Merck, 123871-25MG, Akt Activator II, SC79

General description
A cell-permeable and blood-brain barrier permeant bromo-to-chloro substituted HA14-1 analog that renders Akt in a conformation susceptible to phosphorylation by upstream kinases via specific interaction with Akt pleckstrin homology (PH) domain PtdIns(3,4,5)P3- (PIP3) binding pocket. Shown to enhance both basal and receptor-mediated Akt phosphorylation (Thr308 and Ser473) in a time- and dose-dependent manner (2 to 4 µg/ml) with concomitant inhibition Akt membrane translocation in various cell cultures. Efficiently reduces glutamate-induced neurotoxicity both in primary neuron cultures (EC₅₀ = 4 µg/ml) in vitro and in a murine MCAO (middle cerebral artery occlusion) model (40 mg/kg, i.p.) in vivo.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Pleckstrin homology (PH) domain of Akt
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and immediately freeze (-70°C). Stock solutions are stable for up to 2 weeks at -70°C.
Use only fresh DMSO for reconstitution.
Other Notes
Jo. H., et al. 2012. Proc. Natl. Acad. Sci. USA109, 10581.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)