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Beschreibung

A cell-permeable enlarged PP1 (Cat. No. 567809) analog that acts as a potent, ATP-competitive and reversible inhibitor of asAkt1/2/3 (IC50 = 28, 240 and 120 nM, respectively) over wtAkt1/2/3 (IC50 = >10 µ,M). Shown to hyperphosphorylate Akt-Ser473 and -Thr308 in HEK293 cells coexpressed with myr-HA-asAkt1 or myr-HA-asAkt1/2/3 with no effect on pGSK-3betaSer9 levels and wtAkt expressing cells. Also, specifically blocks the inhibitory function of membrane asCsk with diminished activity towards wtCsk, induces phosphorylation of Lck-Tyr394 and ERK1/2 in primary mouse T cells (EC50 ~0.5 µ,M) and rapidly activates T cell receptor signaling., A cell-permeable enlarged PP1 (Cat. No. 567809) analog that acts as a potent, ATP-competitive and reversible inhibitor of asAkt1/2/3 (IC50 = 28, 240 and 120 nM, respectively) over wtAkt1/2/3 (IC50 = >10 µ,M). Shown to hyperphosphorylate Akt-Ser473 and -Thr308 in HEK293 cells coexpressed with myr-HA-asAkt1 or myr-HA-asAkt1/2/3 with no effect on pGSK-3betaSer9 levels and wtAkt expressing cells. Also, specifically blocks the inhibitory function of membrane asCsk with diminished activity towards wtCsk, induces phosphorylation of Lck-Tyr394 and ERK1/2 in primary mouse T cells (EC50 ~0.5 µ,M) and rapidly activates T cell receptor signaling.

Strukturformel

SAF-529598-10MG

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