Erastin

Name: Erastin
Brand: MedChemExpress
SKU: HY-15763
Rating: 5.0 (526 reviews)

Cat. No.: HY-15763 Purity: 99.62%: FAQs
Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 571203-78-6

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
1 mg * 5	In-stock	Estimated Time of Arrival: December 31
1 mg * 10	In-stock	Estimated Time of Arrival: December 31
5 mg	Get quote
10 mg	Get quote

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Customer Review

Based on 526 publication(s) in Google Scholar

Other Forms of Erastin:

Imidazole ketone erastin Get quote

515 Publications Citing Use of MCE Erastin

Cell Viability Assay

Proliferation Assay

: Erastin purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

MCE Biological Validation

Cell Viability Assay

: HT-1080 cells were seeded at 60000 cells/well in a 24 well plate and were cultured overnight. Then, cells were treated with Erastin (HY-15763) (0-100 nM) for 24 h, and the expression of GPX-4 was measured. The results indicated that Erastin inhibits GPX-4 expression. Primary antibody: GPX-4 antibody (HY-P80450), GAPDH antibody (HY-P80137).

: HT-1080 cells were seeded at 8000 cells/well in a 96-well plate and were cultured overnight. Then, cells were treated with Erastin (HY-15763) (0-400 nM) for 24 h, and the cell viability was assayed by CCK-8 kit (HY-K0301). The results indicated that Erastin inhibits the cell viability.

: HT-1080 cells were seeded at 8000 cells/well in a 96 well plate and were cultured overnight. Then, cells are treated with 200 nM Erastin (HY-15763) in the presence or absence of Ferrostatin-1 (HY-100579) (Fer-1, 0.5 μM) for 24 h. The results indicated that Fer-1 inhibits the ferroptosis induced by Erastin.

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Biological Activity
Purity & Documentation
References
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Description

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]

In Vitro

Erastin (10 μM; 24 h) triggers ferroptosis in ectopic endometrial stromal cells (EESCs), and increases the total ROS level at 9 h^[1].
Erastin shorts mitochondria and increases membrane density in EESCs^[1].
Erastin (10 μM; 9 h) decreases the mRNA expression levels of iron-related proteins, such FPN (iron exporter) in EESCs. However, FPN overexpression significantly inhibits erastin-induced ferroptosis in EESCs^[1].
Erastin (10 μM; 24 h) induces mitochondrial permeability transition pore (mPTP) opening in HT-29 colorectal cancer cells^[2].
Erastin (30 μM; 72 h) significantly inhibits the growth of HT-29 colorectal cancer cells^[2].
The molecular mechanism by which Erastin induces ferroptosis is related to genes regulating iron or mitochondrial fatty acid metabolism. Includes ribosomal protein L8, iron response element binding protein 2 (IREB2), ATP synthase F0 complex subunit C3, citrate synthase, tetrapeptide repeat domain 35, and acyl-CoA synthetase family member 2 (ACSF2)^[3].
Note:
1. Different cell lines may have different sensitivity to a same compound. As reported, A549, HCT116, HepG2, H1299 cells may be insensitive to Erastin^[3]^[4]^[5].
2. Erastin is unstable in solution. Freshly prepared is recommended.

Ferroptosis-sensitive Cell Lines

Ferroptosis-sensitive Cells	Test Conditions
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^[12]	0.1-5 μM; 48 h
MAD-MB-231^[13]	0-100 μM; 72 h; IC₅₀: 9.55 μM
HCC1937^[13]	0-100 μM; 72 h; IC₅₀: 11.58 μM

Ferroptosis-insensitive Cell Lines

Ferroptosis-insensitive Cells	Test Conditions
HCT116^[11]	0-40 μM; 24 h
SW48^[11]	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

MedChemExpress (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.

In Vivo

Erastin can be used in animal modeling to construct ferroptosis induction model.

