5.31551

PKR/PERK Activator, DHBDC

• Synonyme(s) : PKR/PERK Activator, DHBDC, Protein Kinase R (PKR) Activator, Protein Kinase R Like Kinase (PERK) Activator
• Formule empirique (notation de Hill): C₁₇H₁₂O₆
• Numéro CAS: 101068-35-3
• Poids moléculaire : 312.27
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: ~10 μM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white to pink
• Solubilité: DMSO: 100 mg/mL
• Température de stockage: −20°C

Description

Description générale

A cell permeable chromenone derivative that acts as a dual activator of protein kinase R (PKR) and protein kinase R like kinase (PERK). Induces the phosphorylation of IkBa and thereby activates NF-κB pathway. However, the activation of NF-κB is independent of PKR activity. Induces elF2a phosphorylation and activates its downstream effectors CHOP/GADD153. Does not affect the phosphorylation of Akt, MAP kinase, or 4E-BP1. Inhibits the expression of cyclin D1 and E and blocks the growth of CRL-2813 and MCF-7 cells (IC₅₀ = ~ 10 µM). Also shown to reduce JFH1 hepatitis C virus infectivity (~40% inhibition at 5 µM).

A cell permeable chromenone derivative that acts as a dual activator of protein kinase R (PKR) and protein kinase R like kinase (PERK). Induces the phosphorylation of IkBa and thereby activates NF-κB pathway. However, the activation of NF-κB is independent of PKR activity. Induces elF2a phosphorylation and activates its downstream effectors CHOP/GADD153. Does not affect the phosphorylation of Akt, MAP kinase, or 4E-BP1. Inhibits the expression of cyclin D1 and E and blocks the growth of CRL-2813 and MCF-7 cells (IC₅₀ = ~ 10 µM). Also shown to reduce JFH1 hepatitis C virus infectivity (~40% inhibition at 5 µM).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
PKR and PERK

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

Bai, H., et al. 2013. ChemBioChem14, 1255.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable