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5.31551

Sigma-Aldrich

PKR/PERK Activator, DHBDC

Synonym(s):

PKR/PERK Activator, DHBDC, Protein Kinase R (PKR) Activator, Protein Kinase R Like Kinase (PERK) Activator

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About This Item

Empirical Formula (Hill Notation):
C17H12O6
CAS Number:
Molecular Weight:
312.27
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

Quality Level

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: 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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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