Ferroptosis

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Erastin is an iron death activator that acts on the mitochondrial VDAC in a ROS- and iron-dependent manner. Erastin has anti-tumor activity and acts selectively on tumor cells with RAS-carcinogenic mutations.

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.

Liproxstatin-1 is a potent and selective inhibitor of ferroptosis (IC50=22 nM). Liproxstatin-1 protects cells from ferroptosis induced by ferroptosis inducers (e.g., Erastin, RSL3).

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Pioglitazone (U 72107) is an insulin sensitizing agent and thiazolidinedione indicated for the treatment of type 2 diabetes, and has been linked to rare instances of acute liver injury.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Acetylcysteine (NAC) is an N-acetyl derivative of cysteine, a ROS inhibitor and mucolytic agent. Acetylcysteine induces apoptosis, can be used to reduce mucus thickness, and has anti-influenza viral activity.

Cycloheximide (Naramycin A) is a natural product that reversibly inhibits translation elongation, is an antimitotic compound, and is an inhibitor of DNA and protein synthesis.

Cisplatin (CDDP) is a DNA cross-linking agent. Cisplatin has antitumor activity and inhibits DNA synthesis by forming DNA adducts in cancer cells. Cisplatin also activates ferroptosis and induces autophagy.

Deferoxamine Mesylate (DFOM) is an iron chelator and ferroptosis inhibitor. Deferoxamine Mesylate binds free iron into a stable complex and reduces iron accumulation. Deferoxamine Mesylate up-regulates HIF-1α levels and induces apoptosis.

SP600125 (JNK Inhibitor II) is a JNK inhibitor that inhibits JNK1, JNK2, and JNK3 (IC50=40 40 90 nM) with oral potency, reversibility, and ATP-competitive properties. SP600125 inhibits autophagy and induces apoptosis.

Troglitazone (Romglizone) is a PPARγ agonist with anti-inflammatory and anti-tumor activity.

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.

Imidazole ketone erastin (IKE) is an ferroptosis inducer with inhibitory effects on system Xc-cystine glutamate transporter proteins. Imidazole ketone erastin has antitumor activity and induces glutathione depletion and lipid peroxidation.

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of iron death. Ferrostatin-1 potently inhibits Erastin-induced iron death in HT-1080 cells with an EC50 of 60 nM. Ferrostatin-1 also exhibits antioxidant and antifungal activities.

Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2 10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6 20 22 nM for Raf-1 VEGFR-3 B-Raf).

Linagliptin (BI 1356) is a potent, orally bioavailable dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity.

Pioglitazone hydrochloride (AD 4833) is the hydrochloride salt of an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.

DL-Glutamine (2-amino-4-carbamoylbutanoic acid), a non-essential amino acid, exists abundantly throughout the body and is participated in many metabolic processes. It is synthesized from glutamic acid and ammonia, and is the main carrier of nitrogen in the body and is an important energy source for many cells.

L-Glutamine (L-Glutamic acid 5-amide), a non-essential amino acid, is synthesized from glutamic acid and ammonia.

Artesunate (WR-256283) is part of the artemisinin group of drugs that treat malaria. It is a semi-synthetic derivative of artemisinin that is water-soluble and may therefore be given by injection. It is on the World Health Organization's List of Essential Medicines.

Zileuton (A 64077) is a synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma.