Ferrostatin-1 (Fer-1)
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| カタログ番号GC10380 |
Ferrostatin-1は有力なフェロトーシスの阻害剤で、EC50は60nMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 347174-05-4
Sample solution is provided at 25 µL, 10mM.
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Ferrostatin-1は有力なフェロトーシスの阻害剤で、EC50は60nMである。
Ferrostatin-1は分子阻害剤として、フェロトーシスを防ぐことができる。Ferrostatinは膜脂質の酸化損傷を防ぐために作用すると見られている。抗酸化作用を持つアリールアルキルアミンであるFerrostatin-1は、フェロトーシスの最初の阻害剤の一つだと看做されている。Ferrostatin-1は、erastinなどの小分子で処理された癌細胞における酸化、鉄依存な細胞死を減衰する。 [3]
Ferrostatin-1はフェロトーシスの阻害剤で、EC50は60 nM (HT-1080)である。また、Ferrostatin-1はフェロトーシスという非アポトーシス性の細胞死を阻害することもできた。このドーパミン神経芽腫細胞(SH-SY5Y)におけるロテノン誘発酸化ストレス下のFerrostatin-1の精神保護の役割が報告された。Ferrostatin-1は、SH-SY5Y細胞におけるロテノン障害下で生成されるROS/RNSを阻害した。Ferrostatin-1がERストレスを介したアポトーシス経路の活性化に効果的に作用することが確認された。更に、Ferrostatin-1がロテノン誘発性のα-synの凝集を緩和したことも報告されている。[1]
フェロトーシスの特異的な阻害剤であるFerrostatin-1は、神経細胞の死亡を阻止する為に投与され、器官型海馬切片培養(OHSCs)におけるヘモグロビン誘導による鉄沈着を減少した。ICH後にFerrostatin-1を投与されたマウスは、脳の保護と進んだ神経機能が観察された。更に、Ferrostatin-1は脂質活性の酸素種の生産を減少し、体外と体内実験でPTGS2とその遺伝子産物シクロオキシゲナーゼ-2の発現レベルの増加を弱めた。生体内実験では、コラーゲナーゼ注射直後に線条体に1pmolのFerrostatin-1(生理食塩水の中の1μl、0.01%のDMSOに10μMのFerrostatin-1)を注射し、あるいはコラーゲナーゼ注射の二時間後に脳室に注射した。脳室への注射の座標は、ブレグマに対して外側に1.0 mm、後方に0.5 mm、深さに2.5 mmであった[2]。
References:
[1] Kabiraj P, et al. The neuroprotective role of ferrostatin-1 under rotenone-induced oxidative stress in dopaminergic neuroblastoma cells. Protein J. 2015 Oct;34(5):349-58.
[2] Li Q, et al. Inhibition of neuronal ferroptosis protects hemorrhagic brain. JCI Insight. 2017 Apr 6;2(7):e90777. doi: 10.1172/jci.insight.90777.
[3] Hofmans S, et al. Novel Ferroptosis Inhibitors with Improved Potency and ADME Properties. J Med Chem. 2016 Mar 10;59(5):2041-53.
| 細胞実験[1]: | |
細胞株 | SH-S5Y |
準備方法 | DMSO（最大100 mg/ml）またはエタノール（最大100 mg/ml）に可溶。 |
反応条件 | 1 μM, 24時間 |
アプリケーション | Ferrostatin-1はフェロトーシスという非アポトーシス性の細胞死を阻害することもできた。このドーパミン神経芽腫細胞(SH-SY5Y)におけるロテノン誘発酸化ストレス下のFerrostatin-1の精神保護の役割が報告された。Ferrostatin-1は、SH-SY5Y細胞におけるロテノン刺激下で生成されるROS/RNSを阻害した。 |
| 動物実験 [2]: | |
動物モデル | C57BL/6 (ICH, 脳内出血) |
準備方法 | 生理食塩水の中の1μl、0.01%のDMSOに10μMのFerrostatin-1 |
投与形態 | 1pmolのFerrostatin-1、コラーゲナーゼ注射 |
アプリケーション | フェロトーシスの特異的な阻害剤であるFerrostatin-1は、神経細胞の死亡を阻止する為に投与され、器官型海馬切片培養(OHSCs)におけるヘモグロビン誘導による鉄沈着を減少した。ICH後にFerrostatin-1を投与されたマウスは、脳の保護と進んだ神経機能が観察された。更に、Ferrostatin-1は脂質活性の酸素種の生産を減少し、体外と体内実験でPTGS2とその遺伝子産物シクロオキシゲナーゼ-2の発現レベルの増加を弱めた。 |
References: | |
| Cas No. | 347174-05-4 | SDF | |
| 同義語 | Fer-1 | ||
| Canonical SMILES | NC1=C(NC2CCCCC2)C=CC(C(OCC)=O)=C1 | ||
| Formula | C15H22N2O2 | M.Wt | 262.35 |
| 溶解度 | 125mg/ml in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.8117 mL | 19.0585 mL | 38.117 mL |
| 5 mM | 762.3 μL | 3.8117 mL | 7.6234 mL |
| 10 mM | 381.2 μL | 1.9059 mL | 3.8117 mL |
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
Interestingly, ferrostatin-1, an inhibitor of ferropto-sis in mammalian cells, significantly inhibited the antibacterialactivity of Fe(II)Snaq.
