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Merck

527451

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:
608512-97-6
Molecular Weight:
268.29
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD06735404

Key Documents

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Product Name

PKR Inhibitor, InSolution, ≥90%

SMILES string

[s]1c2c(nc1)ccc3c2\C(=C\c4nc[nH]c4)\C(=O)N3

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

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

Quality Level

100

Related Categories

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.

Other Notes

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

Packaging

Packaged under inert gas

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PKR
Reversible: yes

Disclaimer

Toxicity: Irritant (B)

Physical form

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

Preparation Note

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

Legal Information

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

Storage Class

10 - Combustible liquids

wgk

WGK 2

flash_point_f

188.6 °F - closed cup - (Dimethylsulfoxide)

flash_point_c

87 °C - closed cup - (Dimethylsulfoxide)

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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

Global Trade Item Number

SKUGTIN
527451-5MGCN04055977270372

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