Erastin (40 mg/kg; i.p.; once every 3 days for 2 weeks) suppresses endometriotic implants in the mouse endometriosis model, indicating Erastin regresses ectopic lesions by trigging ferroptosis^[1].
Erastin (10 mg/kg, 30 mg/kg; i.p.; once daily for 4 weeks) suppresses HT-29 xenograft growth in SCID mice, with more potent efficacy under 30 mg/kg treatment^[2].

MedChemExpress (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.

Molecular Weight

547.04

Formula

C₃₀H₃₁ClN₄O₄

CAS No.

571203-78-6

Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (22.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.1828 mL	0.9140 mL	1.8280 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (2.29 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (1.83 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 15% Cremophor EL 85% Water
Solubility: 10 mg/mL (18.28 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (297 KB) SDS (393 KB)

COA (0 KB) HNMR (308 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Li Y, et al. Erastin induces ferroptosis via ferroportin-mediated iron accumulation in endometriosis. Hum Reprod. 2021 Mar 18;36(4):951-964. [Content Brief]

[2]. 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. [Content Brief]

[3]. Xie Y, et al. Ferroptosis: process and function. Cell Death Differ. 2016 Mar;23(3):369-79. [Content Brief]

[4]. Gai C, et al. MT1DP loaded by folate-modified liposomes sensitizes erastin-induced ferroptosis via regulating miR-365a-3p/NRF2 axis in non-small cell lung cancer cells. Cell Death Dis. 2020 Sep 14;11(9):751. [Content Brief]

[5]. Yang Y, et al. Piperlongumine Inhibits Thioredoxin Reductase 1 by Targeting Selenocysteine Residues and Sensitizes Cancer Cells to Erastin. Antioxidants (Basel). 2022 Apr 4;11(4):710. [Content Brief]

[6]. Liu N, et al., Activation of the reverse transsulfuration pathway through NRF2/CBS confers erastin-induced ferroptosis resistance. Br J Cancer. 2020 Jan;122(2):279-292. [Content Brief]

[7]. Romani P, et al., Mitochondrial fission links ECM mechanotransduction to metabolic redox homeostasis and metastatic chemotherapy resistance. Nat Cell Biol. 2022 Feb;24(2):168-180. [Content Brief]

[8]. Chen T, et al., Mitochondrial transplantation rescues neuronal cells from ferroptosis. Free Radic Biol Med. 2023 Nov 1;208:62-72. [Content Brief]

[9]. Zhu JF, et al., Ibrutinib facilitates the sensitivity of colorectal cancer cells to ferroptosis through BTK/NRF2 pathway. Cell Death Dis. 2023 Feb 23;14(2):151. [Content Brief]

[10]. Xie Y, et al., The Tumor Suppressor p53 Limits Ferroptosis by Blocking DPP4 Activity. Cell Rep. 2017 Aug 15;20(7):1692-1704. [Content Brief]

[11]. Doll S, et al., FSP1 is a glutathione-independent ferroptosis suppressor. Nature. 2019 Nov;575(7784):693-698. [Content Brief]

[12]. Li P, et al., Inhibition of cannabinoid receptor type 1 sensitizes triple-negative breast cancer cells to ferroptosis via regulating fatty acid metabolism. Cell Death Dis. 2022 Sep 21;13(9):808. [Content Brief]

[13]. Zheng J, et al., Sorafenib fails to trigger ferroptosis across a wide range of cancer cell lines. Cell Death Dis. 2021 Jul 13;12(7):698. [Content Brief]

[14]. Wang J, et al. Tumor suppressor BAP1 suppresses disulfidptosis through the regulation of SLC7A11 and NADPH levels[J]. Oncogenesis, 2024, 13(1): 31. [Content Brief]

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	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

Erastin Related Classifications

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.

Keywords:

Erastin571203-78-6VDACFerroptosisVoltage-dependent anion channel Inhibitorinhibitorinhibit

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Erastin

Customer Review

Other Forms of Erastin:

Erastin Related Antibodies

515 Publications Citing Use of MCE Erastin

MCE Biological Validation

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Purity & Documentation

References

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Erastin Related Antibodies

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Erastin Related Classifications

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