General description
A cell-permeable hydrazone compound that reversibly binds eukaryotic translation initiation factor 4E (eIF4E; KD = 25 µM) and disrupts eIF4E/eIF4G, but not eIF4E/4E-BP1, complex formation. Reported to downregulate the protein, but not mRNA, levels of c-Myc and Bcl-xL in Jurkat cells (8 hrs), leading to apoptotic cell death after prolonged exposure (24 hrs, IC50 ~25 µM). Shown to be brain permeant and reduce neuroligin protein levels, and restore L-LTP threshold and rescue autistic-like behaviours in Eif4ebp2 knockout mice.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
eIF4E
Reversible: yes
Packaging
Packaged under inert gas
Physical form
A 25 mM (5 mg/443 µL) solution of eIF4E/eIF4G Interaction Inhibitor, 4EGI-1 (Cat. No. 324517)
Preparation Note
Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.
Other Notes
Gkogkas, C.G., et al. 2012. Nature493, 371.
Moerke, N. J., et al. 2007. Cell128, 257.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
| Quality Segment | 100 |
| assay | ≥95% (sum of two isomers, HPLC) |
| form | liquid |
| potency | 25 μM Ki |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,avoid repeated freeze/thaw cycles,desiccated (hygroscopic),protect from light |
| shipped in | dry ice |
| storage temp. | −70°C |
| InChI | 1S/C18H12Cl2N4O4S/c19-12-6-5-10(7-13(12)20)15-9-29-18(21-15)23-22-14(17(25)26)8-11-3-1-2-4-16(11)24(27)28/h1-7,9H,8H2,(H,21,23)(H,25,26)/b22-14+ |
| InChI key | KFRKRECSIYXARE-HYARGMPZSA-N |
