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559274

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C16H17BrN6O
CAS Number:
Molecular Weight:
389.25
MDL number:
UNSPSC Code:
12352200

Quality Level

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

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-Ser240/244 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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

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