Erastin

Catalog No.S7242

Erastin Chemical Structure

Molecular Weight(MW): 547.04

Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS.

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Cited by 56 Publications

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Biological Activity

Description Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS.
Targets
Ferroptosis [1]
In vitro

Erastin is selectively lethal to oncogenic RAS-mutant cell lines, and triggers a unique iron-dependent form of non-apoptotic cell death called ferroptosis. [1] [2] Erastin binds directly to VDAC2 and causes mitochondrial damage via ROS production in an NADH-dependent manner, which induces cell death in some tumor cells harbouring activating mutations in the RAS-RAF-MEK pathway. [3] In addition, erastin, via inducing ROS-mediated CID (Caspase-independent cell death), strongly enhances the effect of cisplatin in WT EGFR cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CCF-STTG1 cells NVeyVpRkTnWwY4Tpc44h[XO|YYm= NIfp[mpKdmirYnn0bY9vKG:oIGjjeEBqdiCqdX3hckBES0ZvU2TUS|Eh[2WubIOgZZN{\XO|ZXSgZZMh\2y3dHHtZZRmKHKnbHXhd4Uh[W[2ZYKgNkBpenNiYomg[ox2d3KxbXX0dpktKEmFNUC9NE4zKM7:TT6= NF[we44zPjJ|MUG1Oi=>
human HeLa cells MoD3SpVv[3Srb36gZZN{[Xl? MXTJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCKZVzhJINmdGy|LDDFR|UxRTBwNjFOwG0v NYHJfHBHOTd3Nki3OFg>
human BJ cells NHez[YNHfW6ldHnvckBie3OjeR?= NVToXnZ6UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gRmoh[2WubIOg[ZhxemW|c3nu[{BVTVKWLDDMWEwhW1RiYX7kJHJCWyCJMULWJI12fGGwdDDn[Y5meyClZXzsd{BqdiCycnXz[Y5k\SCxZjDQSE06QDB3OTDifUB1enmyYX6gZox2\SCneHPseZNqd25ibXX0bI9lNCCLQ{WwQVAvQSEQvF2u MofXNVc2Pjh5NEi=
human HT1080 cells MVLGeY5kfGmxbjDhd5NigQ>? M4XHS2lv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFjUNVA5OCClZXzsd{BqdiCycnXz[Y5k\SCxZjDQSE06QDB3OTDifUB1enmyYX6gZox2\SCneHPseZNqd25ibXX0bI9lNCCLQ{WwQVEh|ryPLh?= MX2xO|U3QDd2OB?=
human SVR cells NHHiXItHfW6ldHnvckBie3OjeR?= M2PYXWlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIGPWVkBk\WyuczygSWM2OD1{LkWg{txONg>? Ml3pNVc2Pjh5NEi=
human MES-SA cells MWDGeY5kfGmxbjDhd5NigQ>? MUPJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCPRWOtV2Eh[2WubIOsJGVEPTB;MzFOwG0v MUSxO|U3QDd2OB?=
human SKUT cells MnfiSpVv[3Srb36gZZN{[Xl? MoPGTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iU1vVWEBk\WyuczygSWM2OD12IN88UU4> MoPmNVc2Pjh5NEi=
human Calu1 cells NXWxcZVHTnWwY4Tpc44h[XO|YYm= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGNidHVzIHPlcIx{KGW6cILld5NqdmdiS2LBV{B4cXSqIHHjeIl3[XSrbnegcZV1[XSrb37zJIJ6KHS{eYDhckBjdHWnIHX4Z4x2e2mxbjDhd5NigSxiSVO1NF01KM7:TT6= NYDCN5FGOTd3Nki3OFg>
human LNCaP cells NGD6XoVHfW6ldHnvckBie3OjeR?= MXzJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCOTlPhVEBk\WyuczygSWM2OD14IN88UU4> MkTINVc2Pjh5NEi=
human U2OS cells Mlj5SpVv[3Srb36gZZN{[Xl? MonZTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iVULPV{Bk\WyuczygSWM2OD14IN88UU4> NXHvW2FDOTd3Nki3OFg>
human TC32 cells MWHGeY5kfGmxbjDhd5NigQ>? NEnsVIlKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDUR|MzKGOnbHzz NH\PRnQyPzV4OEe0PC=>
