Erastin得名于eradicator of RAS和小T(ST)抗原表达细胞,是一种铁死亡诱导剂。1 它能在体外诱导铁死亡,这种作用可被铁死亡抑制剂环吡酮胺、Trolox(货号10011659)、铁抑素-1(货号17729)、U-0126(货号70970)、环己酰亚胺(货号14126)和β-巯基乙醇阻断。在HT-1080纤维肉瘤细胞和Calu-1肺癌细胞中,5μM的Erastin可通过xc⁻胱氨酸-谷氨酸转运系统抑制胱氨酸摄取,并在酶偶联荧光测定中抑制谷氨酸释放(半数有效浓度=1.2μM)。它还能选择性诱导表达SV40小T癌蛋白和致癌性Ras的细胞死亡(半数抑制浓度=1.25-5μg/ml)。2
Technical Information
Formal Name
2-[1-[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-quinazolinone
CAS Number
571203-78-6
Molecular Formula
C30H31ClN4O4
Formula Weight
547.1
Purity
≥98%
Formulation
A crystalline solid
Solubility
DMF: 10 mg/mlDMSO: 5 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml
λmax
225, 276, 304 nm
SMILES
O=C1C2=CC=CC=C2N=C(N1C3=CC=CC=C3OCC)C(N4CCN(CC4)C(COC5=CC=C(C=C5)Cl)=O)C
InChi Code
InChI=1S/C30H31ClN4O4/c1-3-38-27-11-7-6-10-26(27)35-29(32-25-9-5-4-8-24(25)30(35)37)21(2)33-16-18-34(19-17-33)28(36)20-39-23-14-12-22(31)13-15-23/h4-15,21H,3,16-20H2,1-2H3
InChi Key
BKQFRNYHFIQEKN-UHFFFAOYSA-N
参考文献:
[1] Yagoda N, von Rechenberg M, Zaganjor E, Bauer AJ, Yang WS, Fridman DJ, Wolpaw AJ, Smukste I, Peltier JM, Boniface JJ, Smith R, Lessnick SL, Sahasrabudhe S, Stockwell BR.RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels.Nature. 2007 Jun 14;447(7146):864-8.
[2] Dixon SJ, Lemberg KM, Lamprecht MR, Skouta R, Zaitsev EM, Gleason CE, Patel DN, Bauer AJ, Cantley AM, Yang WS, Morrison B 3rd, Stockwell BR.Ferroptosis: an iron-dependent form of nonapoptotic cell death.Cell. 2012 May 25;149(5):1060-72.
1. Weiyu Tian, Zijing Yang, et al. "SIRT3 mitigates osteoarthritis by suppressing ferroptosis through activating AMPK signaling pathway." Cell Signal. 2025 Aug 14:135:112063. PMID: 40818538
2. Mengyun Yang, Ze Yu, et al. "Targeting lipid scrambling potentiates ferroptosis and triggers tumor immune rejection." Sci Adv. 2025 Aug 15;11(33):eadx6587. PMID: 40815641
3. Tanvi Gupta, Shang-Rung Wu, et al. "Radiocleavable rare-earth nanoactivators targeting over-expressed folate receptors induce mitochondrial dysfunction and remodel immune suppressive microenvironment in pancreatic cancer." J Nanobiotechnology. 2025 Aug 12;23(1):562. PMID: 40797208
4. Amy E Stewart, Derek K Zachman, et al. "Pathway Coessentiality Map** Reveals Complex II is Required for de novo Purine Biosynthesis in Acute Myeloid Leukemia." bioRxiv. 2025 Mar 2:2025.02.26.640463. PMID: 40060603
5. Leif R Neitzel, Daniela T Fuller, et al. "Inhibition of GPR68 induces ferroptosis and radiosensitivity in diverse cancer cell types." Sci Rep.2025 Feb 3;15(1):4074. PMID: 39900965
6. Elizabeth Jose, Woody March-Steinman, et al. "Temporal coordination of the transcription factor response to H2O2 stress." Nat Commun. 2024 Apr 23;15(1):3440. PMID: 38653977
7. Xin Li, Yanan Hu, et al. "Exosomal let-7a-5p derived from human umbilical cord mesenchymal stem cells alleviates coxsackievirus B3-induced cardiomyocyte ferroptosis via the SMAD2." J Zhejiang Univ Sci B. 2024 May 15;25(5):422-437. PMID: 38725341
8. Chenyang Fan, Xiaohong Guo, et al. "BRD4 inhibitors broadly promote erastin-induced ferroptosis in different cell lines by targeting ROS and FSP1." Discov Oncol. 2024 Apr 3;15(1):98. PMID: 38565708
9. Chen-Yi Wang, Mu-Yu Li, et al. "Rack1‐mediated ferroptosis affects hindgut development in rats with anorectal malformations: Spatial transcriptome insights." Cell Prolif. 2024 Mar 25:e13618. PMID: 38523594
10. Miaomiao Shao, Kangwei Qi, et al. "E3 ubiquitin ligase CHIP interacts with transferrin receptor 1 for degradation and promotes cell proliferation through inhibiting ferroptosis in hepatocellular carcinoma." Cell Signal. 2024 Jun:118:111148. PMID: 38521179
11. Hong-Feng Gu, et al. "Artemisinin ameliorates cognitive decline by inhibiting hippocampal neuronal ferroptosis via Nrf2 activation in T2DM mice." Mol Med. 2024 Mar 7;30(1):35. PMID: 38454322
12. Charles C. Hong, et al. "GPR68-ATF4 signaling is a novel prosurvival pathway in glioblastoma activated by acidic extracellular microenvironment." Exp Hematol Oncol. 2024 Jan 31;13(1):13. PMID: 38291540
13. Zhi-Jun Ou, et al. "The oxidized phospholipid PGPC impairs endothelial function by promoting endothelial cell ferroptosis via FABP3." J Lipid Res. 2024 Feb;65(2):100499. PMID: 38218337
14. Yang Wang, Hongmei Ding, et al. "Alleviated NCOA4-mediated ferritinophagy protected RA FLSs from ferroptosis in lipopolysaccharide-induced inflammation under hypoxia." Inflamm Res. 2024 Mar;73(3):363-379. PMID: 38189810
15. Krishan Kumar Saini, Priyank Chaturvedi, et al. "Loss of PERK function promotes ferroptosis by downregulating SLC7A11 (System Xc⁻) in colorectal cancer." Redox Biol. 2023 Sep;65:102833. PMID: 37536085
16. Qingyu Zhang, Ning Li, et al. "ACSL1-induced ferroptosis and platinum resistance in ovarian cancer by increasing FSP1 N-myristylation and stability." Cell Death Discov. 2023 Mar 8;9(1):83. PMID: 36882396
17. Dong S, Zheng L, et al. "Loss of Lactate/Proton Monocarboxylate Transporter 4 Induces Ferroptosis via the AMPK/ACC Pathway and Inhibition of Autophagy on Human Bladder Cancer 5637 Cell Line" J Oncol 2023;2023 PMID: 36718218
18. Li J, Li W, et al. "Development and validation of a novel ferroptosis‑related lncRNA prognostic signature for pancreatic adenocarcinoma." Mol Med Rep 2023 Feb;27(2) PMID: 36660936
19. Yang Liu, Libo He, et al. "Pharmacological inhibition of sphingolipid synthesis reduces ferroptosis by stimulating the HIF-1 pathway." iScience. 2022 Jun 6;25(7):104533. PMID: 35784791
20. Weilin Liu, Hongqi Chen, et al. "Ferroptosis Inducer Improves the Efficacy of Oncolytic Virus-Mediated Cancer Immunotherapy." Biomedicines. 2022 Jun 15;10(6):1425. PMID: 35740445
21. Xinxin Ren, Xiang Wang, et al. "Integrative bioinformatics and experimental analysis revealed TEAD as novel prognostic target for hepatocellular carcinoma and its roles in ferroptosis regulation." Aging (Albany NY). 2022 Jan 25;14(2):961-974. PMID: 35077390
22. Zixin Zhu, Ya Zhang, et al. "Thymosin beta 4 alleviates non-alcoholic fatty liver by inhibiting ferroptosis via up-regulation of GPX4." Eur J Pharmacol. 2021 Oct 5;908:174351. PMID: 34280397
23. Zongbo Wei, Caili Hao, et al. "Aging lens epithelium is susceptible to ferroptosis." Free Radic Biol Med. 2021 May 1;167:94-108. PMID: 33722625
24. Xinzhi Yang, Jiangang Liu, et al. "miR-18a promotes glioblastoma development by down-regulating ALOXE3-mediated ferroptotic and anti-migration activities." Oncogenesis. 2021 Feb 12;10(2):15. PMID: 33579899
25. Ali Ghoochani, En-Chi Hsu, et al. "Ferroptosis inducers are a novel therapeutic approach for advanced prostate cancer." Cancer Res. 2021 Mar 15;81(6):1583-1594. PMID: 33483372
26. Zhijun Liu, Himani Nailwal, et al. "A class of viral inducer of degradation of the necroptosis adaptor RIPK3 regulates virus-induced inflammation." Immunity. 2021 Feb 9;54(2):247-258.e7. PMID: 33444549
27. Qi Wang, Yaxun Guo, et al. "RNA binding protein DAZAP1 promotes HCC progression and regulates ferroptosis by interacting with SLC7A11 mRNA." Exp Cell Res. 2021 Feb 1;399(1):112453. PMID: 33358859
28. Hu Z, Zhang H, et al. "VDR activation attenuate cisplatin induced AKI by inhibiting ferroptosis." Cell Death Dis. 2020;11(1):73. Published 2020 Jan 29. PMID: 31996668
29. Zhou HH, Chen X, et al. "Erastin Reverses ABCB1-Mediated Docetaxel Resistance in Ovarian Cancer." Front Oncol, 9, 1398 2019 Dec PMID: 31921655
30. Wang H, Liu C, et al. "Inhibition of LONP1 protects against erastin-induced ferroptosis in Pancreatic ductal adenocarcinoma PANC1 cells." Biochem Biophys Res Commun. 2019 Dec 7. pii: S0006-291X(19)32315-0. PMID: 31822343