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| GF109203X Basic information |
| GF109203X Chemical Properties |
| Melting point | 280℃ (decomposition) | | Boiling point | 685.6±55.0 °C(Predicted) | | density | 1.30±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: ~1 mg/mlsoluble | | pka | 8.13±0.60(Predicted) | | form | Liquid | | color | Orange | | Water Solubility | Insoluble in water. | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 6 months. |
| Hazard Codes | Xn | | Risk Statements | 40-22 | | Safety Statements | 36/37 | | WGK Germany | 3 | | RTECS | UX9590000 | | HS Code | 2925199590 |
| GF109203X Usage And Synthesis |
| Description | GF-109203X (133052-90-1) is a potent and selective protein kinase C inhibitor (IC50 = 10 nM; cAMP-dependent protein kinase IC50 = 2 μM and phosphorylase kinase IC50 = 0.7 μM). Inactive against the tyrosine kinases EGFR, PGDFR and Insulin receptor. Potent inhibitor of GSK-3β in cell lysates (IC50 = 360nM) and GSK-3β immunoprecipitates (IC50 = 170nM) derived from rat epididymal adipocytes.2 Cell permeable. | | Uses | Bisindolylmaleimide is used as a highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3, used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals, very potent and selective inhibitor of protein kinase C. | | Biological Activity | Very potent and selective inhibitor of protein kinase C, selective for the α and β 1 isoforms (IC 50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μ M for α , β 1, δ , ε , and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC 50 values are 0.6, 4.6, and 33 μ M respectively). Potent antagonist at the 5-HT 3 receptor (K i = 29.5 nM). Anti-inflammatory in vivo . Also available as part of the Mixed Kinase Inhibitor Tocriset™ . | | Biochem/physiol Actions | A potent and selective competitive inhibitor of protein kinase C (PKC) and of glycogen synthase kinase-3 (GSK-3). Inhibits parathyroid hormone-induced Ca2+ resorption from isolated bone tissue, Staurosporine, another protein kinase inhibitor, actually enhanced Ca2+ resorption elicited by a number of agents, but GF109203X counteracted that enhancement. | | References | 1) Toullec, et al. (1991), The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C; J. Biol .Chem. 266 15771
2) Hers, et al. (1999) The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity; FEBS Lett. 460 433 |
| GF109203X Preparation Products And Raw materials |
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