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Key Documents

527451

Sigma-Aldrich

PKR Inhibitor

InSolution, ≥90%

Synonym(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

Empirical Formula (Hill Notation):
C13H8N4OS
CAS Number:
Molecular Weight:
268.29
MDL number:
UNSPSC Code:
12352200

Quality Level

Assay

≥90% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

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

shipped in

dry ice

storage temp.

−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-

InChI key

VFBGXTUGODTSPK-BAQGIRSFSA-N

General description

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PKR
Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical form

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.

Other Notes

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

Legal Information

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

Certificates of Analysis (COA)

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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
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

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