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Erastin

Erastin

  • CAT Number: I004132
  • CAS Number: 571203-78-6
  • Molecular Formula: C30H31ClN4O4
  • Molecular Weight: 547.1
  • Purity: ≥95%
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<p style=/line-height:25px/>Erastin is a compound that interacts with VDAC, blocked and reversed mitochondrial depolarization after microtubule destabilizers in intact cells and antagonized tubulin-induced VDAC blockage in planar bilayers.<br>IC50 Value: 0.1 uM (VDAC-2) [1]<br>Target: VDAC-2<br>Voltage-dependent anion channels are a class of porin ion channel located on the outer mitochondrial membrane. This major protein of the outer mitochondrial membrane of eukaryotes forms a voltage-dependent anion-selective channel (VDAC) that behaves as a general diffusion pore for small hydrophilic molecules. erastininduced RAS-RAF-MEK-dependent non-apoptotic cell death via VDAC2 [2].<br></p>

Catalog Number I004132
CAS Number 571203-78-6
Molecular Formula

C30H31ClN4O4

Purity 95%
Target VDAC-2
Solubility DMSO: ≤ 6.4 mg/mL (Need ultrasonic)
Storage -20°C
IC50 0.1 uM (VDAC-2) [1]
InChIKey BKQFRNYHFIQEKN-UHFFFAOYSA-N
Reference

</br>1:The Protective Role of Mitochondrial Ferritin on Erastin-Induced Ferroptosis. Wang YQ, Chang SY, Wu Q, Gou YJ, Jia L, Cui YM, Yu P, Shi ZH, Wu WS, Gao G, Chang YZ.Front Aging Neurosci. 2016 Dec 20;8:308. doi: 10.3389/fnagi.2016.00308. eCollection 2016. PMID: 28066232 Free PMC Article</br>2:RSL3 and Erastin differentially regulate redox signaling to promote Smac mimetic-induced cell death. Dächert J, Schoeneberger H, Rohde K, Fulda S.Oncotarget. 2016 Sep 27;7(39):63779-63792. doi: 10.18632/oncotarget.11687. PMID: 27588473 Free PMC Article</br>3:The ferroptosis inducer erastin enhances sensitivity of acute myeloid leukemia cells to chemotherapeutic agents. Yu Y, Xie Y, Cao L, Yang L, Yang M, Lotze MT, Zeh HJ, Kang R, Tang D.Mol Cell Oncol. 2015 May 26;2(4):e1054549. doi: 10.1080/23723556.2015.1054549. eCollection 2015 Oct-Dec. PMID: 27308510 Free PMC Article</br>4:Conjugation to the sigma-2 ligand SV119 overcomes uptake blockade and converts dm-Erastin into a potent pancreatic cancer therapeutic. Ohman KA, Hashim YM, Vangveravong S, Nywening TM, Cullinan DR, Goedegebuure SP, Liu J, Van Tine BA, Tiriac H, Tuveson DA, DeNardo DG, Spitzer D, Mach RH, Hawkins WG.Oncotarget. 2016 Jun 7;7(23):33529-41. doi: 10.18632/oncotarget.9551. PMID: 27244881 Free PMC Article</br>5:Erastin Disrupts Mitochondrial Permeability Transition Pore (mPTP) and Induces Apoptotic Death of Colorectal Cancer Cells. Huo H, Zhou Z, Qin J, Liu W, Wang B, Gu Y.PLoS One. 2016 May 12;11(5):e0154605. doi: 10.1371/journal.pone.0154605. eCollection 2016. PMID: 27171435 Free PMC Article</br>6:Heme oxygenase-1 accelerates erastin-induced ferroptotic cell death. Kwon MY, Park E, Lee SJ, Chung SW.Oncotarget. 2015 Sep 15;6(27):24393-403. PMID: 26405158 Free PMC Article</br>7:Erastin sensitizes glioblastoma cells to temozolomide by restraining xCT and cystathionine-γ-lyase function. Chen L, Li X, Liu L, Yu B, Xue Y, Liu Y.Oncol Rep. 2015 Mar;33(3):1465-74. doi: 10.3892/or.2015.3712. Epub 2015 Jan 13. PMID: 25585997 </br>8:Voltage-dependent anion channels modulate mitochondrial metabolism in cancer cells: regulation by free tubulin and erastin. Maldonado EN, Sheldon KL, DeHart DN, Patnaik J, Manevich Y, Townsend DM, Bezrukov SM, Rostovtseva TK, Lemasters JJ.J Biol Chem. 2013 Apr 26;288(17):11920-9. doi: 10.1074/jbc.M112.433847. Epub 2013 Mar 7. PMID: 23471966 Free PMC Article

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