Sigma-Aldrich Pkr/Perk Activator Dhbdc

Assay

≥98% (HPLC)

Quality Level

100

Form

powder

Potency

~10 μM IC₅₀

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

white to pink

Solubility

DMSO: 100 mg/mL

Storage Temp.

−20°C

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: yesPrimary 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.ChemBioChem 14,1255.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany