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Merck

SML2794

Erastin2

≥98% (HPLC), xc- Cystine/Glutamate transporter system inhibitor, powder

Sinónimos:

2-((4-(2-(4-Chlorophenoxy)acetyl)piperazin-1-yl)methyl)-3-(4-isopropoxybiphenyl-3-yl)quinazolin-4(3H)-one, 2-[[4-[2-(4-Chlorophenoxy)acetyl]-1-piperazinyl]methyl]-3-[4-(1-methylethoxy)[1,1′-biphenyl]-3-yl]-4(3H)-quinazolinone, 35MEW28

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Acerca de este artículo

Fórmula empírica (notación de Hill):
C36H35ClN4O4
Número CAS:
Peso molecular:
623.14
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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Nombre del producto

Erastin2, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C(N(C1=C(OC(C)C)C=CC(C2=CC=CC=C2)=C1)C(CN3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)=N5)C6=C5C=CC=C6

Biochem/physiol Actions

Erastin analog with greatly improved system xc- (SLC7A11/xCT + SLC3A2/4F2hc) inhibitory potency and ferropotosis induction efficacy
Erastin2 is an Erastin analog with greatly improved system xc- (SLC7A11/xCT + SLC3A2/4F2hc) inhibitory potency (Erastin2 IC50 = 3.5 nM/CCF-STTG1; Erastin IC50 = 200 nM/HT-1080, 140 nM/Calu-1; Glu release assay) and ferropotosis induction efficacy (HT-1080 EC50 = 150 nM/Erastin2 vs. 1.2 μM/Erastin).

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Allegra T Aron et al.
Journal of the American Chemical Society, 138(43), 14338-14346 (2016-11-03)
Iron is essential for sustaining life, as its ability to cycle between multiple oxidation states is critical for catalyzing chemical transformations in biological systems. However, without proper regulation, this same redox capacity can trigger oxidative stress events that contribute to
Amy Tarangelo et al.
Cell reports, 22(3), 569-575 (2018-01-19)
How cancer cells respond to nutrient deprivation remains poorly understood. In certain cancer cells, deprivation of cystine induces a non-apoptotic, iron-dependent form of cell death termed ferroptosis. Recent evidence suggests that ferroptosis sensitivity may be modulated by the stress-responsive transcription
Mariana Figuera-Losada et al.
Biochemistry and biophysics reports, 9, 266-272 (2017-09-29)
The inflammatory response in the central nervous system involves activated microglia. Under normal conditions they remove damaged neurons by phagocytosis. On the other hand, neurodegenerative diseases are thought to involve chronic microglia activation resulting in release of excess glutamate, proinflammatory
Bei Liu et al.
Biochemical and biophysical research communications, 497(1), 233-240 (2018-02-11)
Heart failure (HF) is the end stage of cardiovascular disease and is characterized by the loss of myocytes caused by cell death. Puerarin has been found to improve HF clinically, and animal study findings have confirmed its anti-cell-death properties. However
Scott J Dixon et al.
eLife, 3, e02523-e02523 (2014-05-23)
Exchange of extracellular cystine for intracellular glutamate by the antiporter system xc (-) is implicated in numerous pathologies. Pharmacological agents that inhibit system xc (-) activity with high potency have long been sought, but have remained elusive. In this study

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