Erastin

For research use only.

Catalog No.S7242

90 publications

Erastin Chemical Structure

CAS No. 571203-78-6

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

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Selleck's Erastin has been cited by 90 publications

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Choose Selective Ferroptosis Inhibitors

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 BJeH cells MVHGeY5kfGmxbjDhd5NigQ>? NWDHd|lIPiCq M{LzRmlv\HWldHnvckBw\iC{ZXHjeIl3\SCxeInn[Y4he3CnY3nld{Bxem:mdXP0bY9vKGmwIHj1cYFvKEKMZVigZ4VtdHNiZYjwdoV{e2mwZzD3bYxlKHS7cHWgVmFUKGGodHXyJFYhcHK|IHL5JGRETi2kYYPl[EBndG:5IHP5eI9u\XS{aXOgZY5idHm|aYO= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjh|MkOyNUc,OjJ6M{KzNlE9N2F-
human BJeLR cells NV\TSlBTS3m2b4TvfIlkyqCjc4PhfS=> M{[yOVExKM7:TR?= NXLn[3ZwOTJiaB?= MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCToVNWiClZXzsd{BmgHC{ZYPzbY5oKFKDUzDHNVJXKG23dHHueEBifCBzMDD1UUBifCBzMjDodpMh[nlidIL5dIFvKGKudXWgd5RicW6rbne= NFj5T2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkizNlMzOSd-MkK4N|I{OjF:L3G+
human BJ cells MmjCSpVv[3Srb36gZZN{[Xl? NVu5fW9LPC54IN88US=> MWfJcoNz\WG|ZTDpckBqdnS{YXPlcIx2dGG{IH;4bYRifGm4ZTDzdIVkcWW|IHnuJIh2dWGwIFLKJINmdGy|IHX4dJJme3OrbnegWGVTXCxiTGSsJHNVKGGwZDDSRXMhTzF{VjDteZRidnRiZ3Xu[ZMh[2WubIOgZZQhPC54IIXN MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human BJ cells Ml2zSpVv[3Srb36gZZN{[Xl? M1HN[lkh|ryP MYPJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCESjDj[YxteyCneIDy[ZN{cW6pIGTFVnQtKEyWLDDTWEBidmRiUlHTJGcyOlZibYX0ZY51KGenbnXzJINmdGy|IHH0JFkhfU1w MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human BJ cells MW\GeY5kfGmxbjDhd5NigQ>? NUL2U4dEUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gRmoh[2WubIOg[ZhxemW|c3nu[{BVTVKWLDDMWEwhW1RiYX7kJHJCWyCJMULWJI12fGGwdDDn[Y5meyCrbjDwdoV{\W6lZTDv[kBWODF{NjDifUB1enmyYX6gZox2\SCneHPseZNqd25ibXX0bI9lNCCLQ{WwQVMyNjJizszNMi=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human A673 cells NFnpOpNHfW6ldHnvckBie3OjeR?= M{jOZmlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFG2O|Mh[2WubIOsJGVEPTB;M{Cg{txONg>? M2\PcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human MX2 cells NXzFZpFFTnWwY4Tpc44h[XO|YYm= NHzUVJFKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDNXFIh[2WubIOsJGVEPTB;MUig{txONg>? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human HOS cells M1n2d2Z2dmO2aX;uJIF{e2G7 M2X6Z2lv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFjPV{Bk\WyuczCsJGVEPTB;MUeg{txONg>? NVT3cINLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human Hs925.T cells MXrGeY5kfGmxbjDhd5NigQ>? MmDCTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iSIO5NlUvXCClZXzsd{whTUN3ME2xO{DPxE1w MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human Hs51.T cells MlXFSpVv[3Srb36gZZN{[Xl? MYjJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCKc{WxMnQh[2WubIOsJGVEPTB;MUKg{txONg>? M3rtbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human EWS502 cells M{\iXWZ2dmO2aX;uJIF{e2G7 MlK0TY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iRWfTOVAzKGOnbHzzMEBGSzVyPUGwJO69VS5? NEjPN4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human BJ cells MX7GeY5kfGmxbjDhd5NigQ>? M{K2PGlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJHRGWlRiZYjwdoV{e2mwZzDoeY1idiCESjDj[YxteyxiRVO1NF0yOCEQvF2u M3SyfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human TC71 cells