Erastin

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].

Product Specifications

CAS Number

[571203-78-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Disulfidptosis; Ferroptosis; VDAC

Type

Reference compound

Related Pathways

Apoptosis; Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Erastin.html

Purity

99.94

Solubility

DMSO : 12.5 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

Smiles

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

Molecular Formula

C30H31ClN4O4

Molecular Weight

547.04

Precautions

H302, H315, H319, H335

References & Citations

[1]Li Y, et al. Erastin induces ferroptosis via ferroportin-mediated iron accumulation in endometriosis. Hum Reprod. 2021 Mar 18;36 (4) :951-964. |[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.|[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. |[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. |[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.|[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.|[8]Chen T, et al., Mitochondrial transplantation rescues neuronal cells from ferroptosis. Free Radic Biol Med. 2023 Nov 1;208:62-72. |[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. |[10]Xie Y, et al., The Tumor Suppressor p53 Limits Ferroptosis by Blocking DPP4 Activity. Cell Rep. 2017 Aug 15;20 (7) :1692-1704.|[11]Doll S, et al., FSP1 is a glutathione-independent ferroptosis suppressor. Nature. 2019 Nov;575 (7784) :693-698.|[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.|[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. |[14]Wang J, et al. Tumor suppressor BAP1 suppresses disulfidptosis through the regulation of SLC7A11 and NADPH levels[J]. Oncogenesis, 2024, 13 (1) : 31.