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375680 Hesperadin - CAS 422513-13-1 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₉H₃₂N₄O₃S 422513-13-1

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375680-5MG
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      Glass bottle 5 mg
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      Description
      OverviewA cell-permeable indolinone compound that interacts with both the ATP- and the adjacent hydrophobic binding pocket of Aurora B and acts as a rapid and reversible inhibitor of Aurora kinase B activity (IC50 ~ 250 nM) with moderate selectivity over Cdk1/B, Cdk2/E and Cdk4/D1 (IC50 = 1.2, > 10 and > 10 µM). Also, potently inhibits several kinases at 1 µM in a 25-kinase screening panel (100%, 100%, 96%, 88%, 87% and 84% against Lck, PHK, AMPK, MKK1, MAPKAP-K1 and Chk1, respectively). Reported to reduce histone H3-Ser10 phosphorylation, inhibit cytokinesis, promote chromosome biorientation, perturb mitosis and polyploidy in mammalian cells. Recently shown to potently inhibit MST4 kinase (IC50 = 6.18 nM) in an ATP-competitive manner. Dose-dependently accelerates hypoxia-induced apoptosis and decreases survival (EC50 = 10 nM in MST4 LβT2 gonadotrope cells).
      Catalogue Number375680
      Brand Family Calbiochem®
      SynonymsMammalian Ste20-like Kinase 4 Inhibitor, MST4 Inhibitor, Aurora Kinase Inhibitor X, AMPK Inhibitor II
      References
      ReferencesXiong, W., et al. 2016. Mol. Cancer Ther. 15, In press.
      Knowlton, A.L., et al. 2006. Curr. Biol. 16, 1705.
      Kapoor, T.M., et al. 2006. Science 311, 388.
      Hirota, T., et al. 2005. Nature 438, 1176.
      Sessa, F., et al. 2005. Mol. Cell. 18, 379.
      Lampson, M.A., et al. 2004. Nat. Cell Biol. 6, 232.
      Hauf, S., et al. 2003. J. Cell Biol. 161, 281.
      Product Information
      CAS number422513-13-1
      FormYellow solid
      Hill FormulaC₂₉H₃₂N₄O₃S
      Chemical formulaC₂₉H₃₂N₄O₃S
      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 Regulatory Review
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot freeze at -(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

      Hesperadin - CAS 422513-13-1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Hesperadin - CAS 422513-13-1 - Calbiochem Certificates of Analysis

      TitleLot Number
      375680

      References

      Reference overview
      Xiong, W., et al. 2016. Mol. Cancer Ther. 15, In press.
      Knowlton, A.L., et al. 2006. Curr. Biol. 16, 1705.
      Kapoor, T.M., et al. 2006. Science 311, 388.
      Hirota, T., et al. 2005. Nature 438, 1176.
      Sessa, F., et al. 2005. Mol. Cell. 18, 379.
      Lampson, M.A., et al. 2004. Nat. Cell Biol. 6, 232.
      Hauf, S., et al. 2003. J. Cell Biol. 161, 281.
      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.

      Revision31-August-2011 RFH
      SynonymsMammalian Ste20-like Kinase 4 Inhibitor, MST4 Inhibitor, Aurora Kinase Inhibitor X, AMPK Inhibitor II
      DescriptionA cell-permeable indolinone compound that interacts with both the ATP- and the adjacent hydrophobic binding pocket of Aurora B and acts as a rapid and reversible inhibitor of Aurora kinase B activity (IC50 ~250 nM) with moderate selectivity over Cdk1/B, Cdk2/E and Cdk4/D1 (IC50 = 1.2, > 10 and > 10 µM). Also, potently inhibits several kinases at 1 µM in a 25-kinase screening panel (100%, 100%, 96%, 88%, 87% and 84% against Lck, PHK, AMPK, MKK1, MAPKAP-K1 and Chk1, respectively). Reported to reduce histone H3-Ser10 phosphorylation, inhibit cytokinesis, promote chromosome biorientation, perturb mitosis and polyploidy in mammalian cells.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number422513-13-1
      Chemical formulaC₂₉H₃₂N₄O₃S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot freeze at -(20°C). Stock solutions are stable for up to 6 months at -20°C..
      Toxicity Regulatory Review
      ReferencesXiong, W., et al. 2016. Mol. Cancer Ther. 15, In press.
      Knowlton, A.L., et al. 2006. Curr. Biol. 16, 1705.
      Kapoor, T.M., et al. 2006. Science 311, 388.
      Hirota, T., et al. 2005. Nature 438, 1176.
      Sessa, F., et al. 2005. Mol. Cell. 18, 379.
      Lampson, M.A., et al. 2004. Nat. Cell Biol. 6, 232.
      Hauf, S., et al. 2003. J. Cell Biol. 161, 281.