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RSL3

RSL3

产品编号 T3646   CAS 1219810-16-8
别名: RSL3 1S, 1S,3R-RSL3

RSL3 (RSL3 1S) 是一种 GPX4 的抑制剂,抑制阻断 GSH 合成的 system xc- (IC50=100 nM)。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。

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RSL3 Chemical Structure
RSL3, CAS 1219810-16-8
规格 价格/CNY 货期 数量
1 mg ¥ 456 现货
2 mg ¥ 783 现货
5 mg ¥ 1,230 现货
10 mg ¥ 1,930 现货
25 mg ¥ 3,110 现货
50 mg ¥ 4,570 现货
100 mg ¥ 6,520 现货
1 g ¥ 9,820 现货
1 mL * 10 mM (in DMSO) ¥ 1,150 现货
产品目录号及名称: RSL3 (T3646)
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选择批次  
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
产品描述 RSL3 (RSL3 1S) is an inhibitor of GPX4, and inhibits system xc- that blocks GSH synthesis (IC50=100 nM). RSL3 is a VDAC-independent activator of iron death that is selective for tumor cells carrying oncogenic RAS.
靶点活性 GSH:100 nM
体外活性 方法:人肝癌细胞 HepG2、HA22T/VGH 用 RSL3 (0.1-10 μM) 处理 72 h,使用 MTT 方法检测细胞生长抑制情况。
结果:RSL3 剂量依赖性地抑制 HepG2、HA22T/VGH 细胞生长,对 HepG2 细胞的 IC50 约为 0.07 μM,对 HA22T/VGH 细胞的 IC50 约为 0.3 μM。[1]
方法:人胶质母细胞瘤细胞 U87 和 U251 分别用 RSL3 (0.25 μM 和 0.5 μM) 处理 24 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:RSL3 处理诱导 U87 和 U251 细胞中铁死亡相关蛋白 GPX4、ATF4 和 xCT 的表达降低,HO-1 的表达上调。[2]
方法:人结直肠癌细胞 HCT116 和 LoVo 用 RSL3 (3 μM) 处理 24 h,使用 Flow Cytometry 方法分析 Labile iron pool (LIP) 和 ROS 细胞内水平。
结果:RSL3 促进铁死亡相关的 LIP 增加和 ROS 积累。[3]
体内活性 方法:为检测体内抗肿瘤活性,将 RSL3 (100 mg/kg in 20 μL DMSO plus 80 μL corn oil) 腹腔注射给携带人前列腺癌肿瘤 DU145 或 PC3 的 NSG 小鼠,每周两次,持续十六天。
结果:RSL3 治疗显著抑制人前列腺癌肿瘤的生长,表明在体内具有抗肿瘤活性。[4]
方法:为检测体内抗肿瘤活性,将 RSL3 (1 mg/kg) 和 cetuximab (13 mg/kg) 腹腔注射给携带 KRAS 突变人结直肠癌肿瘤 DLD-1 的 BALB/c nude 小鼠,每周一次,持续十六天。
结果:RSL3 治疗显著抑制 KRAS 突变的肿瘤生长,cetuximab 通过激活 p38 MAPK 抑制 Nrf2/HO-1 轴来增强 RSL3 诱导的铁死亡,进一步抑制肿瘤生长。[5]
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

T3646_1

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 1 year

溶解度

DMSO: 44.1 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2682 mL 11.341 mL 22.6819 mL 56.7048 mL
5 mM 0.4536 mL 2.2682 mL 4.5364 mL 11.341 mL
10 mM 0.2268 mL 1.1341 mL 2.2682 mL 5.6705 mL
20 mM 0.1134 mL 0.567 mL 1.1341 mL 2.8352 mL
50 mM 0.0454 mL 0.2268 mL 0.4536 mL 1.1341 mL
100 mM 0.0227 mL 0.1134 mL 0.2268 mL 0.567 mL

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
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参考文献

1. Asperti M, et al. H-ferritin suppression and pronounced mitochondrial respiration make Hepatocellular Carcinoma cells sensitive to RSL3-induced ferroptosis. Free Radic Biol Med. 2021 Jun;169:294-303. 2. Li S, et al. RSL3 Drives Ferroptosis through NF-κB Pathway Activation and GPX4 Depletion in Glioblastoma. Oxid Med Cell Longev. 2021 Dec 26;2021:2915019. 3. Sui X, et al. RSL3 Drives Ferroptosis Through GPX4 Inactivation and ROS Production in Colorectal Cancer. Front Pharmacol. 2018 Nov 22;9:1371. 4. Ghoochani A, et al. Ferroptosis Inducers Are a Novel Therapeutic Approach for Advanced Prostate Cancer. Cancer Res. 2021 Mar 15;81(6):1583-1594. 5. Yang J, et al. Cetuximab promotes RSL3-induced ferroptosis by suppressing the Nrf2/HO-1 signalling pathway in KRAS mutant colorectal cancer. Cell Death Dis. 2021 Nov 13;12(11):1079.

