Erastin

For research use only.

Catalog No.S7242

101 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 101 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 BJeH cells NIDtPJpHfW6ldHnvckBie3OjeR?= NIraNnc3KGh? MYjJcoR2[3Srb36gc4YhemWjY4TpeoUhd3i7Z3XuJJNx\WOrZYOgdJJw\HWldHnvckBqdiCqdX3hckBDUmWKIHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIGLBV{Bi\nSncjC2JIhzeyCkeTDER2Yu[mG|ZXSg[oxwfyCleYTvcYV1emmlIHHuZYx6e2m| NYXCdG8zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4N|I{OjFpPkKyPFMzOzJzPD;hQi=>
human BJeLR cells NYHmS3QyS3m2b4TvfIlkyqCjc4PhfS=> MWKxNEDPxE1? M1XNe|EzKGh? NF3WVIVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDUmWOUjDj[YxteyCneIDy[ZN{cW6pIGLBV{BIOTKYIH31eIFvfCCjdDCxNEB2VSCjdDCxNkBpenNiYomgeJJ6eGGwIHLseYUhe3SjaX7pcoc> M3mzfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OEOyN|IyLz5{MkizNlMzOTxxYU6=
human BJ cells MkDHSpVv[3Srb36gZZN{[Xl? NXn3dZpRPC54IN88US=> MlHqTY5kemWjc3WgbY4hcW62cnHj[YxtfWyjcjDvfIll[XSrdnWgd5Bm[2mnczDpckBpfW2jbjDCTkBk\WyuczDlfJBz\XO|aX7nJHRGWlRuIFzUMEBUXCCjbnSgVmFUKEdzMm[gcZV1[W62IHflcoV{KGOnbHzzJIF1KDRwNjD1US=> M{\Ze|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human BJ cells M4jScWZ2dmO2aX;uJIF{e2G7 M3fabFkh|ryP M2D0[Wlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFLKJINmdGy|IHX4dJJme3OrbnegWGVTXCxiTGSsJHNVKGGwZDDSRXMhTzF{VjDteZRidnRiZ3Xu[ZMh[2WubIOgZZQhQSC3TT6= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human BJ cells MUXGeY5kfGmxbjDhd5NigQ>? MkKxTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iQlqgZ4VtdHNiZYjwdoV{e2mwZzDUSXJVNCCOVDygV3Qh[W6mIGLBV{BIOTKYIH31eIFvfCCpZX7ld{BqdiCycnXz[Y5k\SCxZjDVNFEzPiCkeTD0dplx[W5iYnz1[UBmgGOudYPpc44hdWW2aH;kMEBKSzVyPUOxMlIh|ryPLh?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human A673 cells NYfmW2h4TnWwY4Tpc44h[XO|YYm= NGnGTpRKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDBOlc{KGOnbHzzMEBGSzVyPUOwJO69VS5? M{\1[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human MX2 cells M3zIeWZ2dmO2aX;uJIF{e2G7 MmrNTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iTWiyJINmdGy|LDDFR|UxRTF6IN88UU4> MmDRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human HOS cells MV7GeY5kfGmxbjDhd5NigQ>? MVrJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCKT2OgZ4VtdHNiLDDFR|UxRTF5IN88UU4> NVuyfGR7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human Hs925.T cells MYHGeY5kfGmxbjDhd5NigQ>? MlS4TY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iSIO5NlUvXCClZXzsd{whTUN3ME2xO{DPxE1w MlzhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human Hs51.T cells MmjBSpVv[3Srb36gZZN{[Xl? NEXMVXRKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDId|UyNlRiY3XscJMtKEWFNUC9NVIh|ryPLh?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human EWS502 cells NUTMeZZkTnWwY4Tpc44h[XO|YYm= MVTJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCHV2O1NFIh[2WubIOsJGVEPTB;MUCg{txONg>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human BJ cells NVjYXXY6TnWwY4Tpc44h[XO|YYm= NGOzSGVKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBVTVKWIHX4dJJme3OrbnegbJVu[W5iQlqgZ4VtdHNuIFXDOVA:OTBizszNMi=> NVTvVnpmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human TC71 cells