Erastin

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0 Metric Ton	Negotiable

0 Metric Ton

Negotiable

Min.Order :0 Metric Ton
Purity: >97%

Keywords

Erastin Ferroptosis activator & VDAC modulator 571203-78-6

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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	Activity Description	PMID
human BJeH cells	Function assay		6 h	Induction of reactive oxygen species production in human BJeH cells expressing wild type RAS after 6 hrs by DCF-based flow cytometric analysis	22832321
human BJeLR cells	Cytotoxic assay	10 μM	12 h	Cytotoxicity against human BJeLR cells expressing RAS G12V mutant at 10 uM at 12 hrs by trypan blue staining	22832321
human BJ cells	Function assay	4.6 μM		Increase in intracellular oxidative species in human BJ cells expressing TERT, LT, ST and RAS G12V mutant genes cells at 4.6 uM	17568748

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	GPX4 / cleaved-PARP / cleaved-caspase3 / LC3 / p62 / LDH / HMGB1; TfR1 / p-JNK / JNK / p-P38; HSPA5 / p-EIF2AK3; GRP78;	27308510 31105999 28130223 29383150
Growth inhibition assay	Cell survival;	29348676
Immunofluorescence	HMGB1;	31105999