Merck, 529598-10MG, PP1 Analog IV, 3-IB-PP1

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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Schoenborn, J.R., et al. 2011. Sci. Signal.4, ra59.
Okuzumi, T., et al. 2009. Nat. Chem. Bio.5, 484.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)