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527450

Sigma-Aldrich

PKR Inhibitor

The PKR Inhibitor, also referenced under CAS 608512-97-6, controls the biological activity of PKR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

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Synonym(s):
PKR Inhibitor, Double-stranded RNA-dependent Protein Kinase Inhibitor, C16, Double-stranded RNA-activated Protein Kinase Inhibitor I, EIF2AK2 Inhibitor I
Empirical Formula (Hill Notation):
C13H8N4OS
CAS Number:
608512-97-6
Molecular Weight:
268.29
MDL number:
MFCD06735404

Quality Level

100

Assay

≥90% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange to orange-brown

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C13H8N4OS/c18-13-8(3-7-4-14-5-15-7)11-9(17-13)1-2-10-12(11)19-6-16-10/h1-6H,(H,14,15)(H,17,18)/b8-3-

InChI key

VFBGXTUGODTSPK-BAQGIRSFSA-N

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This Item
116805220485-M328006-M
PKR Inhibitor The PKR Inhibitor, also referenced under CAS 608512-97-6, controls the biological activity of PKR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

527450

PKR Inhibitor

Sigma-Aldrich

Sigma-Aldrich

116805

PKA Inhibitor 5-24

Chk2 Inhibitor The Chk2 Inhibitor, also referenced under CAS 724708-21-8, controls the biological activity of Chk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Millipore

220485-M

Chk2 Inhibitor

ERK Inhibitor The ERK Inhibitor, also referenced under CAS 1049738-54-6, controls the biological activity of ERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Millipore

328006-M

ERK Inhibitor

form

solid

form

lyophilized

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, desiccated (hygroscopic)

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

orange to orange-brown

color

-

color

pale yellow

color

light yellow

solubility

DMSO: 5 mg/mL

solubility

water: 1 mg/mL

solubility

DMSO: 100 mg/mL

solubility

DMSO: 10 mg/mL

General description

An imidazolo-oxindole compound that acts as a potent, ATP-binding site directed inhibitor of PKR. Shown to effectively inhibit RNA-induced PKR autophosphorylation (IC50 = 210 nM) and rescue PKR-dependent translation block (IC50 = 100 nM). Inactive control is also available (Cat. No. 527455). Shown to increase the late phase of long-lasting synaptic potentiation, and enhance long-term memory in mice. Also available as a 50 mM solution in DMSO (Cat. No. 527451).
An imidazolo-oxindole compound that acts as a potent, ATP-binding site directed inhibitor of PKR. Shown to effectively inhibit RNA-induced PKR autophosphorylation (IC50 = 210 nM) and rescue PKR-dependent translation block (IC50 = 100 nM). Shown to increase the late phase of long-lasting synaptic potentiation, and enhance long-term memory in mice. Inactive control is also available (Cat. No. 527455).

Biochem/physiol Actions

Cell permeable: no
Primary Target
PKR
Product does not compete with ATP.
Reversible: no
Target IC50: 210 nM inhibiting RNA-induced PKR autophosphorylation and 100 nM in rescuing PKR-dependent translation block

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

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

Other Notes

Zhu, P.J., et al. 2011. Cell147, 1384.
Jammi, N.V., et al. 2003. Biochem. Biophys. Res. Commun.308, 50.

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

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