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RSL3

产品编号 T3646 CAS 1219810-16-8

别名: RSL3 1S, 1S,3R-RSL3

RSL3 是一种不依赖 VDAC 的铁死亡激活剂，对携带致癌 RAS 的肿瘤细胞具有选择性。它是谷胱甘肽过氧化物酶 4 的抑制剂，可抑制阻断 GSH 合成的半胱氨酸/谷氨酸氨基酸转运系统 xc-，IC50为100 nM。

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RSL3, CAS 1219810-16-8

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纯度: 99.96%

纯度: 99.64%

纯度: 99.39%

纯度: 99.23%

纯度: 98.06%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

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产品描述

RSL3 is a VDAC-independent ferroptosis activator with selectivity for tumor cells bearing oncogenic RAS. RSL3 is the inhibitor of the glutathione peroxidase 4, which can inhibit the cysteine/glutamate amino acid transporter system xc- that blocks GSH synthesis (IC50: 100 nM).

靶点活性

GSH:100 nM

体外活性

Ferroptosis-inducing compounds inactivate GPX4 by direct binding or by depleting glutathione.After binding to GPX4, RSL3 inactivates GPX4 to induce ROS production from lipid peroxidation. RSL3's ability to induce synthetic lethality with oncogenic RAS is rapid and quite potent. This compound inhibits the growth of BJ-TERT/LT/ST/RASV12 and DRD cells as low as 10 ng/mland started to kill sensitive cells as early as 8 hr after treatment[1][2].

CellLine:	PC3 and DU145 cells
Concentration:	0.125，0.5μM
IncubationTime:	6 days
Result:	RSL3 decreased the migration of PC3 and DU145 cells

CellLine:	PIK3CA-mutant CRC cells
Concentration:	0.1 μM
IncubationTime:	24h
Result:	The protein levels of AKT, p-AKT, p-mTOR and mTOR decreased sharply

体内活性

Prostaglandin-endoperoxide synthase (PTGS) is the key enzyme in prostaglandin biosynthesis. There are two isozymes of PTGS: a constitutive PTGS1 and an inducible PTGS2. PTGS2 encoding cyclooxygenase-2 (COX-2) is significantly upregulated after treatment with RSL3 and erastin in mice[1].

Animal Model:	Six- to 10-week-old, sex-matched mice C57BL/6 mice
Dosage:	5 mg/kg
Administration:	I.p. daily for 2 days
Result:	RSL3 markedly suppressed IL-6 and IL-1b mRNA level in a dose-dependent manner

Animal Model:	flank of 6–8 weeks old NSG (NOD-SCID-IL2R γ) (Jackson Laboratory) male mice.
Dosage:	100 mg/kg
Administration:	Ip, biweekly
Result:	Significantly decreased tumor growth and tumor weight at end point of DU145 and PC3. (P<0.01) xenografts

细胞实验

TERT/LT/ST/RASV12 cells are seeded in 10 cm dishes and treated with 1 µM staurosporine, 10 µg/ml erastin, 20 µg/ml RSL5, and 1 µg/ml RSL3 for 16 hr. Both dying cells and live cells in each 10 cm dish are harvested and collected in the same 15 ml tubes by centrifuging cell suspension at 1000 rpm for 5 min. (Only for Reference)

别名	RSL3 1S, 1S,3R-RSL3
化合物与蛋白结合的复合物	Crystal structure of human GPX4-U46C in complex with RSL3
分子量	440.88
分子式	C23H21ClN2O5
CAS No.	1219810-16-8

存储

　|　Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 44.1 mg/mL (100 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Yang WS, et al. Chem Biol. 2008, 15(3):234-245. 2. Y Xie, et al. Cell Death and Differentiation. 2016, 23:369-379. 3. Li H, Shi W, Li X, et al. Ferroptosis is Accompanied by• OH Generation and Cytoplasmic Viscosity Increase Revealed via Dual-Functional Fluorescence Probe[J]. Journal of the American Chemical Society. 2019.

文献引用

1. Hu G, Cui Z, Chen X, et al.Suppressing Mesenchymal Stromal Cell Ferroptosis Via Targeting a Metabolism‐Epigenetics Axis Corrects their Poor Retention and Insufficient Healing Benefits in the Injured Liver Milieu.Advanced Science.2023: 2206439. 2. Feng Y, Luo X, Li Z, et al.A ferroptosis-targeting ceria anchored halloysite as orally drug delivery system for radiation colitis therapy.Nature Communications.2023, 14(1): 5083. 3. Bi G, Liang J, Shan G, et al.Retinol saturase mediates retinoid metabolism to impair a ferroptosis defense system in cancer cells.Cancer Research.2023: CAN-22-3977. 4. Li Y, Yang W, Zheng Y, et al.Targeting fatty acid synthase modulates sensitivity of hepatocellular carcinoma to sorafenib via ferroptosis.Journal of Experimental & Clinical Cancer Research.2023, 42(1): 1-19. 5. Wang X, Ji Y, Qi J, et al.Mitochondrial carrier 1 (MTCH1) governs ferroptosis by triggering the FoxO1-GPX4 axis-mediated retrograde signaling in cervical cancer cells.Cell Death & Disease.2023, 14(8): 1-13. 6. Tan Q, Zhang X, Li S, et al.DMT1 differentially regulates mitochondrial complex activities to reduce glutathione loss and mitigate ferroptosis.Free Radical Biology and Medicine.2023 7. Zhao G, Liang J, Shan G, et al.KLF11 regulates lung adenocarcinoma ferroptosis and chemosensitivity by suppressing GPX4.Communications Biology.2023, 6(1): 570. 8. Bow Y D, Ko C C, Chang W T, et al.A novel quinoline derivative, DFIQ, sensitizes NSCLC cells to ferroptosis by promoting oxidative stress accompanied by autophagic dysfunction and mitochondrial damage.Cancer Cell International.2023, 23(1): 1-11. 9. Gartzke L P, Hendriks K D W, Hoogstra-Berends F, et al.Inhibition of Ferroptosis Enables Safe Rewarming of HEK293 Cells following Cooling in University of Wisconsin Cold Storage Solution.International Journal of Molecular Sciences.2023, 24(13): 10939. 10. Jiang X, Teng X, Shi H, et al.Discovery and optimization of olanzapine derivatives as new ferroptosis inhibitors.Bioorganic Chemistry.2023: 106393.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

RSL3 1219810-16-8 Apoptosis Metabolism oxidation-reduction Ferroptosis GPX Glutathione Peroxidase RSL-3 inhibit RSL3 1S (1S,3R)-RSL3 RSL 3 Inhibitor 1S,3R-RSL3 inhibitor

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RSL3

存储

溶解度

参考文献

文献引用

相关产品

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剂量换算

体内实验配液计算器

计算器

输入分子式，点击计算，可计算出产品的分子量。

技术支持

Keywords