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Key Documents

527451

Sigma-Aldrich

PKR Inhibitor

InSolution, ≥90%

Synonyme(s) :

InSolution PKR Inhibitor, Double-stranded RNA-activated Protein Kinase Inhibitor I, Double-stranded RNA-dependent Protein Kinase Inhibitor I, EIF2AK2 Inhibitor I, C16

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About This Item

Formule empirique (notation de Hill):
C13H8N4OS
Numéro CAS:
Poids moléculaire :
268.29
Numéro MDL:
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

Pureté

≥90% (HPLC)

Forme

liquid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
avoid repeated freeze/thaw cycles
desiccated (hygroscopic)
protect from light

Conditions d'expédition

dry ice

Température de stockage

−20°C

InChI

1S/C13H8N4OS/c18-13-8(3-7-4-14-5-15-7)11-9(17-13)1-2-10-12(11)19-6-16-10/h1-6H,(H,14,15)(H,17,18)/b8-3-

Clé InChI

VFBGXTUGODTSPK-BAQGIRSFSA-N

Description générale

An imidazolo-oxindole compound that acts as a potent, ATP-binding site directed inhibitor of PKR. Shown to effectively inhibit RNA-induced PKR autophosphorylation (IC50 = 210 nM) and rescue PKR-dependent translation block (IC50 = 100 nM). The solid form of this compound (Cat. No. 527450) is also available.

Actions biochimiques/physiologiques

Cell permeable: yes
Primary Target
PKR
Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Irritant (B)

Forme physique

A 50 mM (5 mg/373 µL) solution of PKR Inhibitor (Cat. No. 527450) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C.

Autres remarques

Zhu, P.J., et al. 2011. Cell147, 1384.
Jammi, N.V., et al. 2003. Biochem. Biophys. Res. Commun.308, 50.

Informations légales

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

Code de la classe de stockage

10 - Combustible liquids

Classe de danger pour l'eau (WGK)

WGK 2

Point d'éclair (°F)

188.6 °F - closed cup - (Dimethylsulfoxide)

Point d'éclair (°C)

87 °C - closed cup - (Dimethylsulfoxide)


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Consulter la Bibliothèque de documents

Narasimham V Jammi et al.
Biochemical and biophysical research communications, 308(1), 50-57 (2003-08-02)
The RNA-dependent protein kinase (PKR) is an interferon-induced serine/threonine protein kinase that phosphorylates the alpha subunit of the eukaryotic initiation factor 2 in response to viral infection. Classical genetic approaches for studying the role of PKR in cell signaling have
Harikrishnan Radhakrishnan et al.
Bioengineering & translational medicine, 9(1), e10605-e10605 (2024-01-09)
Primary T cell has been transformed into a cell-based delivery platform that synthesizes complex biologics at the disease site with spatiotemporal resolution. This broadly applicable technology can circumvent toxicities due to systemic administration of biologics that necessitates the use of
Ping Jun Zhu et al.
Cell, 147(6), 1384-1396 (2011-12-14)
The double-stranded RNA-activated protein kinase (PKR) was originally identified as a sensor of virus infection, but its function in the brain remains unknown. Here, we report that the lack of PKR enhances learning and memory in several behavioral tasks while
Mor Angel et al.
Nucleic acids research, 52(9), 5356-5375 (2024-02-17)
Stress granules (SGs) are cytoplasmic assemblies formed under various stress conditions as a consequence of translation arrest. SGs contain RNA-binding proteins, ribosomal subunits and messenger RNAs (mRNAs). It is well known that mRNAs contribute to SG formation; however, the connection between SG

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