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559286 RSK Inhibitor II - CAS 501437-28-1 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
501437-28-1C₁₉H₂₃F₂N₅O₂

Pricing & Availability

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559286-5MG
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      Glass bottle 5 mg
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      Description
      OverviewThe racemic mixture of a cell-permeable dihydropteridinone that acts as a potent and selective RSK inhibitor (IC50 ≤31 nM against RSK1, 2, 3, and 4; [ATP] = 100 µM) by targeting RSK N-terminal kinase domain in an ATP-competitive manner, while inhibiting 11 other kinases only at higher concentrations (IC50 ≥100 nM) and displaying little activity against 39 others. Shown to selectively inhibit RSK-dependent, but not RSK-independent, cellular protein phosphorylations in PMA-stimulated HEK-293 cells and EGF-stimulated Rat-2 cells (IC50 ~1 µM).
      Catalogue Number559286
      Brand Family Calbiochem®
      Synonyms2-(3,5-Difluoro-4-hydroxy-anilino)-8-isopentyl-5,7-dimethyl-7H-pteridin-6-one, racemic, p90 Ribosomal S6 Kinase Inhibitor II, BI-D1870, BID-1870, BID1870
      References
      ReferencesCarriere, A., et al. 2008. Curr. Biol. 18, 1269
      Sapkota, G.P., et al. 2007. Biochem. J. 401, 29.
      Zaru, R., et al. 2007. Nat. Immunol. 8, 1227.
      Product Information
      CAS number501437-28-1
      FormOff-white solid
      Hill FormulaC₁₉H₂₃F₂N₅O₂
      Chemical formulaC₁₉H₂₃F₂N₅O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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
      Global Trade Item Number
      Catalog Number GTIN
      559286-5MG 04055977192377

      Documentation

      RSK Inhibitor II - CAS 501437-28-1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      RSK Inhibitor II - CAS 501437-28-1 - Calbiochem Certificates of Analysis

      TitleLot Number
      559286

      References

      Reference overview
      Carriere, A., et al. 2008. Curr. Biol. 18, 1269
      Sapkota, G.P., et al. 2007. Biochem. J. 401, 29.
      Zaru, R., et al. 2007. Nat. Immunol. 8, 1227.
      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.

      Revision17-April-2012 JSW
      Synonyms2-(3,5-Difluoro-4-hydroxy-anilino)-8-isopentyl-5,7-dimethyl-7H-pteridin-6-one, racemic, p90 Ribosomal S6 Kinase Inhibitor II, BI-D1870, BID-1870, BID1870
      DescriptionThe racemic mixture of a cell-permeable dihydropteridinone that acts as a potent and selective RSK inhibitor (IC50 = 31, 24, 18, and 15 nM against RSK1, 2, 3, and 4, respectively; [ATP] = 100 µM) by targeting RSK N-terminal kinase domain in an ATP-competitive manner, while inhibiting 11 other kinases only at higher concentrations (IC50 ≥100 nM) and displaying little activity against 39 others. Shown to selectively inhibit RSK-dependent, but not RSK-independent, cellular protein phosphorylations in PMA-stimulated human HEK-293 cells and EGF-stimulated rat Rat-2 cells (IC50 ~1 µM). A useful pharmacological reagent for studying RSK-mediated cellular signaling events.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number501437-28-1
      Chemical formulaC₁₉H₂₃F₂N₅O₂
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesCarriere, A., et al. 2008. Curr. Biol. 18, 1269
      Sapkota, G.P., et al. 2007. Biochem. J. 401, 29.
      Zaru, R., et al. 2007. Nat. Immunol. 8, 1227.