Ferrostatin-1 andLiproxstatin-1 were purchased from Glpbio (USA).
Nano Today 35 (2020): 100981. IF: 18.9615 -
Related Biological Data
Ferroptosis is triggered following FGFR4 inhibition in anti-HER2 resistant breast cancer cells. h The ratio of oxidized to nonoxidized lipids was assessed by flow cytometry following C11-BODIPY probe staining in rSKBR3 cells.
Cell death caused by roblitinib was partly rescued by cotreatment with the specific ferroptosis inhibitors ferrostatin-1 (1 μM)(GLPbio), liproxstatin-1 (500 nM) or the iron chelator deferoxamine (DFO, 100 μM).
Nature Communications 13.1 (2022): 2672. PMID: 36642338 IF: 16.6009 -
Related Biological Data
Cytotoxicity of HP NPs + RT after incubation with different ferroptosis inhibitors Fer1, VE, and GSH.
Cells were co-administered by HP NPs (hemin dose: 15 μg ·mL −1 ) with 50 nM Ferrostatin-1(GLPbio), 100 μM vitamin E, and 1 mM glutathione, and treated with radiotherapy (8 Gy).
Acta Biomaterialia (2023). PMID: 36642338 IF: 10.6335 -
Related Biological Data
Cell death pathway and cell morphology (n = 3). (a) The cell viability treated with LDG plus inhibitors of different cell death pathways and action mechanism.
To study the specific cell death pathway induced by liposomes,LDG was administrated in combination with Ferrostatin-1 (Fer-1, ferroptosis inhibitor, 16 μM)（GLPbio）, Desferrioxamine (100 μM), Z-VADFMK (50 μM), 3-MA (25μM), Necrostatin-1 (20 μM), and Nacetylcysteine (20 μM) to measure the cell viability rescuing profile using the CCK8 assay.
Nano Research, 2024: 1-17. IF: 9.8996 -
Related Biological Data
Suggesting that inhibition of LPO ameliorated GLY-triggered ferroptosis in TM3 cells. Consequently, the downregulation of GLY-induced cell viability.
To elucidate the involvement of ferroptosis in GLY-induced cytotoxicity, cells were pre-treated with 10 μM Fer-1（GLPbio） for 6 h and subsequently treated with 1mM GLY for 24 h to assess relevant indicators.
Science of The Total Environment (2024): 169927. PMID: 38199345 IF: 9.8003 -
Related Biological Data
Deoxycholic acid enhanced lipopolysaccharide-induced ferroptosis in intestinal epithelial cells (J) The content of GSH in each group of IEC-6 cells (n ¼ 5 in each group). (K) The content of MDA in each group of IEC-6 cells (n 1/4 5 in each group).
Glucose uptake ability of VSMCs was evaluated by using the fluores-cent glucose Ferrostatin-1 (Fer-1) (GlpBio, USA) according to the manufactur-er’s instruction. cells were plated onto coverslips and incubated with DMEM containing 10 μM Ferrostatin-1 (Fer-1) at room temperature for 1 h.Cell Death Dis.
Molecular Metabolism (2024): 101944. PMID: 38642891 IF: 8.1 -
Related Biological Data
Cells were incubated with different concentrations (0.25 and 0.5 mmol/L) of PA in the presence or absence of either 4 μmol/L Fer-1.
Cells were incubated with different concentrations (0, 0.125, 0.25, 0.5, and 1.0 mmol/L) of PA for 72 h. Intracellular iron levels were determined with an iron colorimetric assay kit, and lipid peroxidation was determined by the fluorescent probe C11 BODIPY 581/591 using flow cytometry.
Free Radical Bio Med(2021). -
Related Biological Data
A7r5 cells were treated with 100% cigarette smoke extract (CSE) for 4 h in the presence or absence of Fer-1 (5 μM), cell viability was assessed using the CCK8 assay (n = 3). (D-J) Changes in mRNA expression of hub genes after 4 h of 100%CSE treatment in the presence or absence of Fer-1 (5 μM) by qRT-PCR (n = 3).
Ferrostatin-1 (Fer-1, GC10380) was purchased from Glpbio Technology Inc. (Montclair, CA, USA) and dissolved in dimethyl sulfoxide (DMSO). In cell culture experiments, Fer-1 was treated 1 h before CSE treatment at a concentration of 5 μM.
Bioengineered Just-Accepted (2021).
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