human SK-N-MC cells MmjJSpVv[3Srb36gZZN{[Xl? M{nZV2lv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIGPLMW4uVUNiY3XscJMtKEWFNUC9NVAh|ryPLh?= NFX3c5oyPzV4OEe0PC=>
human U937 cells NID1W21HfW6ldHnvckBie3OjeR?= MYnJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCXOUO3JINmdGy|LDDFR|UxRTFyIN88UU4> NGrhdVkyPzV4OEe0PC=>
human TC71 cells MVHGeY5kfGmxbjDhd5NigQ>? MnT6TY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iVFO3NUBk\WyuczygSWM2OD1zMDFOwG0v MWqxO|U3QDd2OB?=
human BJ cells M{XSVGZ2dmO2aX;uJIF{e2G7 M{OxcGlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJHRGWlRiZYjwdoV{e2mwZzDoeY1idiCESjDj[YxteyxiRVO1NF0yOCEQvF2u M2X6d|E4PTZ6N{S4
human EWS502 cells MY\GeY5kfGmxbjDhd5NigQ>? MmXTTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iRWfTOVAzKGOnbHzzMEBGSzVyPUGwJO69VS5? MnT4NVc2Pjh5NEi=
human Hs51.T cells NUfUUXJ{TnWwY4Tpc44h[XO|YYm= M1zrPGlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFjzOVEvXCClZXzsd{whTUN3ME2xNkDPxE1w M3;KU|E4PTZ6N{S4
human Hs925.T cells Mn2ySpVv[3Srb36gZZN{[Xl? NY\PVINtUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gTJM6OjVwVDDj[YxteyxiRVO1NF0yPyEQvF2u NXi0NI1iOTd3Nki3OFg>
human HOS cells NHq2T5NHfW6ldHnvckBie3OjeR?= NWPi[phMUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gTG9UKGOnbHzzJEwhTUN3ME2xO{DPxE1w Mk\FNVc2Pjh5NEi=
human MX2 cells NE\wU4tHfW6ldHnvckBie3OjeR?= NUDLcYcxUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gUXgzKGOnbHzzMEBGSzVyPUG4JO69VS5? NV\jZnZNOTd3Nki3OFg>
human A673 cells NIn4SXNHfW6ldHnvckBie3OjeR?= NWPzemt4UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gRVY4OyClZXzsd{whTUN3ME2zNEDPxE1w NEfYV2MyPzV4OEe0PC=>
human BJ cells NFXYZm5HfW6ldHnvckBie3OjeR?= NGXxSGxKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDCTkBk\WyuczDlfJBz\XO|aX7nJHRGWlRuIFzUMEBUXCCjbnSgVmFUKEdzMm[gcZV1[W62IHflcoV{KGmwIIDy[ZNmdmOnIH;mJHUxOTJ4IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCvZYToc4QtKEmFNUC9N|EvOiEQvF2u MVexO|U3QDd2OB?=
human BJ cells NYTrfm92TnWwY4Tpc44h[XO|YYm= M3[4cFkh|ryP NVziOJBkUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gRmoh[2WubIOg[ZhxemW|c3nu[{BVTVKWLDDMWEwhW1RiYX7kJHJCWyCJMULWJI12fGGwdDDn[Y5meyClZXzsd{BifCB7IIXNMi=> NYL1RWo1OTd3Nki3OFg>
human BJ cells NXj6S4tVTnWwY4Tpc44h[XO|YYm= NWTzWnBTPC54IN88US=> NXjqOmJEUW6lcnXhd4UhcW5iaX70doFk\WyudXzhdkBwgGmmYYTpeoUhe3CnY3nld{BqdiCqdX3hckBDUiClZXzsd{BmgHC{ZYPzbY5oKFSHUmSsJGxVNCCVVDDhcoQhWkGVIFexNnYhdXW2YX70JIdmdmW|IHPlcIx{KGG2IESuOkB2VQ>? M4jZZ|E4PTZ6N{S4
human BJeLR cells M3HPPWN6fG:2b4jpZ:Kh[XO|YYm= Mnz4NVAh|ryP M13nO|EzKGh? MoDUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRmpmVFJiY3XscJMh\XiycnXzd4lv\yCUQWOgS|EzXiCvdYThcpQh[XRiMUCgeW0h[XRiMUKgbJJ{KGK7IITyfZBidiCkbIXlJJN1[WmwaX7n NXvwe4hZOjJ6M{KzNlE>
human BJeH cells MUHGeY5kfGmxbjDhd5NigQ>? M1PGZ|YhcA>? NEKyRo1KdmS3Y4Tpc44hd2ZicnXhZ5RqfmVib4j5[4VvKHOyZXPp[ZMheHKxZIXjeIlwdiCrbjDoeY1idiCESnXIJINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJHJCWyCjZoTldkA3KGi{czDifUBFS0ZvYnHz[YQh\myxdzDjfZRwdWW2cnnjJIFv[Wy7c3nz MnvlNlI5OzJ|MkG=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
GPX4 / cleaved-PARP / cleaved-caspase3 / LC3 / p62 / LDH / HMGB1; 

