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203305 Bisindolylmaleimide Inhibitor Set

203305
  
Purchase on Sigma-Aldrich

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

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.