123871

Akt Activator II, SC79

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.

• Synonyme(s) : Akt Activator II, SC79, Ethyl-2-amino-6-chloro-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
• Formule empirique (notation de Hill): C₁₇H₁₇ClN₂O₅
• Numéro CAS: 305834-79-1
• Poids moléculaire : 364.78
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (sum of two isomers, HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• InChI: 1S/C17H17ClN2O5/c1-3-23-16(21)11(8-19)13-10-7-9(18)5-6-12(10)25-15(20)14(13)17(22)24-4-2/h5-7,11,13H,3-4,20H2,1-2H3
• Clé InChI: DXVKFBGVVRSOLI-UHFFFAOYSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Pleckstrin homology (PH) domain of Akt

Conditionnement

Packaged under inert gas

Avertissement

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.

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable