1. Apoptosis Membrane Transporter/Ion Channel
  2. Ferroptosis VDAC
  3. Erastin

Erastin 是一种铁死亡 (ferroptosis) 诱导剂。Erastin 的铁死亡诱导机制与 ROS 和铁依赖性信号传导有关。Erastin 能够抑制电压依赖性阴离子通道 (VDAC2/VDAC3),加速氧化,导致内源活性氧积累。Erastin 还破坏线粒体通透性过渡孔 (mPTP),表现出抗肿瘤活性。

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Erastin Chemical Structure

Erastin Chemical Structure

CAS No. : 571203-78-6

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 293 篇科研文献

Cell Viability Assay
WB
Proliferation Assay
IF

    Erastin purchased from MCE. Usage Cited in: Gene. 2023 May 9;873:147468.  [Abstract]

    Erastin (8, 16 μM; 48 h) reduces the expression of xCT in AGS and BGC-823 cells.

    Erastin purchased from MCE. Usage Cited in: Gene. 2023 May 9;873:147468.  [Abstract]

    Erastin (8 μM; 48 h) greatly induces apoptosis and cell death in AGS and BGC-823 cells.

    Erastin purchased from MCE. Usage Cited in: Nat Cell Biol. 2022 Feb;24(2):168-180.  [Abstract]

    Survival rates of MCF10A-RAS cells cultured on stiff or soft Matrigel and treated for 48 h with Erastin (10-30 μM).

    Erastin purchased from MCE. Usage Cited in: Redox Biol. 2022 Aug;54:102382.  [Abstract]

    After treatment with Ferrostatin-1 (Fer-1, 5 μM) and GW4064 (1 μM) for 2 h, HK2 cells are treated with Erastin (5 μM) for another 24 h. Protein levels of GPX4 are detected by immunoblotting.

    Erastin purchased from MCE. Usage Cited in: Redox Biol. 2022 Aug;54:102382.  [Abstract]

    After treatment with Ferrostatin-1 (Fer-1, 5 μM) and GW4064 (1 μM) for 2 h, HK2 cells are treated with Erastin (5 μM) for another 24 h. After treatment with Fer-1 and GW4064, the cells are incubated with C11-BODIPY 581/591 (2 μM) and Hoechst 33258 for counterstaining; the images were then immediately visualized by confocal microscopy.

    Erastin purchased from MCE. Usage Cited in: Clin Transl Med. 2022 Apr;12(4):e752.  [Abstract]

    Representative images of intracellular mitochondrial superoxide level in SW480 and HT29 cells subjected to the stable knockdown of LINC001606 or stably overexpressing LINC001606 after treatment of DMSO, Erastin (10 μM) and RSL3 (2 μM) for 48 h.

    Erastin purchased from MCE. Usage Cited in: Cell Death Differ. 2020 Sep;27(9):2635-2650.  [Abstract]

    Erastin (10 μM; tail-injected intravenously; for 20 days) treatment of I/R mice significantly increases the protein/mRNA levels of TF and significantly decreased the percentage GSH and protein/mRNA levels of FTH1 and GPX4, but these effects are reversed by Liproxstatin-1 treatment.

    Erastin purchased from MCE. Usage Cited in: Cell Death Differ. 2020 Sep;27(9):2635-2650.  [Abstract]

    H&E and Masson’s staining of lung tissues show that Erastin (10 μM; tail-injected intravenously; for 20 days) aggravated edema, atelectasis, necrosis, alveolar and interstitial inflammation, and pulmonary fibrosis in I/R mice compared with sham mice, but these effects are reversed in I/R + erastin mice treated with Liproxstatin-1.

    Erastin purchased from MCE. Usage Cited in: Cell Death Differ. 2021 Apr;28(4):1222-1236.  [Abstract]

    Western blot analysis of the protein expression levels of BCAT2, AMPK, and pAMPK(T172) in Aspc-1, and HepG2 cells treated with Erastin (20 or 10 μM) Vin the absence or presence of AICAR (AMPK activator, 2 mmol/L) and Compound C (AMPK inhibitor, 1 μmol/L).

    Erastin purchased from MCE. Usage Cited in: Neurotherapeutics. 2020 Oct;17(4):1796-1812.  [Abstract]

    The effect of an inducer or inhibitor of ferroptosis on PC-12 cells. PC-12 cells are treated with 40 μM 6-OHDA in combination with an inducer (1 μM Erastin) of ferroptosis for 24 h. The expression of GPX4, TH, and FTH1 is significantly reduced in cells treated with the combination of erastin and 6-OHDA compared with those treated with 6-OHDA alone.

