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123871 Sigma-Aldrich

Akt Activator II, SC79 - CAS 305834-79-1 - Calbiochem

Akt Activator II, SC79, CAS 305834-79-1, is a cell-permeable compound that interacts with Akt PH domain PIP3 binding pocket and makes it more susceptible to phosphorylation by upstream Kinases.

Synonym: Akt Activator II, SC79 - CAS 305834-79-1 - Calbiochem, Ethyl-2-amino-6-chloro-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate

  • CAS Number 305834-79-1

  • Empirical Formula (Hill Notation) C17H17ClN2O5

  • Molecular Weight 364.78

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Properties

Quality Level   100
assay   ≥98% (sum of two isomers, HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   -20C
color   off-white
solubility   DMSO: 50 mg/mL
shipped in   ambient

Description

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.

Packaging

25 mg in Glass bottle

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.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.

Documents

Certificate of Analysis (COA)

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