Erastin2
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Catalog No.GC43623
One-Click Copy Product Info
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Erastin2 is a potent system xc- inhibitor and ferroptosis-inducing agent.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1695533-44-8
Sample solution is provided at 25 µL, 10mM.
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Erastin2 is a potent system xc- inhibitor and ferroptosis-inducing agent [1].
Erastin2 (5µM, 24h) significantly inhibited the activity of human HAP1 haploid cells, and that erastin2-induced cell death was inhibited by co-treatment with the lipophilic radical-trapping antioxidant ferrostatin-1 or the iron chelator deferoxamine (DFO), but not the pan-caspase inhibitor Q-VD-OPh [1]. Erastin2 induced ferroptosis in HT-1080(1 µM), T98G glioblastoma (1 µM), and A549 non-small-cell lung carcinoma cells (2 µM), and non-transformed IMR-90 diploid fibroblasts (125nM) [2]. Erastin2 (1 µM) inhibited system xc- function, depleted total glutathione (GSH + GSSG), and upregulated CHAC1 expression [2]. Erastin2 (1-10µM) increased FSP1KO cells sensitivity [3]. In the context of erastin2-induced ferroptosis, the onset of cell death correlates with the oxidation of the lipid peroxide-sensitive probe C11 BODIPY 581/591 (C11) (Cat.No. GC40165) specifically at the plasma membrane, linking the onset of cell death to a key terminal marker of the ferroptotic process [1].
References:
[1]. Cao JY, Poddar A, Magtanong L, Lumb JH, Mileur TR, Reid MA, Dovey CM, Wang J, Locasale JW, Stone E, Cole SP. A genome-wide haploid genetic screen identifies regulators of glutathione abundance and ferroptosis sensitivity. Cell reports. 2019 Feb 5;26(6):1544-56.
[2]. Magtanong L, Ko PJ, To M, Cao JY, Forcina GC, Tarangelo A, Ward CC, Cho K, Patti GJ, Nomura DK, Olzmann JA. Exogenous monounsaturated fatty acids promote a ferroptosis-resistant cell state. Cell chemical biology. 2019 Mar 21;26(3):420-32.
[3]. Bersuker K, Hendricks JM, Li Z, Magtanong L, Ford B, Tang PH, Roberts MA, Tong B, Maimone TJ, Zoncu R, Bassik MC. The CoQ oxidoreductase FSP1 acts parallel to GPX4 to inhibit ferroptosis. Nature. 2019 Nov 28;575(7784):688-92.
| Cell experiment [1]: | |
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Cell lines |
Caki-1 cells |
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Preparation Method |
Caki-1 cells were seeded in a 96-well dish at 4000 (cells treated with control shRNA constructs and nutlin-3) or 2000 (all other treatments) cells/well and infected with lentiviruses carrying non-targeting shRNAs (sh-NT) or shRNAs targeting CDKN1A at an M.O.I. of ~1 in media containing 8 µg/mL Polybrene (source). Infected cells were then spun at 1000 rpm for 1 h at room temperature. The next day, virus-containing medium was removed, and cells were incubated in medium containing puromycin (10 µg/mL) and DMSO or nutlin-3 (10 µM) for a further 24 h. Media was then removed and replaced with media containing SYTOX Green (0.022 µM), DMSO or nutlin-3 (10 µM), and DMSO or erastin2 (1 µM), and cell death was assayed for the subsequent 48 h using time-lapse imaging. Cell death was assessed by counting SYTOX Green positive cells over time. |
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Reaction Conditions |
1 µM, for 48 h |
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Applications |
Short hairpin RNA (shRNA)-mediated silencing of CDKN1A in Caki-1 cells likewise abrogated the ability of nutlin-3 pretreatment to delay subsequent erastin2-induced cell death. |
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References: [1]: Dixon SJ, Patel DN, Welsch M, Skouta R, Lee ED, Hayano M, Thomas AG, Gleason CE, Tatonetti NP, Slusher BS, Stockwell BR. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis. elife. 2014 May 20;3:e02523. |
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| Cas No. | 1695533-44-8 | SDF | |
| Synonyms | 35MEW28 | ||
| Canonical SMILES | O=C1N(C2=CC(C3=CC=CC=C3)=CC=C2OC(C)C)C(CN4CCN(C(COC5=CC=C(Cl)C=C5)=O)CC4)=NC6=CC=CC=C61 | ||
| Formula | C36H35ClN4O4 | M.Wt | 623.1 |
| Solubility | 1mg/mL in DMSO, 10mg/mL in DMF | Storage | Store at -20°C,Cprotect 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6049 mL | 8.0244 mL | 16.0488 mL |
| 5 mM | 321 μL | 1.6049 mL | 3.2098 mL |
| 10 mM | 160.5 μL | 802.4 μL | 1.6049 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)