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.
别名:
S6K1 Inhibitor II, DG2, 3-Bromo-4-(4-(2-methoxyphenyl)piperazin-1-yl)-1H-pyrazolo[3,4-d]-pyrimidine
SMILES string
BrC1=NNC2=C1C(N(CC3)CCN3C4=C(C=CC=C4)OC)=NC=N2
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
Quality Level
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)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Zewen Jiang et al.
Cell metabolism, 33(9), 1836-1852 (2021-08-05)
With the increasing prevalence of type 2 diabetes and fatty liver disease, there is still an unmet need to better treat hyperglycemia and hyperlipidemia. Here, we identify isthmin-1 (Ism1) as an adipokine and one that has a dual role in
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