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203305 Bisindolylmaleimide Inhibitor Set

203305
  
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      Overview

      Replacement Information
      Description
      OverviewContains 250 µg each of Bisindolylmaleimide I, HCl (Cat. No. 203291), Bisindolylmaleimide II (Cat. No. 203292), Bisindolylmaleimide III, HCl (Cat. No. 203294), Bisindolylmaleimide IV (Cat. No. 203297), Bisindolylmaleimide V (Cat. No. 203303), and RIM-1 (Cat. No. 557325). Supplied with an informational insert.
      Catalogue Number203305
      Brand Family Calbiochem®
      References
      ReferencesSancelme, M., et al. 1994. J. Antibiotics 47, 792. Shinohara, O., et al. 1994. Biochem. Med. Met. Biol. 51, 85. Chen, C.S., and Poenie, M. 1993. J. Biol. Chem. 268, 15812. Fabre, S., and Prudhomme, M. 1993. Bioorg. Med. Chem. 1, 193. Kuchera, S., et al. 1993. Agents Actions 39, C169. Davis, P.D., et al. 1992. J. Med. Chem. 35, 177. Tollec, D., et al. 1991. J. Biol. Chem. 266, 15771. Johnson, J.A., and Clark, R.B. 1990. Biochem. J. 268, 507. Love, J.T., et al. 1989. Biochem. Biophys. Res. Commun. 162, 138. Meyer, T., et al. 1989. Int. J. Cancer 43, 851. Reugg, U.T., and Burgess, G.M. 1989. Trends Pharmacol. Sci. 10, 218. Hannun, Y.A., and Bell, R. 1988. Science 243, 500. Loomis, C.R., and Bell, R.M. 1988. J. Biol. Chem. 263, 1682. Tamaoki, T., et al. 1986. Biochem. Biophys. Res. Commun. 135, 397.
      Product Information
      FormSolid
      Applications
      Biological Information
      Primary TargetPKC
      Secondary targetPKA
      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 -20°C
      Do not freeze Ok to freeze
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      203305 0

      Documentation

      References

      Reference overview
      Sancelme, M., et al. 1994. J. Antibiotics 47, 792. Shinohara, O., et al. 1994. Biochem. Med. Met. Biol. 51, 85. Chen, C.S., and Poenie, M. 1993. J. Biol. Chem. 268, 15812. Fabre, S., and Prudhomme, M. 1993. Bioorg. Med. Chem. 1, 193. Kuchera, S., et al. 1993. Agents Actions 39, C169. Davis, P.D., et al. 1992. J. Med. Chem. 35, 177. Tollec, D., et al. 1991. J. Biol. Chem. 266, 15771. Johnson, J.A., and Clark, R.B. 1990. Biochem. J. 268, 507. Love, J.T., et al. 1989. Biochem. Biophys. Res. Commun. 162, 138. Meyer, T., et al. 1989. Int. J. Cancer 43, 851. Reugg, U.T., and Burgess, G.M. 1989. Trends Pharmacol. Sci. 10, 218. Hannun, Y.A., and Bell, R. 1988. Science 243, 500. Loomis, C.R., and Bell, R.M. 1988. J. Biol. Chem. 263, 1682. Tamaoki, T., et al. 1986. Biochem. Biophys. Res. Commun. 135, 397.
      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.

      Revision20-May-2008 RFH
      DescriptionInhibition of protein kinase C (PKC) is one of the most direct methods for investigating its role in cellular metabolism and tumorigenesis. The regulatory and catalytic domains of PKC can be subjected to pharmacological intervention by the use of specific inhibitors. Several novel inhibitors have been designed that selectively block either the regulatory or the catalytic domain of PKC. However, many reported inhibitors lack specificity for PKC and may inhibit other protein kinases. Tollec, et al. described bisindolylmaleimides, a family of PKC inhibitors that have structural similarities to staurosporine but display a greater selectivity for PKC. The bisindolylmaleimides differ only slightly in their inhibition constants for rat brain PKC, but their isozyme specificities have not been fully characterized. The structural similarities between bisindolylmaleimides and staurosporine indicate that the inhibitory effect of bisindolyl-maleimides involve the ATP-binding site on the catalytic domain of PKC. RIM-1 is a fluorescent PKC probe that exhibits good specificity and provides a rapid and simple means of visualizing the distribution of PKC in cells. The Calbiochem® Bisindolylmaleimide Inhibitor Set provides an opportunity to try our selection of protein kinase C inhibitors from the bisindolylmaleimide family plus a PKC fluorescent probe. This set includes 250 µg of each of the six reagents listed below. The table lists solubility information, inhibition constants or excitation/emission information and useful references for your research.
      FormSolid
      Storage -20°C
      Do Not Freeze Ok to freeze
      Toxicity Standard Handling
      ReferencesSancelme, M., et al. 1994. J. Antibiotics 47, 792. Shinohara, O., et al. 1994. Biochem. Med. Met. Biol. 51, 85. Chen, C.S., and Poenie, M. 1993. J. Biol. Chem. 268, 15812. Fabre, S., and Prudhomme, M. 1993. Bioorg. Med. Chem. 1, 193. Kuchera, S., et al. 1993. Agents Actions 39, C169. Davis, P.D., et al. 1992. J. Med. Chem. 35, 177. Tollec, D., et al. 1991. J. Biol. Chem. 266, 15771. Johnson, J.A., and Clark, R.B. 1990. Biochem. J. 268, 507. Love, J.T., et al. 1989. Biochem. Biophys. Res. Commun. 162, 138. Meyer, T., et al. 1989. Int. J. Cancer 43, 851. Reugg, U.T., and Burgess, G.M. 1989. Trends Pharmacol. Sci. 10, 218. Hannun, Y.A., and Bell, R. 1988. Science 243, 500. Loomis, C.R., and Bell, R.M. 1988. J. Biol. Chem. 263, 1682. Tamaoki, T., et al. 1986. Biochem. Biophys. Res. Commun. 135, 397.