Imidazole ketone erastin

SKU: orb1689877

Description

Imidazole ketone erastin (IKE) is a small molecule ferroptosis inducer that inhibits the system Xc- transporter, leading to cystine deprivation, glutathione depletion, and lethal lipid peroxidation. It is widely used in vitro and in vivo to investigate ferroptosis mechanisms and evaluate antitumor strategies in cancer research.

Research Area

Cell Biology

Key Properties

• CAS Number: 1801530-11-9
• MW: 655.14
• Purity: 99.87%
• Formula: C₃₅H₃₅ClN₆O₅
• SMILES: CC(C)Oc1ccc(cc1-n1c(CN2CCN(CC2)C(=O)COc2ccc(Cl)cc2)nc2ccccc2c1=O)C(=O)Cn1ccnc1
• Target: Ferroptosis
• Solubility: DMSO:100 mg/mL (152.64 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.11 mM)

Bioactivity

• Target IC50:
  DLBCL cells:100 nM-10 μM|DLBCL cells:> 10 μM|system xc:30 nM
• In Vivo:
  METHODS: To detect anti-tumor activity in vivo, Imidazole ketone erastin (23-40 mg/kg, 5% DMSO in HBSS at pH 4) was injected intraperitoneally into NCG mice harboring human diffuse histiocytic lymphoma SUDHL6 once daily for thirteen days. RESULTS: Imidazole ketone erastin inhibited tumor growth in vivo. METHODS: To test the antitumor activity in vivo, Imidazole ketone erastin (40 mg/kg every two days) and liproxstatin-1 (10 mg/kg once a day) were intraperitoneally injected into C57BL/6 mice with the hepatocellular carcinoma tumor Hepa1-6 for ten days on either a control (Met+) or a methionine-free (Met-) diet. Met-) diet. RESULTS: In mice receiving the control diet, Imidazole ketone erastin treatment effectively reduced tumor growth, and this effect was completely blocked by liproxtatin-1. However, in mice receiving a methionine-free diet, Imidazole ketone erastin treatment failed to inhibit tumor growth.
• In Vitro:
  METHODS: Human astrocytoma cells CCF-STTG1 were incubated with Imidazole ketone erastin for 2 h. Glutamate released into the medium was detected using glutamate oxidase, horseradish peroxidase, and Amplex UltraRed fluorimetric assay. RESULTS: The IC50 for system xc- inhibition by Imidazole ketone erastin was 30 nM. METHODS: 18 DLBCL cell lines were treated with Imidazole ketone erastin (0.0001-100 µM) for 24 h. Cell viability was measured using the Cell Titor-Glo luminescent cell viability test. RESULTS: DLBCL cell lines showed different sensitivities to Imidazole ketone erastin inhibition. 7 cell lines with IC50 <100 nM were categorized as sensitive; 5 cell lines with IC50 >10 µM were categorized as resistant; and 6 cell lines with IC50 between 100 nM and 10 µM were categorized as moderately resistant.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ferroptosis, IKE, Imidazole ketone erastin

Compound Identifiers

PubChem CID

91824786