Этиловый эфир 2-амино-6-хлор-α-циано-3- (этоксикарбонил) -4H-1-бензопиран-4-уксусной кислоты

Описание

SC-79 is an activator of Akt that blocks its membrane translocation while allowing its phosphorylation, in the cytosol, by upstream kinases. For example, both Thr³⁰⁸ and Ser⁴⁷³ on Akt are phosphorylated in serum starved HeLa cells treated for 1 hour with insulin growth factor and SC-79 (4 μg/ml). SC-79 permits phosphorylation and activation of all isoforms of Akt, it is active in multiple cell types, and works in both receptor tyrosine kinase- and G protein-coupled receptor-mediated signaling. SC-79 has been used to elucidate the role of Akt signaling in neuronal survival, glucose-mediated apoptosis in podocytes, and miR-221-regulated cancer cell proliferation.

Использование

SC79 has been used in western blot analysis as a positive control to measure the extent of phosphorylation of Akt and also to activate Akt that has been suppressed by nitidine chloride, a natural bioactive alkaloid.

Общее описание

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.