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Beschreibung

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 µ,g/ml) with concomitant inhibition Akt membrane translocation in various cell cultures. Efficiently reduces glutamate-induced neurotoxicity both in primary neuron cultures (EC50 = 4 µ,g/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 µ,g/ml) with concomitant inhibition Akt membrane translocation in various cell cultures. Efficiently reduces glutamate-induced neurotoxicity both in primary neuron cultures (EC50 = 4 µ,g/ml) in vitro and in a murine MCAO model (40 mg/kg, i.p.) in vivo.