Akt Activator II; SC79

Biochem/physiol Actions

Primary TargetPleckstrin homology (PH) domain of Akt

Cell permeable: yes

General description

A cell-permeable and blood-brain barrier permeant bromo-to-chloro substituted HA14-1 (Cat. No. 371971) 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.

A cell-permeable and blood-brain barrier permeant HA14-1 (Cat. No. 371971) analog that interacts with Akt PH domain PtdIns(3,4,5)P3- (PIP3) binding pocket, rendering Akt in a conformation susceptible to phosphorylation by upstream kinases. Shown to enhance both basal and receptor-mediated Akt phosphorylation (Thr308 and Ser473; 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 model (40 mg/kg, i.p.) in vivo.

Legal Information

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

Other Notes

Jo. H., et al. 2012. Proc. Natl. Acad. Sci. USA109, 10581.

Packaging

25 mg in Glass bottle

Packaged under inert gas

Reconstitution

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.

Warning

Toxicity: Standard Handling (A)