MY\GeY5kfGmxbjDhd5NigQ>? MYLJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCWQ{exJINmdGy|LDDFR|UxRTFyIN88UU4> NFz4WGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human U937 cells M4LCXmZ2dmO2aX;uJIF{e2G7 M1HnT2lv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIGW5N|ch[2WubIOsJGVEPTB;MUCg{txONg>? NUXjfXR5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human SK-N-MC cells MWjGeY5kfGmxbjDhd5NigQ>? NXrhRXZ{UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gV2suVi2PQzDj[YxteyxiRVO1NF0yOCEQvF2u NH6zb4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human TC32 cells MUHGeY5kfGmxbjDhd5NigQ>? M3;afGlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIGTDN|Ih[2WubIO= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human U2OS cells M3jhXGZ2dmO2aX;uJIF{e2G7 MknyTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iVULPV{Bk\WyuczygSWM2OD14IN88UU4> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human LNCaP cells NULiVnBlTnWwY4Tpc44h[XO|YYm= MnnwTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iTF7DZXAh[2WubIOsJGVEPTB;NjFOwG0v NHXuSVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human Calu1 cells MlrsSpVv[3Srb36gZZN{[Xl? MojjTY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3MTDj[YxteyCneIDy[ZN{cW6pIFvSRXMhf2m2aDDhZ5RqfmG2aX7nJI12fGG2aX;ud{BjgSC2conwZY4h[my3ZTDlfINtfXOrb36gZZN{[XluIFnDOVA:PCEQvF2u MnW5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human SKUT cells MUHGeY5kfGmxbjDhd5NigQ>? NXfUNI9XUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gV2tWXCClZXzsd{whTUN3ME20JO69VS5? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human MES-SA cells MXXGeY5kfGmxbjDhd5NigQ>? NYDRSWNpUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gUWVUNVODIHPlcIx{NCCHQ{WwQVMh|ryPLh?= MlvMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human SVR cells MnvtSpVv[3Srb36gZZN{[Xl? M4DJTmlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIGPWVkBk\WyuczygSWM2OD1{LkWg{txONg>? M33oZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human HT1080 cells MXrGeY5kfGmxbjDhd5NigQ>? M3PNXWlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFjUNVA5OCClZXzsd{BqdiCycnXz[Y5k\SCxZjDQSE06QDB3OTDifUB1enmyYX6gZox2\SCneHPseZNqd25ibXX0bI9lNCCLQ{WwQVEh|ryPLh?= M{H3O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human BJ cells M4raOWZ2dmO2aX;uJIF{e2G7 NW[4PZB4UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gRmoh[2WubIOg[ZhxemW|c3nu[{BVTVKWLDDMWEwhW1RiYX7kJHJCWyCJMULWJI12fGGwdDDn[Y5meyClZXzsd{BqdiCycnXz[Y5k\SCxZjDQSE06QDB3OTDifUB1enmyYX6gZox2\SCneHPseZNqd25ibXX0bI9lNCCLQ{WwQVAvQSEQvF2u M2T1SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human HeLa cells NUTub4N1TnWwY4Tpc44h[XO|YYm= MljkTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iSHXMZUBk\WyuczygSWM2OD1yLk[g{txONg>? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human CCF-STTG1 cells M2jjZmZ2dmO2aX;uJIF{e2G7 NXrkeHd2UW6qaXLpeIlwdiCxZjDYZ5QhcW5iaIXtZY4hS0OILWPUWGcyKGOnbHzzJIF{e2W|c3XkJIF{KGeudYThcYF1\SC{ZXzlZZNmKGGodHXyJFIhcHK|IHL5JIZtfW:{b33leJJ6NCCLQ{WwQVAvOiEQvF2u NFTZUZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkKzNVE2Pid-Mk[yN|EyPTZ:L3G+

... 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+40%PEG 300+5%Tween80+ddH2O
For best results, use promptly after mixing.
1.75mg/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 3 years -20°C powder
1 month -80°C in solvent
Synonyms N/A
Smiles CCOC1=CC=CC=C1N2C(=O)C3=CC=CC=C3N=C2C(C)N4CCN(CC4)C(=O)COC5=CC=C(C=C5)Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID