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527450

Imidazolo-oxindole PKR inhibitor C16

Name: Imidazolo-oxindole PKR inhibitor C16
Brand: MM

≥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

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD06735404

Assay:

≥90% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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Properties

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 Segment

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

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

Description

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. 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).

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

Preparation Note

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

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

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Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c