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Chemical Structure| 571203-78-6 Chemical Structure| 571203-78-6

Structure of Erastin
CAS No.: 571203-78-6

Chemical Structure| 571203-78-6

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Erastin is a kind of iron death inducer, which inhibits the voltage-dependent anion flux (VDAC2/VDAC3), leads to the accumulation of endogenous reactive oxygen species, accelerates oxidation, and destroys the mitochondrial permeability transition pore mPTP, showing anti-tumor activity.

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Product Details of Erastin

CAS No. :571203-78-6
Formula : C30H31ClN4O4
M.W : 547.04
SMILES Code : O=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5
MDL No. :MFCD09837984
InChI Key :BKQFRNYHFIQEKN-UHFFFAOYSA-N
Pubchem ID :11214940

Safety of Erastin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Erastin

ferroptosis

Isoform Comparison

Biological Activity

Description
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].

In Vitro:

Cell Line
Concentration Treated Time Description References
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. PMC7969452
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. PMC7969452
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. PMC7969452
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. PMC7969452
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. PMC7969452
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. PMC7969452
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. PMC7969452
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. PMC8643460
IOMM-Lee 6 µM 24 h Erastin induced ACSL4 upregulation in NF2-silenced IOMM-Lee cells, which was alleviated by Fer-1. PMC8643460
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. PMC8643460
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. PMC6978386
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. PMC6978386
Human HT1080 fibrosarcoma cells 2 μM 10-14 h To study the effect of Erastin on HT1080 cells, results showed that Erastin induced ferroptosis. PMC11487270
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. PMC11487270
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. PMC11187894
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. PMC7429834
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−. PMC5899674
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. PMC5899674
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. PMC11473836
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 PMC10897610

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
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. PMC7969452
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. PMC8643460
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. PMC6978386
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. PMC11487270
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. PMC11187894
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. PMC7429834

Protocol

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1.83mL

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