Erastin

For research use only.

Catalog No.S7242

128 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 128 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 M3X0XmZ2dmO2aX;uJIF{e2G7 NVXCT3NqPiCq NUT5bJNpUW6mdXP0bY9vKG:oIILlZYN1cX[nIH;4fYdmdiC|cHXjbYV{KHC{b3T1Z5Rqd25iaX6gbJVu[W5iQlrlTEBk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBTSVNiYX\0[ZIhPiCqcoOgZpkhTEOILXLhd4VlKG[ub4egZ5l1d22ndILpZ{BidmGueYPpdy=> MmXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6M{KzNlEoRjJ{OEOyN|IyRC:jPh?=
human BJeLR cells MoPVR5l1d3SxeHnjxsBie3OjeR?= MWixNEDPxE1? NEnwPYkyOiCq M4CxdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJL\UyUIHPlcIx{KGW6cILld5NqdmdiUlHTJGcyOlZibYX0ZY51KGG2IEGwJJVOKGG2IEGyJIhzeyCkeTD0dplx[W5iYnz1[UB{fGGrbnnu[y=> NHTZN2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkizNlMzOSd-MkK4N|I{OjF:L3G+
human BJ cells NH7NNZhHfW6ldHnvckBie3OjeR?= NXL2emxjPC54IN88US=> NW\BVVF[UW6lcnXhd4UhcW5iaX70doFk\WyudXzhdkBwgGmmYYTpeoUhe3CnY3nld{BqdiCqdX3hckBDUiClZXzsd{BmgHC{ZYPzbY5oKFSHUmSsJGxVNCCVVDDhcoQhWkGVIFexNnYhdXW2YX70JIdmdmW|IHPlcIx{KGG2IESuOkB2VQ>? M3XCdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human BJ cells MnPwSpVv[3Srb36gZZN{[Xl? MljoPUDPxE1? NEi2OXlKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDCTkBk\WyuczDlfJBz\XO|aX7nJHRGWlRuIFzUMEBUXCCjbnSgVmFUKEdzMm[gcZV1[W62IHflcoV{KGOnbHzzJIF1KDlidV2u NIjYTG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human BJ cells M3LOPGZ2dmO2aX;uJIF{e2G7 NWrNOpg2UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gRmoh[2WubIOg[ZhxemW|c3nu[{BVTVKWLDDMWEwhW1RiYX7kJHJCWyCJMULWJI12fGGwdDDn[Y5meyCrbjDwdoV{\W6lZTDv[kBWODF{NjDifUB1enmyYX6gZox2\SCneHPseZNqd25ibXX0bI9lNCCLQ{WwQVMyNjJizszNMi=> Mm\6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human A673 cells NVSwXFBPTnWwY4Tpc44h[XO|YYm= NXfsPHRHUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gRVY4OyClZXzsd{whTUN3ME2zNEDPxE1w MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human MX2 cells NYLyN4hXTnWwY4Tpc44h[XO|YYm= NWfzR3B4UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gUXgzKGOnbHzzMEBGSzVyPUG4JO69VS5? NGrLXIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human HOS cells NHXmTXBHfW6ldHnvckBie3OjeR?= NGq5WIZKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDIU3Mh[2WubIOgMEBGSzVyPUG3JO69VS5? NW\ufWRMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human Hs925.T cells MlPvSpVv[3Srb36gZZN{[Xl? NXjibWNZUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gTJM6OjVwVDDj[YxteyxiRVO1NF0yPyEQvF2u MoDyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Nki3OFgoRjF5NU[4O|Q5RC:jPh?=
human Hs51.T cells NF7Cb4NHfW6ldHnvckBie3OjeR?= NY\QXYdvUW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigbY4hcHWvYX6gTJM2OS6WIHPlcIx{NCCHQ{WwQVEzKM7:TT6= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human EWS502 cells NXfHZ2dWTnWwY4Tpc44h[XO|YYm= M4q4emlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFXXV|UxOiClZXzsd{whTUN3ME2xNEDPxE1w NGXzSZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human BJ cells NFfsbHdHfW6ldHnvckBie3OjeR?= MVfJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDUSXJVKGW6cILld5NqdmdiaIXtZY4hSkpiY3XscJMtKEWFNUC9NVAh|ryPLh?