559274 S6K1 Inhibitor II, DG2 - Calbiochem

559274
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₆H₁₇BrN₆O

Pricing & Availability

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559274-10MGCN
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      Glass bottle 10 mg
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      Description
      OverviewA 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).
      Catalogue Number559274
      Brand Family Calbiochem®
      Synonyms3-Bromo-4-(4-(2-methoxyphenyl)piperazin-1-yl)-1H-pyrazolo[3,4-d]-pyrimidine
      References
      ReferencesWang, B.T., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 15201.
      Okuzumi, T., et al. 2009. Nat. Chem. Biol. 5, 484.
      Product Information
      FormOff-white solid
      Hill FormulaC₁₆H₁₇BrN₆O
      Chemical formulaC₁₆H₁₇BrN₆O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      S6K1 Inhibitor II, DG2 - Calbiochem Certificates of Analysis

      TitleLot Number
      559274

      References

      Reference overview
      Wang, B.T., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 15201.
      Okuzumi, T., et al. 2009. Nat. Chem. Biol. 5, 484.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision08-June-2012 JSW
      Synonyms3-Bromo-4-(4-(2-methoxyphenyl)piperazin-1-yl)-1H-pyrazolo[3,4-d]-pyrimidine
      DescriptionA 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).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₆H₁₇BrN₆O
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml; clear, pale yellow solution)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesWang, B.T., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 15201.
      Okuzumi, T., et al. 2009. Nat. Chem. Biol. 5, 484.