Erastin - CAS 571203-78-6
Catalog number: 571203-78-6
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Targets:
VDAC
Description:
Erastin is an antitumor agent selective for tumor cells bearing oncogenic RAS (i.e. HRAS, KRAS). Erastin produces non-apoptotic tumor cell death by altering mitochondrial voltage-dependent anion channel (VDAC) gating allowing cations to enter mitochondria and leading to release of oxidative species causing oxidative cell death. Erastin blocks and reverses mitochondrial depolarization after microtubule destabilizers in intact cells and antagonized tubulin-induced VDAC blockage in planar bilayers. Reversal of tubulin-VDAC interaction by erastin antagonizes Warburg metabolism and restores oxidative mitochondrial metabolism.
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Purity:
0.98
Appearance:
white solid powder
Synonyms:
Erastin
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1.Heme oxygenase-1 accelerates erastin-induced ferroptotic cell death.
Kwon MY1, Park E1, Lee SJ2, Chung SW1. Oncotarget. 2015 Sep 15;6(27):24393-403.
The oncogenic RAS-selective lethal small molecule Erastin triggers a unique iron-dependent form of nonapoptotic cell death termed ferroptosis. Ferroptosis is dependent upon the production of intracellular iron-dependent reactive oxygen species (ROS), but not other metals. However, key regulators remain unknown. The heme oxygenase (HO) is a major intracellular source of iron. In this study, the role of heme oxygenase in Erastin-triggered ferroptotic cancer cell death has been investigated. Zinc protoporphyrin IX (ZnPP), a HO-1 inhibitor, prevented Erastin-triggered ferroptotic cancer cell death. Furthermore, Erastin induced the protein and mRNA levels of HO-1 in HT-1080 fibrosarcoma cells. HO-1+/+ and HO-1-/- fibroblast, HO-1 overexpression, and chycloheximide-treated experiments revealed that the expression of HO-1 has a decisive effects in Erastin-triggered cell death. Hemin and CO-releasing molecules (CORM) promote Erastin-induced ferroptotic cell death, not by biliverdin and bilirubin.
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CAS 571203-78-6 Erastin

Erastin
(CAS: 571203-78-6)

Erastin is an antitumor agent selective for tumor cells bearing oncogenic RAS (i.e. HRAS, KRAS). Erastin produces non-apoptotic tumor cell death by altering mit...

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CAS 571203-78-6 Erastin

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