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

Erastin 是一種鐵死亡 (ferroptosis) 誘導劑。Erastin 的鐵死亡誘導機制與 ROS 和鐵依賴性信號傳導有關(guān)。Erastin 能夠抑制電壓依賴性陰離子通道 (VDAC2/VDAC3)，加速氧化，導致內(nèi)源活性氧積累。Erastin 還破壞線粒體通透性過渡孔 (mPTP)，表現(xiàn)出抗腫瘤活性。此外，Erastin 能夠阻斷 SLC7A11 介導的胱氨酸攝取，也使 UMRC6-EV 和 -C91A 細胞在葡萄糖饑餓時免于雙硫死亡 (disulfidptosis)。

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Erastin Chemical Structure

Erastin Chemical Structure

CAS No. : 571203-78-6

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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥500
In-stock
1 mg * 5 ￥1800
In-stock
1 mg * 10 ￥3000
In-stock
5 mg   詢價  
10 mg   詢價  

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Customer Review

Other Forms of Erastin:

MCE活性驗證

以上結(jié)果經(jīng)由 MCE 實驗室檢測獲得。

MCE 顧客使用本產(chǎn)品發(fā)表的 474 篇科研文獻

Cell Viability Assay
WB
Proliferation Assay
IF

    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: 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: 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. 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: 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: 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]

    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. 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. 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

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    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. Furthermore, Erastin can block the uptake of cystine mediated by SLC7A11 and also spares UMRC6-EV and -C91A cells from disulfidptosis under glucose starvation[1][2][3][4][5][6][7][8][9][10][11][12][13][14].

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    BJ IC50
    0.9 μM
    Compound: erastin
    Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells in presence of PD-98059 by trypan blue exclusion method
    Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells in presence of PD-98059 by trypan blue exclusion method
    		[PMID: 17568748]
    BJ IC50
    0.9 μM
    Compound: erastin
    Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells in presence of MEK inhibitor 2 by trypan blue exclusion method
    Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells in presence of MEK inhibitor 2 by trypan blue exclusion method
    		[PMID: 17568748]
    BJ IC50
    2 μM
    Compound: erastin
    Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells in presence of MEK 1/2 inhibitor by trypan blue exclusion method
    Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells in presence of MEK 1/2 inhibitor by trypan blue exclusion method
    		[PMID: 17568748]
    BJ IC50
    2.6 μM
    Compound: erastin
    Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes in presence of MEK inhibitor by trypan blue exclusion method
    Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes in presence of MEK inhibitor by trypan blue exclusion method
    		[PMID: 17568748]
    BJ IC50
    31.2 μM
    Compound: erastin
    Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes in presence of U0126 by trypan blue exclusion method
    Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes in presence of U0126 by trypan blue exclusion method
    		[PMID: 17568748]
    Calu-1 IC50
    4 μM
    Compound: erastin
    Inhibition of human Calu1 cells expressing KRAS with activating mutations by trypan blue exclusion assay
    Inhibition of human Calu1 cells expressing KRAS with activating mutations by trypan blue exclusion assay
    		[PMID: 17568748]
    CCF-STTG1 IC50
    200 nM
    Compound: ERA
    Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry
    Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry
    		[PMID: 26231156]
    HT-1080 IC50
    1 μM
    Compound: erastin
    Induction of cell death in human HT1080 cells in presence of PD-98059 by trypan blue exclusion method
    Induction of cell death in human HT1080 cells in presence of PD-98059 by trypan blue exclusion method
    		[PMID: 17568748]
    HT-1080 IC50
    1.3 μM
    Compound: erastin
    Induction of cell death in human HT1080 cells in presence of MEK inhibitor 2 by trypan blue exclusion method
    Induction of cell death in human HT1080 cells in presence of MEK inhibitor 2 by trypan blue exclusion method
    		[PMID: 17568748]
    HT-1080 IC50
    2.5 μM
    Compound: erastin
    Induction of cell death in human HT1080 cells in presence of MEK inhibitor by trypan blue exclusion method
    Induction of cell death in human HT1080 cells in presence of MEK inhibitor by trypan blue exclusion method
    		[PMID: 17568748]
    HT-1080 IC50
    3.4 μM
    Compound: erastin
    Induction of cell death in human HT1080 cells in presence of U0126 by trypan blue exclusion method
    Induction of cell death in human HT1080 cells in presence of U0126 by trypan blue exclusion method
    		[PMID: 17568748]
    HT-1080 IC50
    6 μM
    Compound: erastin
    Induction of cell death in human HT1080 cells in presence of MEK 1/2 inhibitor by trypan blue exclusion method
    Induction of cell death in human HT1080 cells in presence of MEK 1/2 inhibitor by trypan blue exclusion method
    		[PMID: 17568748]
    體外研究
    (In Vitro)

