529598

PP1 Analog IV, 3-IB-PP1

A cell-permeable enlarged PP1 analog that acts as a potent, ATP-competitive and reversible inhibitor of asAkt1/2/3.

• Synonym(s): PP1 Analog IV, 3-IB-PP1, 3-Iodobenzyl PP1 analog
• Empirical Formula (Hill Notation): C₁₆H₁₈IN₅
• CAS Number: 1174182-24-1
• Molecular Weight: 407.25
• UNSPSC Code: 12352202
• NACRES: NA.77
• MDL number: MFCD32633399
• Assay: ≥97% (HPLC)
• Form: powder
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 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
• InChI: 1S/C16H18IN5/c1-16(2,3)22-15-13(14(18)19-9-20-15)12(21-22)8-10-5-4-6-11(17)7-10/h4-7,9H,8H2,1-3H3,(H2,18,19,20)
• InChI key: CVRIGUMSLGSWEZ-UHFFFAOYSA-N

Description

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)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable