buthionine sulfoximine hydrochloride) is a potent inhibitor of glutamylcysteine synthetase biosynthesis.