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Bisindolylmaleimide I (GF 109203X) (CAS 133052-90-1)

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Alternate Names:
3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
Application:
Bisindolylmaleimide I (GF 109203X) is a highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3
CAS Number:
133052-90-1
Purity:
≥98%
Molecular Weight:
412.48
Molecular Formula:
C25H24N4O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Bisindolylmaleimide I (GF 109203X) is a staurosporine (sc-3510) inspired molecule, which may act to display equally potent inhibition, but with vastly superior selectivity, for all of the known isoforms of PKC (IC50 = 8-20 nM). Inhibition is competitive with respect to ATP, which suggests that Bisindolylmaleimide I occupies the ATP binding domain of the PKC isoforms. Bisindolylmaleimide I (GF 109203X) has been used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals. It inhibits PKC within intact platelets and T cells, Fas-mediated apoptosis, and T cell-mediated autoimmune diseases, as well as GSK-3. See sc-24004 for water soluble form of Bisindolylmaleimide I. Bisindolylmaleimide I (GF 109203X) is an inhibitor of PHK/CaM, PKC alpha, PKC beta, PKC delta, PKC epsilon, PKC gamma and SR/HTR3.


Bisindolylmaleimide I (GF 109203X) (CAS 133052-90-1) References

  1. Competitive antagonism of the mouse 5-hydroxytryptamine3 receptor by bisindolylmaleimide I, a 'selective' protein kinase C inhibitor.  |  Coultrap, SJ., et al. 1999. J Pharmacol Exp Ther. 290: 76-82. PMID: 10381762
  2. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity.  |  Hers, I., et al. 1999. FEBS Lett. 460: 433-6. PMID: 10556511
  3. Divergent effects of protein kinase C (PKC) inhibitors staurosporine and bisindolylmaleimide I (GF109203X) on bone resorption.  |  Lee, SK. and Stern, PH. 2000. Biochem Pharmacol. 60: 923-6. PMID: 10974200
  4. Role of protein kinase C in alpha(1)-adrenergic regulation of a(Na)(i) in guinea pig ventricular myocytes.  |  Jo, SH., et al. 2000. Am J Physiol Heart Circ Physiol. 279: H1661-8. PMID: 11009453
  5. Protein kinase C-mediated in vitro invasion of human glioma cells through extracellular-signal-regulated kinase and ornithine decarboxylase.  |  da Rocha, AB., et al. 2000. Pathobiology. 68: 113-23. PMID: 11174068
  6. Bisindolylmaleimide I and V inhibit necrosis induced by oxidative stress in a variety of cells including neurons.  |  Asakai, R., et al. 2002. Neurosci Res. 44: 297-304. PMID: 12413658
  7. Ca2+ sensitization in contraction of human bladder smooth muscle.  |  Takahashi, R., et al. 2004. J Urol. 172: 748-52. PMID: 15247775
  8. A role for ERK1/2 in EGF- and ATP-dependent regulation of amiloride-sensitive sodium absorption.  |  Falin, R., et al. 2005. Am J Physiol Cell Physiol. 288: C1003-11. PMID: 15634742
  9. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.  |  Toullec, D., et al. 1991. J Biol Chem. 266: 15771-81. PMID: 1874734
  10. Effects of the PKC inhibitors chelerythrine and bisindolylmaleimide I (GF 109203X) on delayed rectifier K+ currents.  |  Harmati, G., et al. 2011. Naunyn Schmiedebergs Arch Pharmacol. 383: 141-8. PMID: 21120453
  11. Functional role of muscarinic receptor subtypes in calcium sensitization and their contribution to rho-kinase and protein kinase C pathways in contraction of human detrusor smooth muscle.  |  Shahab, N., et al. 2012. Urology. 79: 1184.e7-13. PMID: 22546411
  12. The bisindolylmaleimide GF 109203X, a selective inhibitor of protein kinase C, does not inhibit the potentiating effect of phorbol ester on ethanol-induced phospholipase C-mediated hydrolysis of phosphatidylethanolamine.  |  Kiss, Z., et al. 1995. Biochim Biophys Acta. 1265: 93-5. PMID: 7857990
  13. Selective inhibition of protein kinase C isozymes by the indolocarbazole Gö 6976.  |  Martiny-Baron, G., et al. 1993. J Biol Chem. 268: 9194-7. PMID: 8486620
  14. Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance.  |  Gekeler, V., et al. 1996. Br J Cancer. 74: 897-905. PMID: 8826855
  15. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.  |  Zhou, T., et al. 1999. Nat Med. 5: 42-8. PMID: 9883838

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Bisindolylmaleimide I (GF 109203X), 1 mg

sc-24003A
1 mg
$105.00

Bisindolylmaleimide I (GF 109203X), 5 mg

sc-24003
5 mg
$242.00