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.
11. Liu J, Meng F, Lv J, et al.Comprehensive Monitoring of Mitochondrial Viscosity Variation during Different Cell Death Processes by a NIR Mitochondria-targeting Fluorescence Probe.Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy.2023: 122602. 12. Li Y, Bao Y, Li Y, et al.RSL3 Inhibits Porcine Epidemic Diarrhea Virus Replication by Activating Ferroptosis.Viruses.2023, 15(10): 2080. 13. Shi H, Jiang X, Cao L, et al.Chemical constituents of Ajuga forrestii and their anti-ferroptosis activity.Fitoterapia.2023: 105461. 14. Li P, Lin Q, Sun S, et al. Inhibition of cannabinoid receptor type 1 sensitizes triple-negative breast cancer cells to ferroptosis via regulating fatty acid metabolism. Cell Death & Disease. 2022, 13(9): 1-15. 15. Peng, Xing, et al. Discovery of phloroglucinols from Hypericum japonicum as ferroptosis inhibitors. Fitoterapia. (2021): 104984. 16. Zhang H, Shan G, Jin X, et al. ARNTL2 is an indicator of poor prognosis, promotes epithelial-to-mesenchymal transition and inhibits ferroptosis in lung adenocarcinoma. Translational Oncology. 2022, 26: 101562. 17. Peng X, Tan Q, Wu L, et al. Ferroptosis Inhibitory Aromatic Abietane Diterpenoids from Ajuga decumbens and Structural Revision of Two 3, 4-Epoxy Group-Containing Abietanes. Journal of Natural Products. 2022 18. Wang F, Liu Y, Ni F, et al. BNC1 deficiency-triggered ferroptosis through the NF2-YAP pathway induces primary ovarian insufficiency. Nature Communications. 2022, 13(1): 1-17. 19. Li W, Luo L X, Zhou Q Q, et al. Phospholipid peroxidation inhibits autophagy via stimulating the delipidation of oxidized LC3-PE. Redox Biology. 2022: 102421. 20. Ning X, Qi H, Yuan Y, et al. Identification of a new small molecule that initiates ferroptosis in cancer cells by inhibiting the system Xc− to deplete GSH. European Journal of Pharmacology. 2022: 175304. 21. Fang Y, Tan Q, Zhou H, et al. Discovery and optimization of 2-(trifluoromethyl) benzimidazole derivatives as novel ferroptosis inducers in vitro and in vivo. European Journal of Medicinal Chemistry. 2022: 114905. 22. Li H, Shi W, Li X, et al. Ferroptosis is Accompanied by• OH Generation and Cytoplasmic Viscosity Increase Revealed via Dual-Functional Fluorescence Probe. Journal of the American Chemical Society. 2019 23. Shan G, Bi G, Zhao G, et al.Inhibition of PKA/CREB1 pathway confers sensitivity to ferroptosis in non-small cell lung cancer.Respiratory Research.2023, 24(1): 1-15. 24. Cao Z, Liu X, Zhang W, et al.Biomimetic Macrophage Membrane-Camouflaged Nanoparticles Induce Ferroptosis by Promoting Mitochondrial Damage in Glioblastoma.ACS nano.2023 25. Teng X, Shi H, Cao L, et al.Chemical Constituents of Ajuga lupulina and Their Anti‐ferroptosis ActivityChemical Constituents of Ajuga lupulina and Their Anti‐ferroptosis Activity.Chemistry & Biodiversity.2024: e202400244. 26. Xu L, Wen B, Wu Q, et al.Long non-coding RNA KB-1460A1. 5 promotes ferroptosis by inhibiting mTOR/SREBP-1/SCD1-mediated polyunsaturated fatty acid desaturation in glioma.Carcinogenesis.2024: bgae016.
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相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 氧化还原化合物库 抗氧化化合物库 经典已知活性库 表型筛选靶点鉴定库 细胞凋亡化合物库 代谢化合物库 抑制剂库 共价抑制剂库 半胱氨酸共价化合物库

剂量换算

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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
g
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
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% ddH2O
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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 inhibit RSL-3 (1S,3R)-RSL3 RSL3 1S 1S,3R-RSL3 Inhibitor RSL 3 inhibitor

 

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