General description

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 µM). 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-3βSer⁹ 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 µM) 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 µM). 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-3βSer⁹ 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 µM) and rapidly activates T cell receptor signaling.

Legal Information

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

Other Notes

Schoenborn, J.R., et al. 2011. Sci. Signal.4, ra59.Okuzumi, T., et al. 2009. Nat. Chem. Bio.5, 484.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)