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.
Storage and Stability:
Short-term Storage: +4°C
Long-term Storage: -20°C
Stable for at least 2 years after receipt when stored at -20°C. Store solutions at -20°C in the dark.
C25H24N4O2 . HCl
Purity: >98% (NMR)
Important Note: This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Product Reference: |
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--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. (Epub ahead of print) (2010)
|Intended for research use only. Not for use in human, therapeutic, or diagnostic applications.|