    Erastin (10 μM；24 小時) 觸發(fā)異位子宮內(nèi)膜間質(zhì)細胞 (EESC) 的鐵死亡，并在 9 小時時增加總 ROS 水平[1]。
    Erastin 能夠縮短 EESC 細胞中的線粒體長度并增加它的膜密度[1]。
    Erastin (10 μM；9 小時) 降低鐵相關(guān)蛋白的 mRNA 表達水平，例如 EESC 中的 FPN (鐵輸出蛋白)。 然而，Erastin 誘導的 EESCs 鐵死亡能夠被 FPN 的過表達顯著抑制[1]。
    Erastin (10 μM；24 小時) 在 HT-29 結(jié)直腸癌細胞中誘導線粒體通透性轉(zhuǎn)換孔 (mPTP) 打開[2]。
    Erastin (30 μM；72 小時) 顯著抑制 HT-29 結(jié)直腸癌細胞的生長[2]。
    Erastin 誘導鐵死亡的分子機制與調(diào)節(jié)鐵或線粒體脂肪酸代謝的基因有關(guān)。包括核糖體蛋白 L8、鐵反應(yīng)元件結(jié)合蛋白 2 (IREB2)、ATP 合酶 F0 復合亞基 C3、檸檬酸合酶、四肽重復結(jié)構(gòu)域 35 和?；o酶 A 合成酶家族成員 2 (ACSF2)[3]。
    Note:
    1. 不同細胞系對同種藥物的敏感程度可能會有所差別，經(jīng)文獻報道，A549， HCT116， HepG2， H1299 細胞系可能對 Erastin 不敏感[3][4][5]。
    2. 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    鐵死亡敏感細胞系

    敏感細胞系 實驗條件
    SKOV3[6] 5-20 μM; 1-7 days
    OVCA429[6] 5-20 μM; 1-7 days
    MCF10A-RAS[7] 0-30 μM; 48 h
    HT-22 neuron[8] 500 nM; 16 h
    NCI-H508[9] 0.1-10 μM; 48?h
    LoVo[9] 0.1-10 μM; 48?h
    LS513[9] 0.1-10 μM; 48?h
    SW480[9] 0.1-10 μM; 48?h
    SW620[9] 0.1-10 μM; 48?h
    SW1116[9] 0.1-10 μM; 48?h
    DLD-1[9] 0.1-10 μM; 48?h
    Caco-2[9] 0.1-10 μM; 48?h
    SW837[10] 0-40 μM; 24 h
    Pfa1[11] 0.1-5 μM; 48 h
    HT-1080[11] 0.1-5 μM; 48 h
    MAD-MB-231[12] 0-100 μM; 72 h; IC50: 9.55 μM
    HCC1937[12] 0-100 μM; 72 h; IC50: 11.58 μM


    鐵死亡不敏感細胞系
    不敏感細胞系 實驗條件
    HCT116[10] 0-40 μM; 24 h
    SW48[10] 0-40 μM; 24 h
    HepG2[5] 0-20 μM; 24 h
    MDA-MB-436[13] 0.1-25 μM; 24 h
    HT-29[13] 0.1-25 μM; 24 h
    U-373[13] 0.1-25 μM; 24 h

    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.
    體內(nèi)研究
    (In Vivo)

    Erastin 可用于動物建模，構(gòu)建鐵死亡誘導模型。

    Erastin (40 mg/kg；腹腔注射；每 3 天一次，持續(xù) 2 周) 抑制小鼠子宮內(nèi)膜異位癥模型中的子宮內(nèi)膜異位植入，表明 Erastin 通過觸發(fā)鐵死亡使異位病變消退[1]。
    Erastin (10 mg/kg、30 mg/kg；腹腔注射；每天一次，持續(xù) 4 周) 抑制 SCID 小鼠的 HT-29 異種移植物生長，在 30 mg/kg 處理下具有更有效的療效[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 號
    性狀

    固體

    顏色

    White to off-white

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years

    *該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 12.5 mg/mL (22.85 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

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

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    90% Corn Oil

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

      此方案可獲得 ≥ 1.25 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。

      以 1 mL 工作液為例，取 100 μL 12.5 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

    • 方案 二

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 1 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 10.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 5 mg/mL (9.14 mM); 懸濁液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

    *該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.76%

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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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