All Photos(2)
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
Empirical Formula (Hill Notation):
C13H8N4OS
CAS Number:
Molecular Weight:
268.29
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
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
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.
Jammi, N.V., et al. 2003. Biochem. Biophys. Res. Commun.308, 50.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
Flash Point(F)
188.6 °F
Flash Point(C)
87 °C
Certificates of Analysis (COA)
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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
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