5.31551

PKR/PERK Activator, DHBDC

• Synonym(s): PKR/PERK Activator, DHBDC, Protein Kinase R (PKR) Activator, Protein Kinase R Like Kinase (PERK) Activator
• Empirical Formula (Hill Notation): C₁₇H₁₂O₆
• Molecular Weight: 312.27

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• potency: ~10 μM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: pink
• solubility: DMSO: 100 mg/mL
• storage temp.: −20°C

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PKR and PERK

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable