RSL3

カタログ番号 T3646 CAS 1219810-16-8

別名: RSL3 1S, 1S,3R-RSL3

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.

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RSL3, CAS 1219810-16-8

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
1 mg	在庫あり	￥ 7,500
2 mg	在庫あり	￥ 11,000
5 mg	在庫あり	￥ 16,500
10 mg	在庫あり	￥ 29,500
25 mg	在庫あり	￥ 62,500
50 mg	在庫あり	￥ 84,500
100 mg	在庫あり	￥ 111,000
500 mg	在庫あり	￥ 248,000
1 g	在庫あり	￥ 328,500
1 mL * 10 mM (in DMSO)	在庫あり	￥ 16,000

バルクのお問い合わせ

バッチを選択

純度: 99.96%

COA DATASHEET SDS HPLC HNMR

純度: 99.64%

COA DATASHEET SDS HPLC HNMR

純度: 99.39%

COA DATASHEET SDS LCMS HPLC HNMR

純度: 99.23%

COA DATASHEET SDS HNMR HPLC

純度: 99.23%

COA DATASHEET SDS

純度: 98.52%

DATASHEET SDS

純度: 98.06%

COA DATASHEET SDS HPLC

純度: 98%

COA DATASHEET SDS HNMR

COA DATASHEET SDS

DATASHEET SDS

COA DATASHEET SDS HNMR HPLC

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	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.
ターゲット＆IC50	GSH:100 nM
In vitro	METHODS: Human hepatocellular carcinoma cells HepG2, HA22T/VGH were treated with RSL3 (0.1-10 μM) for 72 h, and cell growth inhibition was detected by MTT. RESULTS: RSL3 dose-dependently inhibited the growth of HepG2 and HA22T/VGH cells, with an IC50 of about 0.07 μM for HepG2 cells and 0.3 μM for HA22T/VGH cells. [1] METHODS: Human glioblastoma cells U87 and U251 were treated with RSL3 (0.25 μM and 0.5 μM) for 24 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: RSL3 treatment induced a decrease in the expression of iron death-related proteins GPX4, ATF4 and xCT, and an up-regulation in the expression of HO-1 in U87 and U251 cells. [2] METHODS: Human colorectal cancer cells HCT116 and LoVo were treated with RSL3 (3 μM) for 24 h. Labile iron pool (LIP) and ROS intracellular levels were analyzed by Flow Cytometry. RESULTS: RSL3 promoted the increase of LIP and accumulation of ROS associated with iron death. [3]
In vivo	METHODS: To test the antitumor activity in vivo, RSL3 (100 mg/kg in 20 μL DMSO plus 80 μL corn oil) was intraperitoneally injected into NSG mice bearing human prostate cancer tumors DU145 or PC3 twice a week for sixteen days. RESULTS: RSL3 treatment significantly inhibited the growth of human prostate cancer tumors, indicating antitumor activity in vivo. [4] METHODS: To detect anti-tumor activity in vivo, RSL3 (1 mg/kg) and cetuximab (13 mg/kg) were intraperitoneally injected once a week for sixteen days into BALB/c nude mice harboring KRAS-mutant human colorectal cancer tumor DLD-1. RESULTS: RSL3 treatment significantly inhibited the growth of KRAS-mutant tumors. Cetuximab enhanced RSL3-induced iron death by activating p38 MAPK and inhibiting the Nrf2/HO-1 axis, which further inhibited tumor growth. [5]
細胞研究	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)

別名	RSL3 1S, 1S,3R-RSL3
分子量	440.88
分子式	C23H21ClN2O5
CAS No.	1219810-16-8

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

DMSO: 45 mg/mL (102.07 mM)

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.

引用文献

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. 27. Bi G, Liang J, Bian Y, et al.Polyamine-mediated ferroptosis amplification acts as a targetable vulnerability in cancer.Nature Communications.2024, 15(1): 2461. 28. Huang Q, Ru Y, Luo Y, et al.Identification of a targeted ACSL4 inhibitor to treat ferroptosis-related diseases.Science Advances.2024, 10(13): eadk1200. 29. Lv S, Pan Q, Lu W, et al.Tenovin 3 induces apoptosis and ferroptosis in EGFR 19del non small cell lung cancer cells.Scientific Reports.2024, 14(1): 7654.

もっと見る隠し

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

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

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

RSL3

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords