Erastin (CAS 571203-78-6)
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Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations. It is shown to bind mitochondrial volatage-dependent anion channels (VDAC) and alter its gating Erastin rapidly induces an oxidative, non-apoptotic cell death in several human tumors harboring activating mutations in the RAS-RAF-MEK signaling. It has been found to induce the expression of pro-apoptotic proteins, such as Bax and caspases, and inhibit the expression of anti-apoptotic proteins, such as Bcl-2 and XIAP. Additionally, it is a member of the ruthenium red family of compounds and is a potent inhibitor of the cysteine-dependent redox enzyme thioredoxin reductase (TrxR). Erastin has been found to have a wide range of biological activities, including anti-inflammatory, anti-cancer, and anti-apoptotic effects.
Erastin (CAS 571203-78-6) References
- RAS-RAF-MEK-dependent oxidative cell death involving voltage-dependent anion channels. | Yagoda, N., et al. 2007. Nature. 447: 864-8. PMID: 17568748
- Protective effects of the mechanistic target of rapamycin against excess iron and ferroptosis in cardiomyocytes. | Baba, Y., et al. 2018. Am J Physiol Heart Circ Physiol. 314: H659-H668. PMID: 29127238
- ENPP2 protects cardiomyocytes from erastin-induced ferroptosis. | Bai, YT., et al. 2018. Biochem Biophys Res Commun. 499: 44-51. PMID: 29551679
- ATF3 promotes erastin-induced ferroptosis by suppressing system Xc. | Wang, L., et al. 2020. Cell Death Differ. 27: 662-675. PMID: 31273299
- Dosing Time-Dependent Changes in the Anti-tumor Effect of xCT Inhibitor Erastin in Human Breast Cancer Xenograft Mice. | Shiromizu, S., et al. 2019. Biol Pharm Bull. 42: 1921-1925. PMID: 31685775
- Erastin, a ferroptosis-inducing agent, sensitized cancer cells to X-ray irradiation via glutathione starvation in vitro and in vivo. | Shibata, Y., et al. 2019. PLoS One. 14: e0225931. PMID: 31800616
- Nedd4 ubiquitylates VDAC2/3 to suppress erastin-induced ferroptosis in melanoma. | Yang, Y., et al. 2020. Nat Commun. 11: 433. PMID: 31974380
- Inhibitor of apoptosis-stimulating protein of p53 inhibits ferroptosis and alleviates intestinal ischemia/reperfusion-induced acute lung injury. | Li, Y., et al. 2020. Cell Death Differ. 27: 2635-2650. PMID: 32203170
- The Role of Erastin in Ferroptosis and Its Prospects in Cancer Therapy. | Zhao, Y., et al. 2020. Onco Targets Ther. 13: 5429-5441. PMID: 32606760
- NCOA4-mediated ferritinophagy promotes ferroptosis induced by erastin, but not by RSL3 in HeLa cells. | Gryzik, M., et al. 2021. Biochim Biophys Acta Mol Cell Res. 1868: 118913. PMID: 33245979
- Erastin induces ferroptosis via ferroportin-mediated iron accumulation in endometriosis. | Li, Y., et al. 2021. Hum Reprod. 36: 951-964. PMID: 33378529
- Ferroptosis inducer erastin sensitizes NSCLC cells to celastrol through activation of the ROS-mitochondrial fission-mitophagy axis. | Liu, M., et al. 2021. Mol Oncol. 15: 2084-2105. PMID: 33675143
- Erastin‑induced ferroptosis causes physiological and pathological changes in healthy tissues of mice. | Zhao, J., et al. 2021. Mol Med Rep. 24: PMID: 34396451
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Erastin, 5 mg | sc-205677 | 5 mg | $372.00 | |||
Erastin, 50 mg | sc-205677A | 50 mg | $1614.00 |