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Merck
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Key Documents

324879

Sigma-Aldrich

CCT020312

≥98% (HPLC), solid, EIF2AK3 activator, Calbiochem®

Sinonimo/i:

EIF2AK3 Activator, CCT020312, 6-Bromo-3-[5-(4-bromo-phenyl)-1-(3-diethylamino-propionyl)-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl-1H-quinolin-2-one, PERK activator, CCT020312

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About This Item

Formula empirica (notazione di Hill):
C31H30Br2N4O2
Numero CAS:
Peso molecolare:
650.40
Numero MDL:
Codice UNSPSC:
12352200
NACRES:
NA.77

product name

EIF2AK3 Activator, CCT020312, The EIF2AK3 Activator, CCT020312 modulates the biological activity of EIF2AK3.

Livello qualitativo

Saggio

≥98% (HPLC)

Forma fisica

solid

Produttore/marchio commerciale

Calbiochem®

Condizioni di stoccaggio

OK to freeze
protect from light

Colore

yellow-white

Solubilità

DMSO: 50 mg/mL

Condizioni di spedizione

ambient

Temperatura di conservazione

−20°C

Stringa SMILE

O=C1C(C2=NN(C(CCN(CC)CC)=O)C(C3=CC=C(Br)C=C3)C2)=C(C4=CC=CC=C4)C5=CC(Br)=CC=C5N1

Descrizione generale

A dihydropyrazol derivative that acts as a selective activator of eukaryotic translation initiation factor 2-alpha kinase 3 (EIF2AK3/PERK) and increases the phosphorylation of EIF2A at Ser51 in HT29 and MCF7 cells. Does not inhibit the activity of cyclin dependent kinases, but causes a rapid loss of cyclin D expression. Also shown to block Rb protein phosphorylation (EC50 = 4.2 µM) in HT29 cells. Reported to sensitize cancer cells with defective taxane-induced EIF2A phosphorylation to paclitaxel treatment. Induces a long-term inhibition of cell proliferation even after its removal (GI50 = 3.1 µM).

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Altre note

Stockwell, S. R., et al. 2011. Plos One In press.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 2

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


Certificati d'analisi (COA)

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Shin-Ichi Ikeda et al.
Nature communications, 13(1), 5859-5859 (2022-10-11)
Axial length is the primary determinant of eye size, and it is elongated in myopia. However, the underlying mechanism of the onset and progression of axial elongation remain unclear. Here, we show that endoplasmic reticulum (ER) stress in sclera is
Simon R Stockwell et al.
PloS one, 7(1), e28568-e28568 (2012-01-19)
Human cancers often contain genetic alterations that disable G1/S checkpoint control and loss of this checkpoint is thought to critically contribute to cancer generation by permitting inappropriate proliferation and distorting fate-driven cell cycle exit. The identification of cell permeable small
Himanshu Soni et al.
Oncogenesis, 9(2), 18-18 (2020-02-15)
PKR-like kinase (PERK) plays a significant role in inducing angiogenesis in various cancer types including glioblastoma. By proteomics analysis of the conditioned medium from a glioblastoma cell line treated with a PERK inhibitor, we showed that peptidylglycine α-amidating monooxygenase (PAM)
Kai Chen et al.
Aging cell, 21(4), e13592-e13592 (2022-03-18)
Delirium is the most common postoperative complication in older patients after prolonged anesthesia and surgery and is associated with accelerated cognitive decline and dementia. The neuronal pathogenesis of postoperative delirium is largely unknown. The unfolded protein response (UPR) is an

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