IE0310 Erastin 抑制剂/拮抗剂/激动剂 索莱宝

In Vitro

Cell（HepG2 and HepG2.2.15 cells，diluted to a concentration of 20 mmol/L in dimethyl sulfoxide (DMSO)）

Sorafenib (IS0220, Solarbio, Beijing, China), ferrostatin-1, and erastin (IE0310, Solarbio, Beijing, China) were diluted to a concentration of 20 mmol/L in dimethyl sulfoxide (DMSO). Sorafenib was added to the culture media either directly or after plasmid transfection in serial dilutions or at the given concentrations. The CCK-8 assay was used to determine the IC50 of the cells after they had been grown for 1–3 days. The cells were grown for 24 h before being evaluated for other markers.

来源文献：Liu L, Lv Z, Wang M, Zhang D, Liu D, Zhu F. HBV Enhances Sorafenib Resistance in Hepatocellular Carcinoma by Reducing Ferroptosis via SRSF2-Mediated Abnormal PCLAF Splicing. Int J Mol Sci. 2023 Feb 7;24(4):3263. doi: 10.3390/ijms24043263. PMID: 36834680; PMCID: PMC9967099.

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标题:Circ_0000190 sponges miR-382-5p to suppress cell proliferation and motility and promote cell death by targeting ZNRF3 in gastric cancer

成员:Jiang Man, Mo Rui, Liu Chang, Wu Haijian

论文因子:3.241 发表期刊:JOURNAL OF BIOCHEMISTRY pmid:35037032

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标题:ALKBH5 inhibits thyroid cancer progression by promoting ferroptosis through TIAM1–Nrf2/HO-1 axis

成员:Li Wei, Huang Guo, Wei Jinrong, Cao Hong, Jiang Guoqin

论文因子:3.842 发表期刊:MOLECULAR AND CELLULAR BIOCHEMISTRY pmid:36070054

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标题:CircRNA-ST6GALNAC6 increases the sensitivity of bladder cancer cells to erastin-induced ferroptosis by regulating the HSPB1/P38 axis

成员:Wang Li, Wu Shuiqing, He Haiqing, Ai Kai, Xu Ran, Zhang Lei, Zhu Xuan

论文因子:5.502 发表期刊:LABORATORY INVESTIGATION pmid:35945269

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标题:HBV Enhances Sorafenib Resistance in Hepatocellular Carcinoma by Reducing Ferroptosis via SRSF2-Mediated Abnormal PCLAF Splicing

成员:Lijuan Liu, Zhao Lv, Miao Wang, Dongyan Zhang, Dongying Liu, Fan Zhu

论文因子:5.6 发表期刊:INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES pmid:36834680

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标题:Ubiquitin-specific peptidase 10 attenuates the ferroptosis to promote thyroid cancer malignancy by facilitating GPX4 via elevating SIRT6

成员:Feng Lian, Dandan Dong, Jiaxi Pu, Guanghua Yang, Jing Yang, Shaofei Yang, Yijie Wang, Bin Zhao, Minhao Lu

论文因子:4.5 发表期刊:ENVIRONMENTAL TOXICOLOGY pmid:37860888

基本信息
CAS	No.571203-78-6
英文名称	Erastin
分子式	C30H31ClN4O4
分子量	547.04
溶解性	Soluble in DMSO ≥10mg/mL;Soluble in Water ＜1mg/mL(该产品在溶液状态不稳定，建议您现用现配)
纯度	≥98%
外观(性状)	White to off-white Solid
储存条件	Powder:2-8℃，2 years
MDL	MFCD09837984
SMILES	O=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5
InChIKey	BKQFRNYHFIQEKN-UHFFFAOYSA-N
InChI	InChI=1S/C30H31ClN4O4/c1-3-38-27-11-7-6-10-26(27)35-29(32-25-9-5-4-8-24(25)30(35)37)21(2)33-16-18-34(19-17-33)28(36)20-39-23-14-12-22(31)13-15-23/h4-15,21H,3,16-20H2,1-2H3
PubChem CID	11214940
靶点	Ferroptosis
通路	Apoptosis
背景说明	Erastin是铁诱导的细胞死亡 (ferroptosis) 激活剂。
生物活性	Erastin是Ferroptosis激活剂[1-3]。
In Vitro	Erastin引发氧化，铁依赖性细胞死亡。用RSL分子erastin(10μM)处理NRAS突变体HT-1080纤维肉瘤细胞导致细胞溶质和脂质ROS在2小时开始时间依赖性增加[1]。由erastin引发的细胞死亡被抗氧化剂(例如α-生育酚，丁基化羟基甲苯和β-胡萝卜素)和铁螯合剂(例如去铁胺)显著抑制，表明莫斯汀诱导的铁蛋白沉积症需要ROS-和铁依赖性信号传导。 。 Erastin可直接与BJeLR细胞中的VDAC2/3结合。 VDAC2和VDAC3的击倒，而不是VDAC1，导致耐擦伤性。 Erastin具有通过直接抑制胱氨酸/谷氨酸逆向转运系统Xc活性来降低谷胱甘肽水平的能力，同时激活ER应激反应[2]。 Erastin有效抑制HT-29细胞存活。 Erastin显示出剂量依赖性效应，30μM的erastin表现出最显著的效果[3]。
细胞实验	在良好耐受的剂量下腹膜内注射erastin可显著抑制严重联合免疫缺陷小鼠的HT-29异种移植物生长[3]。
细胞实验	为了测试erastin对结肠直肠癌细胞存活的活性，用增加浓度的erastin(0.1-30μM)处理HT-29细胞。进行MTT测定[3]。
动物实验	小鼠：每天用10或30mg/kg体重的erastin(腹膜内注射，持续4周)或载体对照(盐水)处理小鼠。计算肿瘤体积。每周还记录小鼠体重[3]。
数据来源文献	[1]. Dixon SJ， et al. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012 May 25;149(5):1060-72. [2]. Xie Y， et al. Ferroptosis: process and function. Cell Death Differ. 2016 Mar;23(3):369-79. [3]. Huo H， et al. Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells. PLoS One. 2016 May 12;11(5):e0154605.
单位	瓶