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CAS No.: 1801530-11-9

IKE (Imidazole ketone erastin )/咪唑酮伊拉斯汀（PUN30119） Catalog No. CSN24168

Synonyms: PUN30119;IKE;Imidazole ketone erastin

IKE is a potent, metabolically stable inhibitor of system X_c^- and inducer of ferroptosis potentially suitable for in vivo applications.

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400-920-2911

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实验方案

技术信息

生物活性

描述Ferroptosis is a form of regulated cell death that can be induced by inhibition of the cystine-glutamate antiporter, system x_c_-. Among the existing system x_c_- inhibitors, imidazole ketone erastin (IKE) is a potent, metabolically stable inhibitor of system x_c_- and inducer of ferroptosis potentially suitable for in vivo applications^[1]. The IC₅₀ of GSH depletion by IKE was 34 nM in SUDHL6 cells. Analysis of lipid reactive oxygen species (ROS) by flow cytometry using the lipid peroxidation probe C11-BODIPY revealed a dose-dependent increase in lipid ROS upon IKE treatment in SUDHL6 cells. Immunofluorescence staining with an anti-dihydropyridine-MDA-lysine adduct antibody (mAb 1F83) revealed that dihydropyridine-MDA-lysine adduct abundance was increased upon IKE treatment^[1]. The system x_c_- component SLC7A11, prostaglandin-endoperoxide synthase 2 (PTGS2, which encodes cyclooxygenase-2), and ChaC GSH-specific γ-glutamylcyclotransferase 1 (CHAC1) expression was significantly increased in SUDHL6 cells following IKE treatment^[1]. IKE exhibits antitumor activity in DLBCL (diffuse large B cell lymphoma) xenograft model, which correlates with an increase of lipid peroxidation in tumors. These findings suggest that IKE can be effective as a potential therapeutic regimen for DLBCL^[1].
动物研究
剂量
Mice: 23 mg/kg, 40 mg/kg, 50 mg/kg^[1] (i.p., p.o.); 17 mg/kg^[1] (i.v.)

给药途径
i.p., p.o., i.v.
参考文献

动物研究
剂量	Mice: 23 mg/kg, 40 mg/kg, 50 mg/kg^[1] (i.p., p.o.); 17 mg/kg^[1] (i.v.)
给药途径	i.p., p.o., i.v.

[1] Zhang Y, Tan H, Daniels JD, Zandkarimi F, Liu H, Brown LM, Uchida K, O'Connor OA, Stockwell BR. 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. doi: 10.1016/j.chembiol.2019.01.008. Epub 2019 Feb 21. PMID: 30799221; PMCID: PMC6525071.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5264 mL
- 7.6319 mL
- 15.2639 mL
- 5 mM
- 0.3053 mL
- 1.5264 mL
- 3.0528 mL
- 10 mM
- 0.1526 mL
- 0.7632 mL
- 1.5264 mL

技术信息

CAS号

1801530-11-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C35H35ClN6O5

运输

蓝冰

分子量

655.14

别名

PUN30119;IKE;Imidazole ketone erastin

溶解度

DMSO	11.0 mg/mL (16.8 mM)
Water	insoluble

动物实验配方

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IKE (Imidazole ketone erastin )/咪唑酮伊拉斯汀（PUN30119） Catalog No. CSN24168

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