527451

InSolution PKR Inhibitor

The InSolution 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.

• 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: 608512-97-6
• Molecular Weight: 268.29
• MDL number: MFCD06735404

Properties

• Quality Level: 100
• 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

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). 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