Erastin is an inducer of ferroptosis, initiating cell death through mechanisms involving reactive oxygen species (ROS) and iron-dependent pathways. It targets and inhibits the voltage-dependent anion channels (VDAC2/VDAC3), which leads to an increase in oxidation and subsequently, a buildup of ROS within cells. Furthermore, Erastin interferes with the mitochondrial permeability transition pore (mPTP), displaying anti-tumor properties[1].[2].[3].
体内研究
For animal studies, Erastin is utilized to create models demonstrating ferroptosis. Administered intraperitoneally at 40 mg/kg every three days for a duration of two weeks, Erastin reduces endometriotic lesions in mice with endometriosis, suggesting it alleviates ectopic lesions by inducing ferroptosis[1].
At dosages of 10 mg/kg and 30 mg/kg, given intraperitoneally once daily for four weeks, Erastin curbs the growth of HT-29 xenografts in SCID mice, with the higher dosage displaying greater effectiveness[2].
体外研究
Upon administration at a concentration of 10 μM for 24 hours, Erastin incites ferroptosis in ectopic endometrial stromal cells (EESCs), coupled with an elevation in the total ROS levels observed at 9 hours post-treatment[1].
At a similar concentration and duration of 9 hours, Erastin leads to a reduction in the mRNA levels of iron metabolism-related proteins, such as FPN (an iron exporter), in EESCs. Nevertheless, overexpressing FPN significantly counters the ferroptosis induced by Erastin in these cells[1].
In HT-29 colorectal cancer cells, Erastin, at 10 μM over 24 hours, triggers the opening of the mitochondrial permeability transition pore (mPTP)[2].
When used at a concentration of 30 μM for 72 hours, it markedly impedes the proliferation of HT-29 colorectal cancer cells[2].
Erastin/爱拉斯汀 细胞实验
Cell Line
Concentration
Treated Time
Description
References
N27 cells
36~116 nM (erastin), 29~73 nM (RSL3)
24 hours
GNF-5837 significantly inhibits erastin- and RSL3-induced ferroptosis
Int J Mol Sci. 2022;23(24):16205.
HT-1080 cells
36~116 nM (erastin), 29~73 nM (RSL3)
24 hours
GNF-5837 significantly prevents ferroptosis
Int J Mol Sci. 2022;23(24):16205.
HT-22 cells
36~116 nM (erastin), 29~73 nM (RSL3)
24 hours
GNF-5837 significantly prevents ferroptosis
Int J Mol Sci. 2022;23(24):16205.
KYSE510 cells
50 μM and 100 μM
24 hours
Evaluate the effects of Erastin on cell viability and ATP levels, results showed Erastin decreased cell viability and ATP levels.
Anim Cells Syst (Seoul). 2024 May 11;28(1):237-250.
KYSE30 cells
50 μM and 100 μM
24 hours
Evaluate the effects of Erastin on cell viability and ATP levels, results showed Erastin decreased cell viability and ATP levels.
Anim Cells Syst (Seoul). 2024 May 11;28(1):237-250.
HT22 mouse hippocampal neuronal cells
0.8 μM
24 hours
To evaluate the protective effect of catechol estrogens against erastin/RSL3-induced ferroptosis. Results showed that four catechol estrogens (2-OH-E1, 2-OH-E2, 4-OH-E1, and 4-OH-E2) significantly inhibited erastin/RSL3-induced cell death and reduced the accumulation of NO, ROS, and lipid-ROS.
Sci Rep. 2024 Oct 14;14(1):23988.
Res1-6 and Hepa1-6 cells
5.0 μM
30 minutes
Detect lipid ROS levels, finding that Res1-6 cells showed significantly reduced lipid ROS levels induced by erastin
Cell Rep Med. 2024 Feb 20;5(2):101415.
KYSE510
50 μM, 100 μM
24 hours
To evaluate the effect of Erastin on KYSE510 cell proliferation, results showed that Erastin significantly inhibited cell proliferation and colony formation ability, decreased ATP levels and increased ROS production.
