Imidazole Ketone Erastin
(Synonyms: IKE) 目录号 : GC52190
Imidazole Ketone Erastin是一种有效的、代谢稳定的系统xc- 抑制剂和铁凋亡诱导剂。
Cas No.:1801530-11-9
Sample solution is provided at 25 µL, 10mM.
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Imidazole Ketone Erastin is an effective and metabolically stable system xc- inhibitor and ferroptosis inducer. Ferroptosis is a regulated form of cell death that can be induced by inhibiting the cystine-glutamate antiporter system xc- [1].
In vitro, Imidazole Ketone Erastin (0.1 nM-100 µM; 24 h) effectively reduces the number of DLBCL cells by inducing lipid peroxidation and ferroptosis, with 18 DLBCL cell lines displaying varying sensitivities to the inhibition by Imidazole Ketone Erastin [1]. Imidazole Ketone Erastin (1-250 nM; 24 h) depletes reduced glutathione in a dose-dependent manner, with an IC50 of 34 nM in SUDHL 6 cells, and also increases lipid ROS [1].
In vivo, Imidazole Ketone Erastin (23, 40 mg/kg/d; i.p.) inhibits tumor growth in a mouse model of diffuse large B cell lymphoma, leading to a significant reduction in tumor growth and body weight loss starting from day 9 [1]. Imidazole Ketone Erastin (40 mg/kg; i.p.) administered every other day for 22 days to mice with a model of chronic arthritis significantly alleviates symptoms of synovitis and promotes the rapid resolution of inflammation [2].
References:
[1]Zhang, Y., Tan, H., Daniels, J.D., et al. Imidazole ketone erastin induces ferroptosis and slows tumor growth in a mouse lymphoma model. Cell Chem. Biol. 26(5), 623-633 (2019).
[2] TNF antagonist sensitizes synovial fibroblasts to ferroptotic cell death in collagen-induced arthritis mouse models[J]. Nature Communications[2024-03-08].
Imidazole Ketone Erastin是一种有效的、代谢稳定的系统xc- 抑制剂和铁凋亡诱导剂。铁凋亡是一种受调节的细胞死亡形式,其可通过抑制胱氨酸-谷氨酸反向转运蛋白系统xc- 而诱导[1]。
在体外,Imidazole Ketone Erastin (0.1 nM-100 µM; 24 h) 通过诱导脂质过氧化和铁凋亡可以有效减少DLBCL细胞数量,18种DLBCL细胞系均显示出对Imidazole Ketone Erastin抑制的不同敏感性[1]。Imidazole Ketone Erastin(1-250 nM; 24 h)以剂量依赖性方式消耗还原型谷胱甘肽,在SUDHL 6细胞中IC50 为34 nM,还增加脂质ROS[1]。
在体内,Imidazole Ketone Erastin (23, 40 mg/kg/d; i.p.) 抑制弥漫性大 B 细胞淋巴瘤小鼠模型中的肿瘤生长,从第9天开始导致肿瘤生长和体重减轻显着减少[1]。Imidazole Ketone Erastin(40 mg/kg; i.p.)每两天一次对慢性关节炎模型小鼠进行治疗,持续22天,显著减轻了滑膜炎症状,促进了炎症的迅速消退[2]。
| Cell experiment [1]: | |
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Cell lines |
DLBCL cells |
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Preparation Method |
DLBCL cells were plated at 10,000 cells per well in white 384-well plates in technical duplicates and incubated overnight. The cells were then treated with 8 µL medium containing a two-fold dilution series of vehicle , Imidazole Ketone Erastin (0.1 nM-100 µM ) with or without Fer-1. After 24 h incubation, 40 µL of 50% Cell Titer-Glo 50% cell culture medium was added to each well and incubated at room temperature with shaking for 15 min. |
|
Reaction Conditions |
0.1 nM-100 µM; 24 h |
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Applications |
Imidazole ketone erastin (0.1nM-100µM;24h) potently reduces DLBCL cell number by lipid peroxidation and ferroptosis. |
| Animal experiment [2]: | |
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Animal models |
Male NCG mice |
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Preparation Method |
NCG mice, 6-weeks old, were injected with 10 million SUDHL0-6 cells subcutaneously. The mice were treated after the tumor size reached 100 mm3. Mice were separated randomly into treatment groups and dosed with 23 mg/kg Imidazole Ketone Erastin , 40 mg/kg Imidazole Ketone Erastin , 23 mg/kg Imidazole Ketone Erastin PEG-PLGA nanoparticles , vehicle 1, and vehicle 2 once daily by IP for 14 days. |
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Dosage form |
23, 40 mg/kg/d ; 14 days ; i.p. |
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Applications |
Imidazole Ketone Erastin inhibited tumor growth in a diffuse large B cell lymphoma mouse model, caused a significant decrease in tumor growth and weight loss starting from day 9. |
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References: [1] Zhang, Y., Tan, H., Daniels, J.D., et al. Imidazole ketone erastin induces ferroptosis and slows tumor growth in a mouse lymphoma model. Cell Chem. Biol. 26(5), 623-633 (2019). |
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| Cas No. | 1801530-11-9 | SDF | Download SDF |
| 别名 | IKE | ||
| Canonical SMILES | O=C1N(C2=CC(C(CN3C=NC=C3)=O)=CC=C2OC(C)C)C(CN4CCN(C(COC5=CC=C(Cl)C=C5)=O)CC4)=NC6=CC=CC=C61 | ||
| 分子式 | C35H35ClN6O5 | 分子量 | 655.1 |
| 溶解度 | DMF: 10mg/mL; DMSO: 100mg/mL; DMSO:PBS (pH 7.2) (1:2): 0.25mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5265 mL | 7.6324 mL | 15.2648 mL |
| 5 mM | 0.3053 mL | 1.5265 mL | 3.053 mL |
| 10 mM | 0.1526 mL | 0.7632 mL | 1.5265 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet