375680 | Hesperadin - CAS 422513-13-1 - Calbiochem

375680
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₉H₃₂N₄O₃S 422513-13-1

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.