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527450

Sigma-Aldrich

Imidazolo-oxindole PKR inhibitor C16

≥90% (HPLC), solid, PKR inhibitor, Calbiochem®

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C13H8N4OS
CAS Number:
608512-97-6
Molecular Weight:
268.29
MDL number:
MFCD06735404
UNSPSC Code:
12352200
NACRES:
NA.77

product name

PKR Inhibitor, The PKR Inhibitor, also referenced under CAS 608512-97-6, controls the biological activity of PKR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Quality Level

100

Assay

≥90% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange to orange-brown

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°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). Inactive control is also available (Cat. No. 527455). Shown to increase the late phase of long-lasting synaptic potentiation, and enhance long-term memory in mice. Also available as a 50 mM solution in DMSO (Cat. No. 527451).
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). Shown to increase the late phase of long-lasting synaptic potentiation, and enhance long-term memory in mice. Inactive control is also available (Cat. No. 527455).

Biochem/physiol Actions

Cell permeable: no
Primary Target
PKR
Product does not compete with ATP.
Reversible: no
Target IC50: 210 nM inhibiting RNA-induced PKR autophosphorylation and 100 nM in rescuing PKR-dependent translation block

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

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

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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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