    Erastin purchased from MCE. Usage Cited in: Eur J Pharmacol. 2020 Dec 5;888:173574.  [Abstract]

    With the various dosage of ferroptosis inducer Erastin treatment for 24 h, the cell viability is determined by SRB method.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Erastin is a ferroptosis inducer. Erastin exhibits the mechanism of ferroptosis induction related to ROS and iron-dependent signaling. Erastin inhibits voltage-dependent anion channels (VDAC2/VDAC3) and accelerates oxidation, leading to the accumulation of endogenous reactive oxygen species. Erastin also disrupts mitochondrial permeability transition pore (mPTP) with anti-tumor activity[1][2][3].

    体外研究
    (In Vitro)

    Erastin (10 μM;24 小时) 触发异位子宫内膜间质细胞 (EESC) 的铁死亡,并在 9 小时时增加总 ROS 水平[1]
    Erastin 能够缩短 EESC 细胞中的线粒体长度并增加它的膜密度[1]
    Erastin (10 μM;9 小时) 降低铁相关蛋白的 mRNA 表达水平,例如 EESC 中的 FPN (铁输出蛋白)。 然而,Erastin 诱导的 EESCs 铁死亡能够被 FPN 的过表达显著抑制[1]
    Erastin (10 μM;24 小时) 在 HT-29 结直肠癌细胞中诱导线粒体通透性转换孔 (mPTP) 打开[2]
    Erastin (30 μM;72 小时) 显著抑制 HT-29 结直肠癌细胞的生长[2]
    Erastin 诱导铁死亡的分子机制与调节铁或线粒体脂肪酸代谢的基因有关。包括核糖体蛋白 L8、铁反应元件结合蛋白 2 (IREB2)、ATP 合酶 F0 复合亚基 C3、柠檬酸合酶、四肽重复结构域 35 和酰基辅酶 A 合成酶家族成员 2 (ACSF2)[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[1]

    Cell Line: Normal endometrial stromal cells (NESCs) and endometrial stromal cells (EESCs)
    Concentration: 0, 0.5, 0.8, 1, 1.5, 2, 2.5, 5, 10 μM
    Incubation Time: 24 hours
    Result: Induced cell detachment and overt death in EESCs, but not NESCs.

    Apoptosis Analysis[1]

    Cell Line: EESCs infected with adenovirus expressing FPN cDNA (co-incubation for 24 hr)
    Concentration: 0, 0.5, 1.5, 2.5, 5 and 2.5 μM
    Incubation Time: 24 hours
    Result: Induced ferroptosis by decreasing the levels of total ROS and lipid ROS. And reversed by the overexpression of FPN in adenovirus-infected cells.
    体内研究
    (In Vivo)

    Erastin 可用于动物建模,构建铁死亡诱导模型。

    Erastin (40 mg/kg;腹腔注射;每 3 天一次,持续 2 周) 抑制小鼠子宫内膜异位症模型中的子宫内膜异位植入,表明 Erastin 通过触发铁死亡使异位病变消退[1]
    Erastin (10 mg/kg、30 mg/kg;腹腔注射;每天一次,持续 4 周) 抑制 SCID 小鼠的 HT-29 异种移植物生长,在 30 mg/kg 处理下具有更有效的疗效[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Mouse model of endometriosis[1]
    Dosage: 40 mg/kg
    Administration: Intraperitoneal injection; once every 3 days for 2 weeks
    Result: Showed little impact on body weight of mice and hair of mice displayed neat and glossy.
    Reduced the volume of ectopic lesions.
    分子量

    547.04

    Formula

    C30H31ClN4O4

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 12.5 mg/mL (22.85 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8280 mL 9.1401 mL 18.2802 mL
    5 mM 0.3656 mL 1.8280 mL 3.6560 mL
    查看完整储备液配制表

    * 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 1.25 mg/mL (2.29 mM); 澄清溶液

      此方案可获得 ≥ 1.25 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 方案 二

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1 mg/mL (1.83 mM); 澄清溶液

      此方案可获得 ≥ 1 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: 50% PEG300    50% Saline

      Solubility: 5 mg/mL (9.14 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.76%

    参考文献

    完整储备液配制表

    * 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8280 mL 9.1401 mL 18.2802 mL 45.7005 mL
    5 mM 0.3656 mL 1.8280 mL 3.6560 mL 9.1401 mL
    10 mM 0.1828 mL 0.9140 mL 1.8280 mL 4.5700 mL
    15 mM 0.1219 mL 0.6093 mL 1.2187 mL 3.0467 mL
    20 mM 0.0914 mL 0.4570 mL 0.9140 mL 2.2850 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    Erastin
    目录号:
    HY-15763
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