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
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About This Item
Empirical Formula (Hill Notation):
C16H17BrN6O
CAS Number:
Molecular Weight:
389.25
UNSPSC Code:
12352200
MDL number:
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
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
Preparation Note
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.
Okuzumi, T., et al. 2009. Nat. Chem. Biol.5, 484.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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