erastin-2

Erastin2 is a ferroptosis inducer and inhibitor of the system xc- cystine glutamate transporter.[1][2] It inhibits glutamate release in CCF-STTG1 cells (IC50 = 0.0035 µM) and induces cell death in HAP1 cells at 5 µM, an effect blocked by ferrostatin-1 or deferoxamine.[1][2] Erastin2 also induces ferroptotic cell death in HT-1080 cells (EC50 = 0.15 µM), an effect blocked by β-mercaptoethanol (EC50 > 20 µM).[3] Additionally, it increases lipid peroxidation in HT-1080 cells at 1 µM.

SLC7A11-IN-2 (Compound 1) is an inhibitor of SLC7A11 xCT. It disrupts the oxidative balance in HeLa cells by decreasing intracellular glutathione levels and increasing oxidative stress, thereby inducing cell death with an IC50 of 10.23 μM. Molecular dynamics simulations have demonstrated that SLC7A11-IN-2 exhibits a stronger binding affinity to SLC7A11 compared to Erastin. This compound is useful for research in the field of cervical cancer.

Pantothenate Kinase Inhibitor (PANKi) is a reversible inhibitor of pantothenate kinase (PanK; IC50s = 70, 92, and 25 nM for PanK1β, PanK2, and PanK3, respectively), the rate-limiting enzyme in the synthesis of coenzyme A .1It binds to the ATP-PanK3 complex with an apparent binding constant of 300 nM and exhibits mixed-type inhibition with respect to ATP and pantothenate. PANKi inhibits CoA biosynthesis in C3A cells (IC50= 0.9 μM) with no effect on cell viability when used at concentrations up to 8 μM. PANKi (5 μM) synergizes with BSO to induce ferroptosis in PANC-1 cells and sensitizes the cells to imidazole ketone erastin-induced ferroptosis.2 1.Sharma, L.K., Leonardi, R., Lin, W., et al.A high-throughput screen reveals new small-molecule activators and inhibitors of pantothenate kinasesJ. Med. Chem.58(3)1563-1568(2015) 2.Badgley, M.A., Kremer, D.M., Maurer, H.C., et al.Cysteine depletion induces pancreatic tumor ferroptosis in miceScience368(6486)85-89(2020)