559274

S6K1 Inhibitor II, DG2

The S6K1 Inhibitor II, DG2 controls the biological activity of S6K1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): S6K1 Inhibitor II, DG2, 3-Bromo-4-(4-(2-methoxyphenyl)piperazin-1-yl)-1H-pyrazolo[3,4-d]-pyrimidine
• Empirical Formula (Hill Notation): C₁₆H₁₇BrN₆O
• CAS Number: 871340-88-4
• Molecular Weight: 389.25
• MDL number: MFCD22580420
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL, clear, pale yellow
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: BrC1=NNC2=C1C(N(CC3)CCN3C4=C(C=CC=C4)OC)=NC=N2

Description

General description

A cell-permeable pyrazolopyrimidine compound that acts as a potent, ATP-competitive and reversible inhibitor of S6K1 (p70 ribosomal protein S6 kinase 1; IC₅₀ = 9.1 nM) with ~2,400 reduced activity towards Akt (IC₅₀ = 22 µM). Shown to completely block rpS6-Ser^240/244 phosphorylation in L6 cells at 2.5 µM without inducing pAkt-Thr³⁰⁸ and Ser⁴⁷³, and display substantial selectivity in a 219-kinase panel (1 µM of DG2 in the presence of 10 µM of ATP; IC₅₀ ≥50%; Clk1, Clk2, Dyrk1A, Dyrk3, Flt3, Flt3-D835Y, Flt4, GSK-3α/β, KDR, MAP4K4, Mink1, PKA, PRKG1, PRKG2, Ret-V804L, Ret-Y791F, RSK1, RSK3, RSK2, MSK2, MSK1 and p70S6K).

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

Wang, B.T., et al. 2011. Proc. Natl. Acad. Sci. USA108, 15201.
Okuzumi, T., et al. 2009. Nat. Chem. Biol.5, 484.

Legal Information

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

Safety Information

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