= NYjoSnE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human TC71 cells MXLGeY5kfGmxbjDhd5NigQ>? MoX4TY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iVFO3NUBk\WyuczygSWM2OD1zMDFOwG0v NWexNY54RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human U937 cells NX7mZWx5TnWwY4Tpc44h[XO|YYm= MmLITY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iVUmzO{Bk\WyuczygSWM2OD1zMDFOwG0v NELhZo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human SK-N-MC cells M4m1UWZ2dmO2aX;uJIF{e2G7 NEj4ZpJKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDTT{1PNU2FIHPlcIx{NCCHQ{WwQVExKM7:TT6= M3SyPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human TC32 cells NELufmVHfW6ldHnvckBie3OjeR?= Mn7NTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iVFOzNkBk\Wyucx?= M3W4T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human U2OS cells NGm2Xo9HfW6ldHnvckBie3OjeR?= MlzNTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iVULPV{Bk\WyuczygSWM2OD14IN88UU4> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human LNCaP cells MXvGeY5kfGmxbjDhd5NigQ>? M1ztOWlv\HWldHnvckBw\iClZXzsJIRm[XSqIHnuJIh2dWGwIFzOR4FRKGOnbHzzMEBGSzVyPU[g{txONg>? NFG2bXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human Calu1 cells MYnGeY5kfGmxbjDhd5NigQ>? MoiwTY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3MTDj[YxteyCneIDy[ZN{cW6pIFvSRXMhf2m2aDDhZ5RqfmG2aX7nJI12fGG2aX;ud{BjgSC2conwZY4h[my3ZTDlfINtfXOrb36gZZN{[XluIFnDOVA:PCEQvF2u NVfJN|RlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1Olg4PDhpPkG3OVY5PzR6PD;hQi=>
human SKUT cells MVnGeY5kfGmxbjDhd5NigQ>? NI\kTodKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDTT3VVKGOnbHzzMEBGSzVyPUSg{txONg>? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human MES-SA cells NWDBRW96TnWwY4Tpc44h[XO|YYm= MXXJcoR2[3Srb36gc4Yh[2WubDDk[YF1cCCrbjDoeY1idiCPRWOtV2Eh[2WubIOsJGVEPTB;MzFOwG0v NF3PO4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human SVR cells MlLlSpVv[3Srb36gZZN{[Xl? NHHORotKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDTWnIh[2WubIOsJGVEPTB;Mj61JO69VS5? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4OEe0PEc,OTd3Nki3OFg9N2F-
human HT1080 cells NWnPNmFkTnWwY4Tpc44h[XO|YYm= NGnSe2ZKdmS3Y4Tpc44hd2ZiY3XscEBl\WG2aDDpckBpfW2jbjDIWFExQDBiY3XscJMhcW5icILld4Vv[2Vib3[gVGQuQThyNUmgZpkhfHK7cHHuJIJtfWViZYjjcJV{cW:wIH3leIhw\CxiSVO1NF0yKM7:TT6= NEHwVWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human BJ cells MX3GeY5kfGmxbjDhd5NigQ>? Mn:wTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iQlqgZ4VtdHNiZYjwdoV{e2mwZzDUSXJVNCCOVDygV3Qh[W6mIGLBV{BIOTKYIH31eIFvfCCpZX7ld{Bk\WyuczDpckBxemW|ZX7j[UBw\iCSRD25PFA2QSCkeTD0dplx[W5iYnz1[UBmgGOudYPpc44hdWW2aH;kMEBKSzVyPUCuPUDPxE1w M13y[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[4O|Q5Lz5zN{W2PFc1QDxxYU6=
human HeLa cells MlLaSpVv[3Srb36gZZN{[Xl? MkHoTY5lfWO2aX;uJI9nKGOnbHyg[IVifGhiaX6gbJVu[W5iSHXMZUBk\WyuczygSWM2OD1yLk[g{txONg>? NFXBfos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{W2PFc1QCd-MUe1Olg4PDh:L3G+
human CCF-STTG1 cells NVzR[Y52TnWwY4Tpc44h[XO|YYm= M3\VNGlvcGmkaYTpc44hd2ZiWHP0JIlvKGi3bXHuJGNETi2VVGTHNUBk\WyuczDhd5Nme3OnZDDhd{BodHW2YX3heIUhemWuZXHz[UBi\nSncjCyJIhzeyCkeTDmcJVwem:vZYTyfUwhUUN3ME2wMlIh|ryPLh?= M2HnOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkOxNVU3Lz5{NkKzNVE2PjxxYU6=

... 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 (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