PP1 Analog IV, 3-IB-PP1 - Calbiochem (C15-1304-972)

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Molecular Weight: 407.25. Empirical Formula: C₁₆H₁₈IN₅. Quality Level: 100. Assay: ≥. 97% (HPLC). form: powder. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 0.5 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. SMILES string: NC1: NC: NC2: C1C(CC3: CC(I): CC: C3): NN2C(C)(C)C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.