General description
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.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Pleckstrin homology (PH) domain of Akt
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
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.
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
- UPC:
- 41141922
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 123871-25MG