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Kinase Kit Resource

Protein Kinase C (PKC) Pathway and Related Products

Inhibitor Resource
  Bisindolylmaleimide I
Cat. No. 203290  
All Categories » Calbiochem » Inhibitors » Kinase and Phosphatase » Protein Kinase C (PKC)

2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-maleimide
Gö 6850
GF 109203X

Deep orange solid. A highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (Ki = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCa-, bI-, bII-, g-, d-, and e- isozymes. Potently inhibits GSK-3 in primary adipocyte lysates (IC50 = 360 nM) and in GSK-3b immunoprecipitates (IC50 = 170 nM). May inhibit protein kinase A at a much higher concentration (Ki = 2 µM). Purity: ≥95% by HPLC. CAS 133052-90-1.

Ref.: Hers, I., et al. 1999. FEBS Lett. 460, 433. Ku, W.-C., et al. 1997. Biochem. Biophys. Res. Commun. 241, 730. Gekeler, V., et al. 1996. Br. J. Cancer 74, 897. Kiss, Z., et al. 1995. Biochim. Biophys. Acta 1265, 93. Toullec, D., et al. 1991. J. Biol. Chem. 266, 15771.
Sold under license of U.S. Patent 5,380,746.

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250 µgY$40.00
1 mgY$123.00

SolubilityMolecular FormulaMol. Wt.
DMSO C25H24N4O2 412.5 


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203290: Bisindolylmaleimide I - English
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Related Categories:
All Categories » Calbiochem » Inhibitors » Kinase and Phosphatase » Protein Kinase C (PKC)

Selected Citations:
  1. Alexandra Thiel, Mira Heinonen, Johanna Rintahaka, Tuija Hallikainen, and Annabrita Hemmes, Dan A. Dixon, Caj Haglund, and Ari Ristimaki. (2006) EXPRESSION OF CYCLOOXYGENASE-2 IS REGULATED BY GSK-3 IN GASTRIC CANCER CELLS. Journal of Biological Chemistry in press,.
  2. Xiaohua Jiang, et al. (2005) Hyperhomocystinemia impairs endothelial function and eNOS activity via PKC activation. Arteriosclerosis, Thrombosis, and Vascular Biology in press,.
  3. Ademi E. Santiago-Walker, et al. (2005) Protein Kinase C δ Stimulates Apoptosis by Initiating G1 Phase Cell Cycle Progression and S Phase Arrest. Journal of Biological Chemistry 280, 32107-32114.
  4. Wojciech Wojciechowski, et al. (2005) Enhanced Expression of CD20 in Human Tumor B Cells is Controlled Through ERK-Dependent Mechanisms. Journal of Immunology 174, 7859-7868.
  5. Justin C. Mason, et al. (2004) Decay-accelerating actor induction on vascular endothelium by vascular endothelial growth factor (VEGF) is mediated via a VEGF receptor-2 (VEGF-R2)- and protein kinase C-α/ε (PKCα/ε)-dependent cytoprotective signaling pathway a. Journal of Biological Chemistry 279, 41611-41618.
  6. Michael J. Cross, et al. (2002) The Shb Adaptor Protein Binds to Tyrosine 766 in the FGFR-1 and Regulates the Ras/MEK/MAPK Pathway via FRS2 Phosphorylation in Endothelial Cells. Molecular Biology of the Cell 13, 2881-2893.