MkHvSpVv[3Srb36gZZN{[Xl? M1yxRWlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIGTDO|Eh[2WubIOsJGVEPTB;MUCg{txONg>? NV3Ie5dnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human U937 cells NV3ZNWNMTnWwY4Tpc44h[XO|YYm= MnnCTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iVUmzO{Bk\WyuczygSWM2OD1zMDFOwG0v MlS4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human SK-N-MC cells M3TOfmZ2dmO2aX;uJIF{e2G7 M33uWWlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIGPLMW4uVUNiY3XscJMtKEWFNUC9NVAh|ryPLh?= NELsblE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human TC32 cells MW\GeY5kfGmxbjDhd5NigQ>? MnroTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iVFOzNkBk\Wyucx?= NIOzVFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human U2OS cells MlnpSpVv[3Srb36gZZN{[Xl? NGK4c5lKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDVNm9UKGOnbHzzMEBGSzVyPU[g{txONg>? NF2w[VU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human LNCaP cells NWD6WWlRTnWwY4Tpc44h[XO|YYm= Ml7STY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iTF7DZXAh[2WubIOsJGVEPTB;NjFOwG0v NGXTbHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human Calu1 cells NUnP[Gp1TnWwY4Tpc44h[XO|YYm= NU[z[Ih1UW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1NUBk\WyuczDlfJBz\XO|aX7nJGtTSVNid3n0bEBi[3SrdnH0bY5oKG23dHH0bY9veyCkeTD0dplx[W5iYnz1[UBmgGOudYPpc44h[XO|YYmsJGlEPTB;NDFOwG0v M2LP[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human SKUT cells NXTnclhLTnWwY4Tpc44h[XO|YYm= MmOwTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iU1vVWEBk\WyuczygSWM2OD12IN88UU4> NYj1WnpGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human MES-SA cells M37k[GZ2dmO2aX;uJIF{e2G7 NWDHe4hoUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gUWVUNVODIHPlcIx{NCCHQ{WwQVMh|ryPLh?= NInOVoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human SVR cells M4fX[2Z2dmO2aX;uJIF{e2G7 NXPvSIhxUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gV3ZTKGOnbHzzMEBGSzVyPUKuOUDPxE1w M{SzN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human HT1080 cells MWfGeY5kfGmxbjDhd5NigQ>? NVnGXGVqUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gTHQyODhyIHPlcIx{KGmwIIDy[ZNmdmOnIH;mJHBFNTl6MEW5JIJ6KHS{eYDhckBjdHWnIHX4Z4x2e2mxbjDt[ZRpd2RuIFnDOVA:OSEQvF2u Ml3DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human BJ cells MlHWSpVv[3Srb36gZZN{[Xl? MmL2TY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iQlqgZ4VtdHNiZYjwdoV{e2mwZzDUSXJVNCCOVDygV3Qh[W6mIGLBV{BIOTKYIH31eIFvfCCpZX7ld{Bk\WyuczDpckBxemW|ZX7j[UBw\iCSRD25PFA2QSCkeTD0dplx[W5iYnz1[UBmgGOudYPpc44hdWW2aH;kMEBKSzVyPUCuPUDPxE1w Mmf5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human HeLa cells M1TE[mZ2dmO2aX;uJIF{e2G7 NIXENYVKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDI[WxiKGOnbHzzMEBGSzVyPUCuOkDPxE1w MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human CCF-STTG1 cells NED5TpZHfW6ldHnvckBie3OjeR?= M1H5[mlvcGmkaYTpc44hd2ZiWHP0JIlvKGi3bXHuJGNETi2VVGTHNUBk\WyuczDhd5Nme3OnZDDhd{BodHW2YX3heIUhemWuZXHz[UBi\nSncjCyJIhzeyCkeTDmcJVwem:vZYTyfUwhUUN3ME2wMlIh|ryPLh?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ|MUG1Okc,OjZ{M{GxOVY9N2F-

... 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