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Merck

5.31551

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:
101068-35-3
Molecular Weight:
312.27
MDL number:
MFCD00006395
NACRES:
NA.77
UNSPSC Code:
12352200

assay

≥98% (HPLC)

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

Quality Level

100

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PKR and PERK

Disclaimer

Toxicity: Standard Handling (A)

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).

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

Other Notes

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

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.

Legal Information

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

Storage Class

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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Global Trade Item Number

SKUGTIN
5.31551.000104055977260373

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