Piperazine Erastin
Based on 9 publication(s) in Google Scholar
Piperazine erastin is an analog of erastin which induces an iron-dependent form of non-apoptotic cell death, termed ferroptosis. Piperazine erastin can be used in cancer research.
For research use only. We do not sell to patients.
- Purity : 99.12%
- CAS No.: 1538593-71-3
- Formula: C35H41ClN6O4
- Molecular Weight:645.19
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-100218A
RSL3GPX4 Inhibitor -
HY-100579
Ferrostatin-1Ferroptosis Inhibitor -
HY-138153
JKE-1674GPX4 Inhibitor -
HY-136057
iFSP1FSP1 Inhibitor -
HY-100887R
Piperazine Erastin (Standard)Ferroptosis Inducer -
HY-163002
viFSP1FSP1 Inhibitor -
HY-153629
FSEN1FSP1 Inhibitor -
HY-158775
FerroptocideFerroptosis Inducers
Publications Citing Use of MedChemExpress (MCE) Piperazine Erastin
More- Cancer Commun (Lond). 2022 Apr;42(4):287-313. [Abstract]
- Nat Commun. 2020 Mar 6;11(1):1251. [Abstract]
- Redox Biol. 2021 Jan:38:101801. [Abstract]
- Redox Biol. 2019 Jun:24:101211. [Abstract]
- Int J Biol Sci. 2022 Jun 21;18(10):4135-4150. [Abstract]
- Cell Death Discov. 2021 Apr 16;7(1):83. [Abstract]
- J Cancer. 2023 May 15;14(8):1336-1349. [Abstract]
- Oxid Med Cell Longev. 2022 Jun 1:2022:2985249. [Abstract]
- Research Square Preprint. 2021 Sep.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCF-STTG1 | IC50 |
800 nM
Compound: PE
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Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry
Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry
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[PMID: 26231156] |
| HT-1080 | GI50 |
1196 nM
Compound: PE
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Growth inhibition of human HT1080 cells after 48 hrs by alamar blue assay
Growth inhibition of human HT1080 cells after 48 hrs by alamar blue assay
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[PMID: 26231156] |
In Vitro
Erastin is a ferroptosis activator. It triggers a unique iron-dependent form of non-apoptotic cell death that is termed as ferroptosis. Piperazine erastin is a more effective analog of erastin which is more water-soluble (0.086 mM for erastin versus 1.4 mM for piperazine erastin) and more metabolically stable. Piperazine erastin is affected similarly by cell death modulators as erastin and displays a distinct pattern from other non-FIN lethal compounds[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1538593-71-3
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Appearance Solid
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Molecular Weight 645.19
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Formula C35H41ClN6O4
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Color White to off-white
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SMILES
O=C1N(C2=CC(CN3CCNCC3)=CC=C2OC(C)C)C(CN4CCN(C(COC5=CC=C(Cl)C=C5)=O)CC4)=NC6=C1C=CC=C6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (9)
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Journal Impact Factor
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Most Recent
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Cancer Commun (Lond)
Essential roles of exosome and circRNA_101093 on ferroptosis desensitization in lung adenocarcinoma. [Abstract]2022 Apr;42(4):287-313. PMID: 35184419 -
Nat Commun
DJ-1 suppresses ferroptosis through preserving the activity of S-adenosyl homocysteine hydrolase. [Abstract]2020 Mar 6;11(1):1251. PMID: 32144268 -
Redox Biol
The m6A reader YTHDC2 inhibits lung adenocarcinoma tumorigenesis by suppressing SLC7A11-dependent antioxidant function. [Abstract]2021 Jan:38:101801. PMID: 33232910 -
Redox Biol
2019 Jun:24:101211. PMID: 31108460 -
Int J Biol Sci
2022 Jun 21;18(10):4135-4150. PMID: 35844792 -
Cell Death Discov
O-GlcNAcylation enhances sensitivity to RSL3-induced ferroptosis via the YAP/TFRC pathway in liver cancer. [Abstract]2021 Apr 16;7(1):83. PMID: 33863873 -
J Cancer
PERK/ATF3-Reduced ER Stress on high potassium environment in the suppression of tumor ferroptosis. [Abstract]2023 May 15;14(8):1336-1349. PMID: 37283787 -
Oxid Med Cell Longev
Activated Stellate Cell Paracrine HGF Exacerbated Pancreatic Cancer Cell Ferroptosis Resistance. [Abstract]2022 Jun 1:2022:2985249. PMID: 35693705 -
Solvent & Solubility
In Vitro:
DMSO : 33.33 mg/mL (51.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5499 mL | 7.7497 mL | 15.4993 mL | 38.7483 mL |
| 5 mM | 0.3100 mL | 1.5499 mL | 3.0999 mL | 7.7497 mL | |
| 10 mM | 0.1550 mL | 0.7750 mL | 1.5499 mL | 3.8748 mL | |
| 15 mM | 0.1033 mL | 0.5166 mL | 1.0333 mL | 2.5832 mL | |
| 20 mM | 0.0775 mL | 0.3875 mL | 0.7750 mL | 1.9374 mL | |
| 25 mM | 0.0620 mL | 0.3100 mL | 0.6200 mL | 1.5499 mL | |
| 30 mM | 0.0517 mL | 0.2583 mL | 0.5166 mL | 1.2916 mL | |
| 40 mM | 0.0387 mL | 0.1937 mL | 0.3875 mL | 0.9687 mL | |
| 50 mM | 0.0310 mL | 0.1550 mL | 0.3100 mL | 0.7750 mL |
Piperazine Erastin Related Classifications
HY-100887 Related Classifications
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