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Imidazole Ketone Erastin (IKE) is an inducer for ferroptosis iron death. It is also a potent, selective, and metabolically stable system XC -- inhibitor. IKE is more water-soluble than Erastin. Inducing iron death in diffuse large B-cell lymphoma cells (e.g. Sudhl-5/6/16).
| Cell Experiment | |
|---|---|
| Cell lines | DLBCL cell line |
| Preparation method | DLBCL cells are plated at 10,000 cells per well in white 384-well plates (32 μL per well) in technical duplicates and incubated overnight. The cells are then treated with 8 μL medium containing a two-fold dilution series of vehicle (DMSO), IKE (starting from 100 μM) with or without Fer-1 (starting from 200 μM). After 24 h incubation, 40 μL of 50% CellTiter-Glo / 50% cell culture medium is added to each well and incubated at room temperature with shaking for 15 min. Luminescence is measured. All cell viability data are normalized to the DMSO vehicle condition. Experiments are performed three independent times with different passages for each cell line. From these data, dose-response curves and IC50 values are computed. |
| Concentrations | 0-100 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Non-obese diabetic/ severe combined immunodeficiency (NOD/SCID) mice |
| Formulation | dissolved in 5% DMSO/95% HBSS at pH 4 solution |
| Dosages | 50 mg/kg, 17 mg/kg |
| Administration | IP and PO and IV |
| Molecular Weight | 655.14 |
| Formula | C35H35ClN6O5 |
| CAS Number | 1801530-11-9 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Ferroptosis Products |
|---|
| Deferiprone
Deferiprone is the only orally active iron-chelating agent with an affinity for ferric ion (iron III)，binds with ferric ions to form neutral 3:1 (deferiprone:iron) complexes that are stable over a wide range of pH values. |
| Erastin
Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. *The compound is unstable in solutions, it must be prepared freshly and used immediately. |
| Ferrostatin-1
Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM. |
| Lithocholic acid
Lithocholic acid is a bile acid that acts as a detergent to solubilize fats for absorption, can also activate the vitamin D receptor. |
| Idebenone
Idebenone, a mitochondrial protector, has neuroprotective properties and can be used to study Alzheimer's disease, Huntington's disease, and can cross the blood-brain barrier. Idebenone (oxidized form) inhibited arachidonic acid enzyme metabolism in astrocyte homogenates (IC50=16.65 μM). Idebenone is a coenzyme Q10 analogue and antioxidant that induces apoptosis (apoptotic) in human dopaminergic neuroblastoma SHSY-5Y cells. |
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