1. Apoptosis
  2. Ferroptosis
  3. Erastin2

Erastin2, an Erastin (HY-15763) analog, is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter

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Erastin2 Chemical Structure

Erastin2 Chemical Structure

CAS No. : 1695533-44-8

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Based on 1 publication(s) in Google Scholar

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Description

Erastin2, an Erastin (HY-15763) analog, is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter[1][2][3][4]

In Vitro

Erastin2 (2 μM, 48 h) induced ferroptosis correlates with acute amino acid deprivationinduced proliferative arrest in a manner that can be independent of mTOR inhibition and GCN2/ATF4 pathway activation in both U-2 OSN and HT-1080N cells in response to erastin2[1].
Erastin2 (1 μM, 48 h) -induced HT-1080 TP53 KO fibrosarcoma cell death are sensitive regardless of nutlin-3 pretreatment [4].
p53 sabilization suppresses Erastin2 (1 μM, 48 h) -induced ferroptosis in response to system xc(-) inhibition in HT-1080 TP53 KO fibrosarcoma cells[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HT-1080N fibrosarcoma cells
Concentration: 1 or 2 μM
Incubation Time: 48 h
Result: Consistently initiated cell death 8 h earlier than Camptothecin (HY-16560), such that Camptothecin (HY-16560) may not have time to act before the induction of ferroptosis has already committed cells to death via this pathway in HT-1080N fibrosarcoma cells.
The six most potent compounds (Fer-1, SKI II, phenothiazine, JNJ-26854165, AZD3463, and bazedoxifene) all suppressed Erastin2 and ML162-induced ferroptosis with sub-150 nM potency in HT-1080N fibrosarcoma cells.

Cell Proliferation Assay[1]

Cell Line: U-2 OSN and HT-1080N cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Deprivation of glutamine, lysine, valine, methionine, and arginine, all suppressed ferroptosis in both U-2 OSN and HT-1080N cells in response to erastin2.

Cell Proliferation Assay[4]

Cell Line: Human HT-1080 TP53 KO fibrosarcoma cells
Concentration: 1 μM, pretreated for 48 h with or without Nutlin-3 (HY-50696)
Incubation Time: 48 h
Result: Control cells pretreated with nutlin-3 were less sensitive to erastin2-induced cell death, by contrast, TP53 KO cells were equally sensitive to erastin2 regardless of nutlin-3 pretreatment.
Molecular Weight

623.14

Formula

C36H35ClN4O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(N=C(CN3CCN(CC3)C(COC4=CC=C(C=C4)Cl)=O)N1C5=C(OC(C)C)C=CC(C6=CC=CC=C6)=C5)C=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (160.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6048 mL 8.0239 mL 16.0478 mL
5 mM 0.3210 mL 1.6048 mL 3.2096 mL
View the 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, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation
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, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6048 mL 8.0239 mL 16.0478 mL 40.1194 mL
5 mM 0.3210 mL 1.6048 mL 3.2096 mL 8.0239 mL
10 mM 0.1605 mL 0.8024 mL 1.6048 mL 4.0119 mL
15 mM 0.1070 mL 0.5349 mL 1.0699 mL 2.6746 mL
20 mM 0.0802 mL 0.4012 mL 0.8024 mL 2.0060 mL
25 mM 0.0642 mL 0.3210 mL 0.6419 mL 1.6048 mL
30 mM 0.0535 mL 0.2675 mL 0.5349 mL 1.3373 mL
40 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0030 mL
50 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8024 mL
60 mM 0.0267 mL 0.1337 mL 0.2675 mL 0.6687 mL
80 mM 0.0201 mL 0.1003 mL 0.2006 mL 0.5015 mL
100 mM 0.0160 mL 0.0802 mL 0.1605 mL 0.4012 mL
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Erastin2 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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