Erastin Inhibitor CAS No. 571203-78-6

Cat. No.	Name	Size	Price	Add Cart
KI3671	Erastin	5 mg	$250
KI3671	Erastin	50 mg	$1310

Chemical Characteristic

Product Name	Erastin
CAS No.	571203-78-6
Molecular Weight	547.04
Formula	C₃₀H₃₁ClN₄O₄
Chemical Name	2-[1-[4-[2-(4-Chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-quinazolinone
Smiles	n1c(n(c(=O)c2ccccc12)c1c(cccc1)OCC)C(C)N1CCN(CC1)C(=O)COc1ccc(cc1)Cl
Chemical Structure

Biological activities

Erastin is a compound that interacts with VDAC, blocked and reversed mitochondrial depolarization after microtubule destabilizers in intact cells and antagonized tubulin-induced VDAC blockage in planar bilayers ^[1]. Voltage-dependent anion channels are a class of porin ion channel located on the outer mitochondrial membrane. This major protein of the outer mitochondrial membrane of eukaryotes forms a voltage-dependent anion-selective channel (VDAC) that behaves as a general diffusion pore for small hydrophilic molecules. Erastin induced RAS-RAF-MEK-dependent non-apoptotic cell death via VDAC2. In vitro, the IC50 of erastin to VDAC2 is 0.1 ?M ^[2]. Erastin can be used by 5 or 10 ?g/mL with 6-11 hours in BJ-TERT/LT/ST/RASV12 cells ^[3].

References

[1] Simamura E, Shimada H, Hatta T, et al. Mitochondrial voltage-dependent anion channels (VDACs) as novel pharmacological targets for anti-cancer agents. J Bioenerg Biomembr. 2008, 40(3):213-217. [2] Maldonado EN, Sheldon KL, DeHart DN, et al. Voltage-dependent anion channels modulate mitochondrial metabolism in cancer cells: regulation by free tubulin and erastin. J Biol Chem. 2013, 288(17):11920-11929. [3] Dixon SJ, Lemberg KM, Lamprecht MR, et al. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012, 149(5):1060-1072.

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