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). The solid form of this compound (Cat. No. 527450 ) is also available.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PKR
Reversible: yes
Packaging
Packaged under inert gas
Physical form
A 50 mM (5 mg/373 µL) solution of PKR Inhibitor (Cat. No. 527450 ) in DMSO.
Preparation Note
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 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
Disclaimer
Toxicity: Irritant (B)
| Quality Segment | 100 |
| assay | ≥90% (HPLC) |
| form | liquid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,avoid repeated freeze/thaw cycles,desiccated (hygroscopic),protect from light |
| shipped in | dry ice |
| storage temp. | −20°C |
| SMILES string | [s]1c2c(nc1)ccc3c2\C(=C\c4nc[nH]c4)\C(=O)N3 |
| 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 |
