Erastin is a compound that interacts with VDAC, blocks and reverses mitochondrial depolarization after microtubule destabilizers in intact cells and antagonized tubulin-induced VDAC blockage in planar bilayers. It is also a ferroptosis inducer. (Unstable in solution, please prepare and use now).
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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 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
human A673 cells
Function assay
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.
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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