Anim Cells Syst (Seoul). 2024 May 11;28(1):237-250
KYSE30
50 μM, 100 μM
24 hours
To evaluate the effect of Erastin on KYSE30 cell proliferation, results showed that Erastin significantly inhibited cell proliferation and colony formation ability, decreased ATP levels and increased ROS production.
Anim Cells Syst (Seoul). 2024 May 11;28(1):237-250
KYSE510
50 μM, 100 μM
24 hours
Evaluate the effect of Erastin on the proliferation of KYSE510 cells. Results showed that Erastin significantly inhibited cell proliferation and colony formation ability, reduced ATP levels, and increased ROS production.
Anim Cells Syst (Seoul). 2024 May 11;28(1):237-250
KYSE30
50 μM, 100 μM
24 hours
Evaluate the effect of Erastin on the proliferation of KYSE30 cells. Results showed that Erastin significantly inhibited cell proliferation and colony formation ability, reduced ATP levels, and increased ROS production.
Anim Cells Syst (Seoul). 2024 May 11;28(1):237-250
NCI-H660
1.25, 2.5, 5, 10, 20 μM
72 h
To evaluate the effect of Erastin on prostate cancer cell growth, results showed that Erastin significantly reduced the viability of NCI-H660 cells.
Cancer Res. 2021 Mar 15;81(6):1583-1594.
LNCaP
1.25, 2.5, 5, 10, 20 μM
72 h
To evaluate the effect of Erastin on prostate cancer cell growth, results showed that Erastin significantly reduced the viability of LNCaP cells.
Cancer Res. 2021 Mar 15;81(6):1583-1594.
C4-2
1.25, 2.5, 5, 10, 20 μM
72 h
To evaluate the effect of Erastin on prostate cancer cell growth, results showed that Erastin significantly reduced the viability of C4-2 cells.
Cancer Res. 2021 Mar 15;81(6):1583-1594.
22Rv1
1.25, 2.5, 5, 10, 20 μM
72 h
To evaluate the effect of Erastin on prostate cancer cell growth, results showed that Erastin significantly reduced the viability of 22Rv1 cells.
Cancer Res. 2021 Mar 15;81(6):1583-1594.
ARCaP
1.25, 2.5, 5, 10, 20 μM
72 h
To evaluate the effect of Erastin on prostate cancer cell growth, results showed that Erastin significantly reduced the viability of ARCaP cells.
Cancer Res. 2021 Mar 15;81(6):1583-1594.
PC3
1.25, 2.5, 5, 10, 20 μM
72 h
To evaluate the effect of Erastin on prostate cancer cell growth, results showed that Erastin significantly reduced the viability of PC3 cells.
Cancer Res. 2021 Mar 15;81(6):1583-1594.
DU145
1.25, 2.5, 5, 10, 20 μM
72 h
To evaluate the effect of Erastin on prostate cancer cell growth, results showed that Erastin significantly reduced the viability of DU145 cells.
Cancer Res. 2021 Mar 15;81(6):1583-1594.
PM3
6 µM
24 h
Erastin enhanced ACSL4 expression and reduced GPX4, which was alleviated by Fer-1. However, exogenous overexpression of wild-type NF2 abrogated the changes induced by Erastin and Fer-1.
Neuro Oncol. 2021 Dec 1;23(12):2014-2027.
IOMM-Lee
6 µM
24 h
Erastin induced ACSL4 upregulation in NF2-silenced IOMM-Lee cells, which was alleviated by Fer-1.
Neuro Oncol. 2021 Dec 1;23(12):2014-2027.
CH157
6 µM
24 h
Erastin enhanced ACSL4 expression and reduced GPX4, which was alleviated by Fer-1. However, exogenous overexpression of wild-type NF2 abrogated the changes induced by Erastin and Fer-1.
Neuro Oncol. 2021 Dec 1;23(12):2014-2027.
G-361 melanoma cells
5 µM
24 h
To investigate the degradation of VDAC2/3 by Erastin, it was found that the protein levels of VDAC2/3 were significantly reduced after Erastin treatment, indicating that Erastin induced the degradation of VDAC2/3.
Nat Commun. 2020 Jan 23;11(1):433.
A375 melanoma cells
5 µM
24 h
To investigate the degradation of VDAC2/3 by Erastin, it was found that the fluorescence intensity of VDAC2/3 was significantly reduced after Erastin treatment, indicating that Erastin induced the degradation of VDAC2/3.
Nat Commun. 2020 Jan 23;11(1):433.
human HT1080 fibrosarcoma cells
2 μM
10-14 h
To study the effect of Erastin on HT1080 cells, results showed that Erastin induced ferroptosis.
Nat Commun. 2024 Oct 17;15(1):8971.
mouse embryonic fibroblast (MEF) cells
2 μM
8-12 h
To study the effect of Erastin on MEF cells, results showed that Erastin induced ferroptosis.
Nat Commun. 2024 Oct 17;15(1):8971.
4T1 cells
2.9 μM
24 h
CuP/Er enhances ferroptosis via ROS generation, lipid peroxidation, and GSH depletion, and induces cuproptosis, leading to mitochondrial dysfunction and irreparable mitochondrial damage.
Adv Sci (Weinh). 2024 Jun;11(23):e2310309.
Mouse lung epithelial (MLE-2) cells
10 μM
24 h
To investigate the effect of Erastin on hypoxia/reoxygenation (HR)-induced acute lung injury (ALI) and ferroptosis. Results showed that Erastin significantly increased the expression of ferroptosis-related proteins in HR-induced MLE-2 cells, and liproxstatin-1 reversed this effect.
Cell Death Differ. 2020 Sep;27(9):2635-2650.
HT-1080 cells
5 μM
6 h
To evaluate the effect of Erastin on glutathione (GSH) levels, results showed that Erastin significantly reduced intracellular GSH levels, indicating it induces ferroptosis by inhibiting system xc−.
Nat Chem Biol. 2018 May;14(5):507-515.
HT-1080 cells
10 μM
6 h
To evaluate the lipid peroxidation induced by Erastin and FINO 2, results showed that both Erastin and FINO 2 increased the fluorescence intensity of C-11 BODIPY, indicating they induced lipid peroxidation, with FINO 2 showing a stronger effect.
Nat Chem Biol. 2018 May;14(5):507-515.
Erastin/爱拉斯汀 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
Cholangiocarcinoma xenograft model
Intraperitoneal injection
15 mg/kg
Once every 2 days, total of 10 times, lasting 20 days
To evaluate the effect of IDH1 mutation on erastin-induced tumor growth inhibition in cholangiocarcinoma, results showed that IDH1 mutation promoted the tumor-suppressive effect of erastin
Open Med (Wars). 2022 May 6;17(1):863-870
BALB/c nude mice
Cholangiocarcinoma xenograft model
Intraperitoneal injection
15 mg/kg
Once every 2 days, a total of 10 times, for 20 days
To investigate the effect of IDH1 mutation on erastin-induced tumor growth inhibition in cholangiocarcinoma, results showed that IDH1 mutation promoted erastin-induced tumor growth inhibition
Open Med (Wars). 2022 May 6;17(1):863-870
NSG (NOD-SCID-IL2R γ) male mice
DU145, ARCaP, PC3, H660 prostate cancer xenograft models
Intraperitoneal injection
20 mg/kg
Once daily
To evaluate the effect of Erastin on prostate cancer xenograft tumor growth, results showed that Erastin significantly delayed tumor growth.
Cancer Res. 2021 Mar 15;81(6):1583-1594.
Nude mice
Subcutaneous transplantation of IOMM-Lee cells
Intraperitoneal injection
15 mg/kg
Twice every other day for 35 days
Erastin slowed tumor growth rate, and MEF2C knockdown further enhanced the tumor inhibition effect of Erastin. NF2 or E-cadherin overexpression restored the growth of Erastin-treated shMEF2C 1# IOMM-Lee tumors.
Neuro Oncol. 2021 Dec 1;23(12):2014-2027.
Nude mice
Subcutaneous melanoma model
Intraperitoneal injection
15 mg/kg
Twice every other day for 20 days
To investigate the effect of Nedd4 knockdown on Erastin-induced ferroptosis in melanoma cells, it was found that Nedd4 knockdown significantly enhanced Erastin-induced tumor reduction and ferroptosis.
Nat Commun. 2020 Jan 23;11(1):433.
Nude mice
OS-RC-2 tumor model
Intraperitoneal injection
40 mg/kg
Every other day for 12 days
To study the synergistic effect of IKE and SAM on tumor growth suppression, results showed that SAM enhanced the inhibitory effect of IKE.
Nat Commun. 2024 Oct 17;15(1):8971.
Mice
MC38 colon cancer model
Intravenous injection
30 mg/kg
Once every three days for a total of three doses
CuP/Er significantly inhibits tumor growth by inducing ferroptosis and cuproptosis, and further enhances the antitumor effect when combined with an anti-PD-L1 antibody, preventing tumor metastasis.
Adv Sci (Weinh). 2024 Jun;11(23):e2310309.
Mice
Intestinal ischemia/reperfusion (I/R)-induced acute lung injury (ALI) model
Tail vein injection
10 μM
Daily for 20 days
To investigate the effect of Erastin on intestinal ischemia/reperfusion (I/R)-induced acute lung injury (ALI) and ferroptosis. Results showed that Erastin significantly increased oxidative stress markers (MDA, Fe2+) and decreased GSH levels in I/R mice, and liproxstatin-1 reversed this effect.
Induction of cell death in human A673 cells, EC50=30 μM.
17568748
human BJ cells
Function assay
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, IC50=0.9 μM.
17568748
human BJ cells
Function assay
Induction of cell death in TERT expressing human BJ cells, EC50=10 μM.
17568748
human BJ cells
Function assay
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, IC50=31.2 μM.
17568748
human BJ cells
9 μM
Function assay
Induction of cell death in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells at 9 uM.
17568748
human BJ cells
4.6 μM
Function assay
Increase in intracellular oxidative species in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells at 4.6 uM
17568748
human BJeH cells
Function assay
6 h
Induction of reactive oxygen species production in human BJeH cells expressing wild type RAS after 6 hrs by DCF-based flow cytometric analysis
22832321
human BJeLR cells
10 μM
Cytotoxic assay
12 h
Cytotoxicity against human BJeLR cells expressing RAS G12V mutant at 10 uM at 12 hrs by trypan blue staining
22832321
human Calu1 cells
Function assay
Inhibition of human Calu1 cells expressing KRAS with activating mutations by trypan blue exclusion assay, IC50=4 μM.
17568748
human CCF-STTG1 cells
Function assay
Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry, IC50=0.2 μM.
26231156
human EWS502 cells
Function assay
Induction of cell death in human EWS502 cells, EC50=10 μM.
17568748
human HeLa cells
Function assay
Induction of cell death in human HeLa cells, EC50=0.6 μM.
17568748
human HOS cells
Function assay
Induction of cell death in human HOS cells , EC50=17 μM.
17568748
human Hs51.T cells
Function assay
Induction of cell death in human Hs51.T cells, EC50=12 μM.
17568748
human Hs925.T cells
Function assay
Induction of cell death in human Hs925.T cells, EC50=17 μM.
17568748
human HT1080 cells
Function assay
Induction of cell death in human HT1080 cells in presence of PD-98059 by trypan blue exclusion method, IC50=1 μM.
17568748
human LNCaP cells
Function assay
Induction of cell death in human LNCaP cells, EC50=6 μM.
17568748
human MES-SA cells
Function assay
Induction of cell death in human MES-SA cells, EC50=3 μM.
17568748
human MX2 cells
Function assay
Induction of cell death in human MX2 cells, EC50=18 μM.
17568748
human SK-N-MC cells
Function assay
Induction of cell death in human SK-N-MC cells, EC50=10 μM.
17568748
human SKUT cells
Function assay
Induction of cell death in human SKUT cells, EC50=4 μM.
17568748
human SVR cells
Function assay
Induction of cell death in human SVR cells, EC50=2.5 μM.
17568748
human TC32 cells
Function assay
Induction of cell death in human TC32 cells
17568748
human TC71 cells
Function assay
Induction of cell death in human TC71 cells, EC50=10 μM.
17568748
human U2OS cells
Function assay
Induction of cell death in human U2OS cells, EC50=6 μM.
17568748
human U937 cells
Function assay
Induction of cell death in human U937 cells, EC50=10 μM.
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