Ferroptosis Inhibitor

Dopamine hydrochloride (ASL279) is a catecholamine neurotransmitter that is produced in the substantia nigra, ventral tegmental area, and hypothalamus of the brain. Dopamine hydrochloride (ASL279) plays several important roles in the brain and body. Dopamine hydrochloride (ASL279) acts through D2 dopamine receptors to induce endocytosis of VEGFR2, which is critical for promoting angiogenesis.

Dopamine is a catecholamine neurotransmitter that is produced in the substantia nigra, ventral tegmental area, and hypothalamus of the brain. Dopamine plays several important roles in the brain and body. Dopamine acts through D2 dopamine receptors to induce endocytosis of VEGFR2, which is critical for promoting angiogenesis.

Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.

Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with K_is of 140 and 110 nM, respectively.

Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.

Nordihydroguaiaretic acid is a 5-lipoxygenase (5LOX) (IC₅₀=8 μM) and tyrosine kinase inhibitor.

Gastrodin, a main constituent of a Chinese herbal medicine Tianma, has been known to display anti-inflammatory effects. Gastrodin inhibits ethanol-induced hepatocellular apoptosis. Gastrodin inhibits H₂O₂-induced ferroptosis through its antioxidative effect. Gastrodin can be used for study of dizziness, epilepsy, stroke and dementia.

Butylated hydroxytoluene is an antioxidant widely used in foods and in food-related products. Butylated hydroxytoluene is a Ferroptosis inhibitor.

Gamma-glutamylcysteine (γ-Glu-Cys) is an orally active, blood-brain barrier permeable dipeptide. Gamma-glutamylcysteine activates AMPK, SIRT1, IL-4/STAT6, AC/cAMP/PI3K, IGF-1R/IRS1/PI3K, and Nrf2 signaling pathways; it inhibits NF-κB, JAK1/STAT1/3, MAPKs, cadmium-induced p38 MAPK, JNK, and PI3K/Akt signaling pathways. Gamma-glutamylcysteine regulates macrophage polarization, modulates the trafficking of CD36 and GLUT4, induces glutathione synthesis, improves metabolic dysfunction, reduces lipid deposition, ameliorates glucose homeostasis, inhibits apoptosis (Apoptosis), stabilizes mitochondria, suppresses lipid peroxidation, iron accumulation and ferroptosis (Ferroptosis), reduces ds-HMGB1 levels, reverses mechanical hyperalgesia, and alleviates hepatic lipid droplet formation. Gamma-glutamylcysteine is applicable to research related to inflammatory bowel disease, type 2 diabetes, cadmium-induced neurotoxicity, Alzheimer's disease, cerebral ischemia/reperfusion injury, neuropathy, and alcoholic liver disease.

Dexrazoxane, as an intracellular iron chelating agent, reduces the formation of superoxide radicals and has cardioprotective, anti-inflammatory, antioxidant, anti-tumor and neuroprotective activities. Dexrazoxane inhibits ferroptosis of H9c2 cells by inhibiting HMGB1. Dexrazoxane induces DNA damage and apoptosis in human fibrosarcoma cells .

Linagliptin is a highly potent, selective DPP-4 inhibitor with IC₅₀ of 1 nM.

Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC₅₀s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.

Pipecolic acid is an orally bioavailable, blood-brain barrier-permeable metabolite of lysine with antioxidant, inhibitor, and inducer activity. Pipecolic acid modulates the YAP-GPX4 signaling pathway, reduces retinal vascular tube formation, and mitigates ferroptosis. Pipecolic acid potentiates voltage-sensitive Ca²⁺ channel currents and induces neuronal apoptosis. Pipecolic acid can be used for the research of diabetic retinopathy.

Taurolithocholic acid sodium salt is an orally active bile acid and antiviral agent. Taurolithocholic acid sodium salt upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid sodium salt also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid sodium salt serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid sodium salt shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid sodium salt not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis.

DL-alpha-Tocopherol is a synthetic vitamin E, with antioxidation effect. DL-alpha-Tocopherol protects human skin fibroblasts against the cytotoxic effect of UVB.

Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a K_d of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).

EPI-743 (Vatiquinone; α-Tocotrienol quinone; PTC-743; NCT04378075) is a potent cellular oxidative stress protectant, inhibits ferroptosis in cells, which could be used for the study for mitochondrial diseases. EPI-743 is a synthetic analog of vitamin E with oral activity, targets repletion of reduced intracellular glutathione.

Ciclopirox (HOE296b) is a synthetic and orally active antifungal agent that can be used for superficial mycoses reseaech. Ciclopirox olamine has a very broad spectrum of activity and inhibits dermatophytes, yeasts, molds, and many Gram-positive and Gram-negative species pathogenic. Ciclopirox also has anticancer and anti-inflammatory effect.

Eugenol is an essential oil found in cloves with antibacterial, anthelmintic and antioxidant activity. Eugenol is shown to inhibit lipid peroxidation.

Trans-3-Indoleacrylic acid is a tryptophan metabolite, which promotes tumor development through inhibition of RSL3 (HY-100218A) induced ferroptosis via AHR-ALDH1A3-FSP1-CoQ10 axis, and facilitates colorectal carcinogenesis