PubMed: 27308510     


HL-60 and Jurkat cells were treated with erastin (5 μM) for 24 h and subjected to western blot analysis of the indicated proteins in whole cell extracts or supernatant. 

TfR1 / p-JNK / JNK / p-P38; 

PubMed: 31105999     


HL-60/NRAS (Q61L) cells were treated with erastin (5 μM) combined with SP600125 (10 μM) and SB202190 (10 μM) for 48 h. TfR1 expression and the phosphorylation of p38 (p-P38) and JNK1/2 (p-JNK1/2) were assayed by western blot. 

HSPA5 / p-EIF2AK3; 

PubMed: 28130223     


Western blot analysis indicated protein expression in PDAC cells following treatment with erastin (2.5-40 μM) for 24 hours (n=3, *p < 0.05 versus untreated group). 

GRP78; 

PubMed: 29383150     


Cells were treated with 50 μM erastin for various time(1-24 h). Whole-cell extracts were analyzed with immunoblotting assay.

27308510 31105999 28130223 29383150
Growth inhibition assay
Cell survival; 

PubMed: 29348676     


The A375 and G-361 human melanoma cells were treated with erastin (2.5-40 µM) or RSL3 (0.1-10 µM) with or without a cell death inhibitor (ferrostatin-1, 1 µM; ZVAD-FMK, 10 µM; necrosulfonamide, 0.5 µM) for 24 h. Cell death was assayed using a CCK-8 kit. Data shown represent mean ± SD from three independent experiments. ****p < 0.0001.

29348676
Immunofluorescence
HMGB1; 

PubMed: 31105999     


HL-60/NRAS (Q61L) cells were treated with erastin (5 μM) with or without Fer-1 (1 μM) pretreatment for 48 h, and then the nuclear/cytosolic HMGB1 expression was assayed by immunofluorescence(Green, HMGB1; blue, nucleus). 

31105999

Protocol

Cell Research:[1]
- Collapse
  • Cell lines: BJ-TERT/LT/ST/RASV12 cells
  • Concentrations: 5 or 10 μg/mL
  • Incubation Time: 6-11 hours
  • Method: BJ-TERT/LT/ST/RASV12 cells are seeded in 100 mm dishes and allowed to grow overnight. Cells are treated with erastin (5 or 10 μg/ml) for 6, 8, or 11 hr. A camptothecin-treated (0.4 μg/ml) control is maintained, treated at the time of seeding for 20 hours. After the treatment, cells are harvested with trypsin/EDTA and washed once with fresh medium containing serum and then twice with phosphate-buffered saline. Cells are resuspended in 1× binding buffer. 100 μL is incubated with 5 μL of Annexin V-FITC and propidium iodiode for 15 min in the dark at room temperature. Then 400 μl of the 1× binding buffer s added and the cells analyzed by flow cytometry. Data are acquired and analyzed using Cellquest software. Only viable cells that do not stain with propidium iodiode are analzyed for Annexin V-FITC staining using the FL1 channel.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 19 mg/mL (34.73 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
2.5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 547.04
Formula

C30H31ClN4O4

CAS No. 571203-78-6
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID