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
• 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: liquid
• Storage condition: OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

Properties

• Quality Segment: 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
• 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). 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

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.

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: Irritant (B)

Safety Information

• 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)