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505300 RSK2 Inhibitor, RMM-46 - Calbiochem

505300
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₄H₂₆N₄O₅

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      Description
      OverviewA cell-permeable cyanoacrylamide compound that acts as a potent, reversible, and selective inhibitor of ribosomal S6 kinase 2 (RSK2; IC50 = 12 and 2.5 nM for wild-type and T493M RSK2, respectively). Shown to act by covalently modifying Cys436 at the ATP-binding site. Exhibits good selectivity over NEK2 and PLK1 (IC50 = 530 nM and 2.2 µM) and does not affect the activity of a panel of 26 other protein kinases. Also shown to block phosphorylation of mitogen and stress activated kinases (MSK) 1, 2, and 3 in PMA-stimulated COS7 cells (IC50 ~100 nM) and CREB phosphorylation in PMA- or UV-stimulated HeLa cells (IC50 ~ 300 nM).
      Catalogue Number505300
      Brand Family Calbiochem®
      Synonyms(E)-2-Cyano-N-(1-hydroxy-2-methylpropan-2-yl)-3-(3-(3,4,5-trimethoxyphenyl)-1H-indazol-5-yl)acrylamide, RMM46, RSK Inhibitor IV
      References
      ReferencesMiller, R.M., et al. 2013. J. Am. Chem. Soc. 135, 5298.
      Product Information
      FormYellow solid
      Hill FormulaC₂₄H₂₆N₄O₅
      Chemical formulaC₂₄H₂₆N₄O₅
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetRSK2
      Primary Target IC<sub>50</sub>12 and 2.5 nM for wild-type and T493M RSK2, respectively
      Secondary targetMSK 1, 2 , 3
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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

      RSK2 Inhibitor, RMM-46 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Miller, R.M., et al. 2013. J. Am. Chem. Soc. 135, 5298.
      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.

      Revision18-October-2013 JSW
      Synonyms(E)-2-Cyano-N-(1-hydroxy-2-methylpropan-2-yl)-3-(3-(3,4,5-trimethoxyphenyl)-1H-indazol-5-yl)acrylamide, RMM46, RSK Inhibitor IV
      DescriptionA cell-permeable cyanoacrylamide compound that acts as a potent, reversible, and selective inhibitor of ribosomal S6 kinase 2 (RSK2; IC50 = 12 and 2.5 nM for wild-type and T493M RSK2, respectively). Shown to act by covalently modifying Cys436 at the ATP-binding site. Exhibits good selectivity over NEK2 and PLK1 (IC50 = 530 nM and 2.2 µM) and does not affect the activity of a panel of 26 other protein kinases. Also shown to block phosphorylation of mitogen and stress activated kinases (MSK) 1, 2, and 3 in PMA-stimulated COS7 cells (IC50 ~100 nM) and CREB phosphorylation in PMA- or UV-stimulated HeLa cells (IC50 ~ 300 nM).
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₄H₂₆N₄O₅
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      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
      ReferencesMiller, R.M., et al. 2013. J. Am. Chem. Soc. 135, 5298.