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Imidazole ketone erastin

Catalog No. T5523   CAS 1801530-11-9
Synonyms: IKE

Imidazole ketone erastin (IKE) (IKE) is an inducer of ferroptosis. It has inhibition of the system Xc- cystine/glutamate transporter.

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Imidazole ketone erastin Chemical Structure
Imidazole ketone erastin, CAS 1801530-11-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 80.00
2 mg In stock $ 115.00
5 mg In stock $ 212.00
10 mg In stock $ 297.00
25 mg In stock $ 497.00
50 mg In stock $ 723.00
100 mg In stock $ 987.00
500 mg In stock $ 1,980.00
1 mL * 10 mM (in DMSO) In stock $ 192.00
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Purity: 99.87%
Purity: 99.02%
Purity: 98.98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Imidazole ketone erastin (IKE) (IKE) is an inducer of ferroptosis. It has inhibition of the system Xc- cystine/glutamate transporter.
In vitro Human astrocytoma cells (CCF-STTG1) were used, which contain the system xc?.17 Following a 2 h incubation period, glutamate released into the medium was detected fluorometrically using glutamate oxidase, horseradish peroxidase, and Amplex UltraRed. Dramatic improvement of the half-maximal inhibitory constants (IC50) for system xc? inhibition was observed for IKE (IC50: 30 nM), compared to erastin and PE [1].
In vivo In a diffuse large B cell lymphoma (DLBCL) xenograft model, IKE exerted an antitumor effect by inhibiting system xc-, leading to glutathione depletion, lipid peroxidation, and the induction of ferroptosis biomarkers [2].
Synonyms IKE
Molecular Weight 655.14
Formula C35H35ClN6O5
CAS No. 1801530-11-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (152.64 mM)

TargetMolReferences and Literature

1. Larraufie MH, et al. Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4787-4792. 2. Zhang Y, et al. Imidazole Ketone Erastin Induces Ferroptosis and Slows Tumor Growth in a Mouse Lymphoma Model. Cell Chem Biol. 2019 May 16;26(5):623-633.e9.

TargetMolCitations

1. Liu D, Liang C, Huang B, et al.Tryptophan Metabolism Acts as a New Anti‐Ferroptotic Pathway to Mediate Tumor Growth.Advanced Science.2023: 2204006. 2. Bi G, Liang J, Shan G, et al.Retinol saturase mediates retinoid metabolism to impair a ferroptosis defense system in cancer cells.Cancer Research.2023: CAN-22-3977. 3. Besskaya V, Zhang H, Bian Y, et al.Hepatic nuclear factor 4 alpha promotes the ferroptosis of lung adenocarcinoma via transcriptional activation of cytochrome P450 oxidoreductase.PeerJ.2023, 11: e15377. 4. Yan R, Xie E, Li Y, et al. The structure of erastin-bound xCT–4F2hc complex reveals molecular mechanisms underlying erastin-induced ferroptosis. Cell Research. 2022-32(7)P1-4 5. Shan G, Bi G, Zhao G, et al.Inhibition of PKA/CREB1 pathway confers sensitivity to ferroptosis in non-small cell lung cancer.Respiratory Research.2023, 24(1): 1-15.

Related compound libraries

This product is contained In the following compound libraries:
Apoptosis Compound Library Inhibitor Library NO PAINS Compound Library Bioactive Compounds Library Max Cell Cycle Compound Library Ferroptosis Compound Library Bioactive Compound Library

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Keywords

Imidazole ketone erastin 1801530-11-9 Apoptosis Ferroptosis IKE inhibitor inhibit

 

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