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Erastin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Erastin图片
包装与价格:
包装价格(元)
1mg电议
5mg电议
1mg * 5电议
10mg电议
1mg * 10电议
50mg电议

产品介绍

Erastin 是一种铁死亡诱导剂。 Erastin 结合并抑制电压依赖性阴离子通道 (VDAC2/VDAC3)。

Cell lines

143B/BJeHLT/BJeLR/Calu-1/HT-1080

Preparation Method

Soluble in DMSO to 20 mM.

Reaction Conditions

10 μM, 72 h

Applications

Erastin inhibited cystine uptake via system xcand triggered ferroptosis in a variety of cellular contexts.(HT-1080: erastin IC50= 0.20 μM; Calu-1: erastin IC50= 0.14 μM)

Animal models

BALB/c nude mice (colorectal cancer)

Preparation Method

Soluble in DMSO to 20 mM

Dosage form

10 mg/kg, intravenous injection

Applications

Erastin inhibited ALDH1 activity, and reduced sphere size and number in colorectal cancer cells.

文献引用
产品描述

Erastin is a cell-permeable ferroptosis activatior and an antitumor agent that is selective for cell expressing oncogene RAS.

Erastin induces ferroptosis through directly binding to VDAC2/3 to alter the permeability of the outer mitochondrial membrane, which decreases the rate of NADH oxidation. Besides exerting targeted effects, erastin also enhances chemotherapy, targeted therapy, and immunotherapy in certain cancer cells, suggesting a potential role of erastin in cancer cell treatment.[3]

Erastin and its analogs specifically inhibited cystine uptake via system xc, and triggered ferroptosis in a variety of cellular contexts and act much more potently than SAS. Moreover, Erastin was ~2500 times more potent than SAS as an inhibitor of system xcfunction in both HT-1080 and Calu-1 cells (HT-1080: erastin IC50= 0.20 μM, SAS IC50= 450 μM; Calu-1: erastin IC50= 0.14 μM, SAS IC50= 460 μM).[1]

Erastin, an inhibitor of SLC7A11, was found to hold a remarkably stronger cytotoxic effect on colorectal CSCs via in vitro and in vivo experiments. Besides, Erastin attenuated the chemoresistance of colorectal CSCs (colorectal cancer stem cells). For in vivo experiment, Erastin (10 mg/kg) was intravenously injected into mice with colorectal cancer every two days. It was found that Erastin inhibited ALDH1 activity, and reduced sphere size and number in colorectal cancer cells. [2]

References:
[1]. Dixon SJ, et al. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis. Elife. 2014 May 20;3:e02523.
[2]. Xu X, et al. Targeting SLC7A11 specifically suppresses the progression of colorectal cancer stem cells via inducing ferroptosis. Eur J Pharm Sci. 2020 Sep 1;152:105450.
[3]. Yang Y, et al. Nedd4 ubiquitylates VDAC2/3 to suppress erastin-induced ferroptosis in melanoma. Nat Commun. 2020 Jan 23;11(1):433.