Bisindolylmaleimide I

CHF 70.00
In stock
AG-CR1-0009-M0011 mgCHF 70.00
AG-CR1-0009-M0055 mgCHF 210.00
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Product Details
Synonyms GF-109203X; Gö 6850; BIM I
Product Type Chemical
Properties
Formula

C25H24N4O2

MW 412.5
CAS 133052-90-1
Purity Chemicals ≥98% (NMR)
Appearance Orange solid.
Solubility Soluble in DMSO.
InChi Key QMGUOJYZJKLOLH-UHFFFAOYSA-N
Smiles CN(C)CCCN1C=C(C2=C1C=CC=C2)C1=C(C(=O)NC1=O)C1=CNC2=C1C=CC=C2
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • Cell permeable kinase inhibitor with improved selectivity for protein kinase C (PKC) (Ki = 10 nM) [1].
  • Competetive 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].
Product References
  1. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C: D. Toullec, et al.; J. Biol. Chem. 266, 15771 (1991) 
  2. 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) 
  3. 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) 
  4. Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture: W.C. Ku, et al.; BBRC 241, 730 (1997) 
  5. 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) 
  6. 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)
  7. Direct block of hERG potassium channels by the protein kinase C inhibitor bisindolylmaleimide I (GF109203X): D. Thomas, et al.; Cardiovasc. Res. 64, 467 (2004) 
  8. 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) 
  9. 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)
  10. Bisindolylmaleimide I enhances osteogenic differentiation: F. Zhou, et al.; Prot. Cell 3, 311 (2012)
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