Erastin

For research use only.

Catalog No.S7242

142 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. Solutions of Erastin are best fresh-prepared.

Selleck's Erastin has been cited by 142 publications

Purity & Quality Control

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. Solutions of Erastin are best fresh-prepared.
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 NVPPV21YTnWwY4Tpc44h[XO|YYm= NYq4e5BrPiCq NVPrOZRDUW6mdXP0bY9vKG:oIILlZYN1cX[nIH;4fYdmdiC|cHXjbYV{KHC{b3T1Z5Rqd25iaX6gbJVu[W5iQlrlTEBk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBTSVNiYX\0[ZIhPiCqcoOgZpkhTEOILXLhd4VlKG[ub4egZ5l1d22ndILpZ{BidmGueYPpdy=> NX[wRXk6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4N|I{OjFpPkKyPFMzOzJzPD;hQi=>
human BJeLR cells M{PRW2N6fG:2b4jpZ:Kh[XO|YYm= NEjjOocyOCEQvF2= M{T1OVEzKGh? MmHCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRmpmVFJiY3XscJMh\XiycnXzd4lv\yCUQWOgS|EzXiCvdYThcpQh[XRiMUCgeW0h[XRiMUKgbJJ{KGK7IITyfZBidiCkbIXlJJN1[WmwaX7n NGfESZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkizNlMzOSd-MkK4N|I{OjF:L3G+
human BJ cells MnHoSpVv[3Srb36gZZN{[Xl? MmD0OE43KM7:TR?= NFXZUppKdmO{ZXHz[UBqdiCrboTyZYNmdGy3bHHyJI95cWSjdHn2[UB{eGWlaXXzJIlvKGi3bXHuJGJLKGOnbHzzJIV5eHKnc4PpcochXEWUVDygUHQtKFOWIHHu[EBTSVNiR{GyWkBufXSjboSg[4Vv\XNiY3XscJMh[XRiND62JJVO MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human BJ cells NGj5RmlHfW6ldHnvckBie3OjeR?= NYHreGRDQSEQvF2= MknrTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iQlqgZ4VtdHNiZYjwdoV{e2mwZzDUSXJVNCCOVDygV3Qh[W6mIGLBV{BIOTKYIH31eIFvfCCpZX7ld{Bk\WyuczDheEA6KHWPLh?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human BJ cells MkTTSpVv[3Srb36gZZN{[Xl? NHTOVodKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDCTkBk\WyuczDlfJBz\XO|aX7nJHRGWlRuIFzUMEBUXCCjbnSgVmFUKEdzMm[gcZV1[W62IHflcoV{KGmwIIDy[ZNmdmOnIH;mJHUxOTJ4IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCvZYToc4QtKEmFNUC9N|EvOiEQvF2u NHGyZZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human A673 cells NEjTSWJHfW6ldHnvckBie3OjeR?= M4fpTmlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFG2O|Mh[2WubIOsJGVEPTB;M{Cg{txONg>? Mm[5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human MX2 cells MXvGeY5kfGmxbjDhd5NigQ>? MkfyTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iTWiyJINmdGy|LDDFR|UxRTF6IN88UU4> M3Xle|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human HOS cells M3\BfmZ2dmO2aX;uJIF{e2G7 NVTsbGM{UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gTG9UKGOnbHzzJEwhTUN3ME2xO{DPxE1w MlX2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human Hs925.T cells NXy3[4JHTnWwY4Tpc44h[XO|YYm= MoiyTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iSIO5NlUvXCClZXzsd{whTUN3ME2xO{DPxE1w NYq1SZdJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human Hs51.T cells NH75fVdHfW6ldHnvckBie3OjeR?= NUG2WmxFUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gTJM2OS6WIHPlcIx{NCCHQ{WwQVEzKM7:TT6= NYjPb2R6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human EWS502 cells NHvVTndHfW6ldHnvckBie3OjeR?= NWLHV4U6UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gSXdUPTB{IHPlcIx{NCCHQ{WwQVExKM7:TT6= NUPXNFRLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human BJ cells MXXGeY5kfGmxbjDhd5NigQ>? MnHKTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gWGVTXCCneIDy[ZN{cW6pIHj1cYFvKEKMIHPlcIx{NCCHQ{WwQVExKM7:TT6= NEDOW4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human TC71 cells MkXkSpVv[3Srb36gZZN{[Xl? M4n5VGlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIGTDO|Eh[2WubIOsJGVEPTB;MUCg{txONg>? NGXDRXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human U937 cells M{ThVmZ2dmO2aX;uJIF{e2G7 NH76R3RKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDVPVM4KGOnbHzzMEBGSzVyPUGwJO69VS5? M37VblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human SK-N-MC cells Mmj1SpVv[3Srb36gZZN{[Xl? MXTJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCVSz3OMW1EKGOnbHzzMEBGSzVyPUGwJO69VS5? MoDHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human TC32 cells MlnwSpVv[3Srb36gZZN{[Xl? NYXONWF7UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gWGM{OiClZXzsdy=> NHHWR3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human U2OS cells MojESpVv[3Srb36gZZN{[Xl? NH2yUmFKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDVNm9UKGOnbHzzMEBGSzVyPU[g{txONg>? M4HXXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human LNCaP cells MmrJSpVv[3Srb36gZZN{[Xl? NFz4bFRKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDMUmNiWCClZXzsd{whTUN3ME22JO69VS5? NYi4fpB7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human Calu1 cells NHjUc3pHfW6ldHnvckBie3OjeR?= MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGNidHVzIHPlcIx{KGW6cILld5NqdmdiS2LBV{B4cXSqIHHjeIl3[XSrbnegcZV1[XSrb37zJIJ6KHS{eYDhckBjdHWnIHX4Z4x2e2mxbjDhd5NigSxiSVO1NF01KM7:TT6= M4LjOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human SKUT cells MVLGeY5kfGmxbjDhd5NigQ>? Mm[xTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iU1vVWEBk\WyuczygSWM2OD12IN88UU4> M4ezfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human MES-SA cells MkDoSpVv[3Srb36gZZN{[Xl? NFv4U49KdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDNSXMuW0FiY3XscJMtKEWFNUC9N{DPxE1w M2L3[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human SVR cells NGrSUVNHfW6ldHnvckBie3OjeR?= M37nemlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIGPWVkBk\WyuczygSWM2OD1{LkWg{txONg>? NVjafIJpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human HT1080 cells MXzGeY5kfGmxbjDhd5NigQ>? Mmm2TY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iSGSxNFgxKGOnbHzzJIlvKHC{ZYPlcoNmKG:oIGDEMVk5ODV7IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCvZYToc4QtKEmFNUC9NUDPxE1w M4XVclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human BJ cells MXXGeY5kfGmxbjDhd5NigQ>? M4XaWGlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFLKJINmdGy|IHX4dJJme3OrbnegWGVTXCxiTGSsJHNVKGGwZDDSRXMhTzF{VjDteZRidnRiZ3Xu[ZMh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiUFStPVgxPTliYomgeJJ6eGGwIHLseYUh\XilbIXzbY9vKG2ndHjv[EwhUUN3ME2wMlkh|ryPLh?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human HeLa cells M3TMTGZ2dmO2aX;uJIF{e2G7 MYrJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCKZVzhJINmdGy|LDDFR|UxRTBwNjFOwG0v M{\OdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human CCF-STTG1 cells NV:wepVlTnWwY4Tpc44h[XO|YYm= MX;Jcohq[mm2aX;uJI9nKFildDDpckBpfW2jbjDDR2YuW1SWR{GgZ4VtdHNiYYPz[ZN{\WRiYYOg[4x2fGGvYYTlJJJmdGWjc3WgZYZ1\XJiMjDodpMh[nliZnz1c5JwdWW2comsJGlEPTB;MD6yJO69VS5? NGjlfGw9[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
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). 

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. 

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. 

GRP78; 

PubMed: 29383150     


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

28130223 31105999 27308510 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 warmed (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