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Chemical Structure
Chemical Structure
Chemical Structure

Bisindolylmaleimide I . hydrochloride [GF-109203X; Goe 6850]

Research Use Only
AG-CR1-0110
AdipoGen Life Sciences
CAS Number176504-36-2
Product group Chemicals
Estimated Purity>98%
Molecular Weight412.5 . 36.5
Price on request
Packing Size
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    Bisindolylmaleimide I . hydrochloride [176504-36-2]
  • Delivery Days Customer
    10
  • CAS Number
    176504-36-2
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Molecular Formula
    C25H24N4O2 . HCl
  • Molecular Weight
    412.5 . 36.5
  • Scientific Description
    Cell permeable kinase inhibitor with improved selectivity for protein kinase C (PKC) (Ki = 10 nM) [1]. Competitive inhibitor for the ATP-binding site of PKC [1]. Anti-inflammatory [2]. Binds to P-glycoprotein [3]. Telomerase activity inhibitor [4]. Potent glycogen synthase kinase-3 (GSK-3) inhibitor [5]. Necrosis inhibitor [6]. Blocks hERG potassium channels [7-9]. Promotes osteoblastogenesis in human mesenchymal stem cells [10]. - Chemical. CAS: 176504-36-2. Formula: C25H24N4O2 . HCl. MW: 412.5 . 36.5. Cell permeable kinase inhibitor with improved selectivity for protein kinase C (PKC) (Ki = 10 nM). Competitive inhibitor for the ATP-binding site of PKC. Anti-inflammatory. Binds to P-glycoprotein. Telomerase activity inhibitor. Potent glycogen synthase kinase-3 (GSK-3) inhibitor. Necrosis inhibitor. Blocks hERG potassium channels. Promotes osteoblastogenesis in human mesenchymal stem cells.
  • SMILES
    Cl.CN(C)CCCN1C=C(C2=C1C=CC=C2)C1=C(C(=O)NC1=O)C1=CNC2=C1C=CC=C2
  • Storage Instruction
    -20°C,2°C to 8°C
  • UNSPSC
    51202000

References

  • The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C: D. Toullec, et al.; J. Biol. Chem. 266, 15771 (1991)
  • Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3- (dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H- pyrrole-2,5- dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model: S. Kuchera, et al.; Agents Actions 39, C169 (1993)
  • Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance: V. Gekeler, et al.; Br. J. Cancer 74, 897 (1996)
  • Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture: W.C. Ku, et al.; BBRC 241, 730 (1997)
  • The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity: I. Hers, et al.; FEBS Lett. 460, 433 (1999)
  • Bisindolylmaleimide I and V inhibit necrosis induced by oxidative stress in a variety of cells including neurons: R. Asakai, et al.; Neurosci. Res. 44, 297 (2002)
  • Direct block of hERG potassium channels by the protein kinase C inhibitor bisindolylmaleimide I (GF109203X): D. Thomas, et al.; Cardiovasc. Res. 64, 467 (2004)
  • The protein kinase C inhibitor, bisindolylmaleimide (I), inhibits voltage-dependent K+ channels in coronary arterial smooth muscle cells: W.S. Park, et al.; Life Sci. 77, 512 (2005)
  • Effects of the PKC inhibitors chelerythrine and bisindolylmaleimide I (GF 109203X) on delayed rectifier K(+) currents: G. Harmati, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 383, 141 (2011)
  • Bisindolylmaleimide I enhances osteogenic differentiation: F. Zhou, et al.; Prot. Cell 3, 311 (2012)