Erastin2
(Synonyms: 35MEW28) 目录号 : GC43623
Erastin2 是一种有效的系统 xc 抑制剂和铁死亡诱导剂。
Cas No.:1695533-44-8
Sample solution is provided at 25 µL, 10mM.
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Erastin2 is a potent system xc- inhibitor and ferroptosis-inducing agent [1].
Erastin2 (5µM, 24h) significantly inhibited the activity of human HAP1 haploid cells, and that erastin2-induced cell death was inhibited by co-treatment with the lipophilic radical-trapping antioxidant ferrostatin-1 or the iron chelator deferoxamine (DFO), but not the pan-caspase inhibitor Q-VD-OPh [1]. Erastin2 induced ferroptosis in HT-1080(1 µM), T98G glioblastoma (1 µM), and A549 non-small-cell lung carcinoma cells (2 µM), and non-transformed IMR-90 diploid fibroblasts (125nM) [2]. Erastin2 (1 µM) inhibited system xc- function, depleted total glutathione (GSH + GSSG), and upregulated CHAC1 expression [2]. Erastin2 (1-10µM) increased FSP1KO cells sensitivity [3]. In the context of erastin2-induced ferroptosis, the onset of cell death correlates with the oxidation of the lipid peroxide-sensitive probe C11 BODIPY 581/591 (C11) (Cat.No. GC40165) specifically at the plasma membrane, linking the onset of cell death to a key terminal marker of the ferroptotic process [1].
References:
[1]. Cao JY, Poddar A, Magtanong L, Lumb JH, Mileur TR, Reid MA, Dovey CM, Wang J, Locasale JW, Stone E, Cole SP. A genome-wide haploid genetic screen identifies regulators of glutathione abundance and ferroptosis sensitivity. Cell reports. 2019 Feb 5;26(6):1544-56.
[2]. Magtanong L, Ko PJ, To M, Cao JY, Forcina GC, Tarangelo A, Ward CC, Cho K, Patti GJ, Nomura DK, Olzmann JA. Exogenous monounsaturated fatty acids promote a ferroptosis-resistant cell state. Cell chemical biology. 2019 Mar 21;26(3):420-32.
[3]. Bersuker K, Hendricks JM, Li Z, Magtanong L, Ford B, Tang PH, Roberts MA, Tong B, Maimone TJ, Zoncu R, Bassik MC. The CoQ oxidoreductase FSP1 acts parallel to GPX4 to inhibit ferroptosis. Nature. 2019 Nov 28;575(7784):688-92.
Erastin2 是一种有效的系统 xc 抑制剂和铁死亡诱导剂[1]。
Erastin2 (5µM, 24h) 显着抑制人 HAP1 单倍体的活性细胞，并且 erastin2 诱导的细胞死亡被亲脂性自由基捕获抗氧化剂 ferrostatin-1 或铁螯合剂去铁胺 (DFO) 共同治疗抑制，但泛半胱天冬酶抑制剂 Q-VD-OPh [ 1]。 Erastin2 在 HT-1080（1 77777#181；M）、T98G 胶质母细胞瘤（1 77777#181；M）和 A549 非小细胞肺癌细胞（2 77777#8181；M）和未转化的 IMR-90 二倍体成纤维细胞（ 125nM）[2]。 Erastin2 (1 µM) 抑制系统 xc- 功能，耗尽总谷胱甘肽 (GSH + GSSG)，并上调 CHAC1 表达 [2]。 Erastin2 (1-10µM) 增加 FSP1KO 细胞敏感性 [3]。在 erastin2 诱导的铁死亡的背景下，细胞死亡的发生与脂质过氧化物敏感探针 C11 BODIPY 581/591 (C11)（货号 GC40165）的氧化相关，特别是在质膜上，与细胞死亡是铁死亡过程的关键终末标志物[1]。
| Cell experiment [1]: | |
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Cell lines |
Caki-1 cells |
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Preparation Method |
Caki-1 cells were seeded in a 96-well dish at 4000 (cells treated with control shRNA constructs and nutlin-3) or 2000 (all other treatments) cells/well and infected with lentiviruses carrying non-targeting shRNAs (sh-NT) or shRNAs targeting CDKN1A at an M.O.I. of ~1 in media containing 8 µg/mL Polybrene (source). Infected cells were then spun at 1000 rpm for 1 h at room temperature. The next day, virus-containing medium was removed, and cells were incubated in medium containing puromycin (10 µg/mL) and DMSO or nutlin-3 (10 µM) for a further 24 h. Media was then removed and replaced with media containing SYTOX Green (0.022 µM), DMSO or nutlin-3 (10 µM), and DMSO or erastin2 (1 µM), and cell death was assayed for the subsequent 48 h using time-lapse imaging. Cell death was assessed by counting SYTOX Green positive cells over time. |
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Reaction Conditions |
1 µM, for 48 h |
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Applications |
Short hairpin RNA (shRNA)-mediated silencing of CDKN1A in Caki-1 cells likewise abrogated the ability of nutlin-3 pretreatment to delay subsequent erastin2-induced cell death. |
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References: [1]: Dixon SJ, Patel DN, Welsch M, Skouta R, Lee ED, Hayano M, Thomas AG, Gleason CE, Tatonetti NP, Slusher BS, Stockwell BR. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis. elife. 2014 May 20;3:e02523. |
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| Cas No. | 1695533-44-8 | SDF | |
| 别名 | 35MEW28 | ||
| 化学名 | 2-[[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]methyl]-3-[4-(1-methylethoxy)[1,1'-biphenyl]-3-yl]-4(3H)-quinazolinone | ||
| Canonical SMILES | O=C1N(C2=CC(C3=CC=CC=C3)=CC=C2OC(C)C)C(CN4CCN(C(COC5=CC=C(Cl)C=C5)=O)CC4)=NC6=CC=CC=C61 | ||
| 分子式 | C36H35ClN4O4 | 分子量 | 623.1 |
| 溶解度 | 1mg/mL in DMSO, 10mg/mL in DMF | 储存条件 | Store at -20°C,Cprotect from light |
| 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 | 1.6049 mL | 8.0244 mL | 16.0488 mL |
| 5 mM | 0.321 mL | 1.6049 mL | 3.2098 mL |
| 10 mM | 0.1605 mL | 0.8024 mL | 1.6049 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