527450

Imidazolo-oxindole PKR inhibitor C16

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

• Synonyma: PKR Inhibitor, Double-stranded RNA-dependent Protein Kinase Inhibitor, C16, Double-stranded RNA-activated Protein Kinase Inhibitor I, EIF2AK2 Inhibitor I
• Empirický vzorec (Hillův zápis): C₁₃H₈N₄OS
• Číslo CAS: 608512-97-6
• Molekulová hmotnost: 268.29
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD06735404
• Assay: ≥90% (HPLC)
• Form: solid
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Vlastnosti

• Název produktu: 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
• 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

Popis

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)

Bezpečnostní informace

• Skladovací třída: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable