- GF109203X
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- $1.00
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2020-01-15
- CAS:133052-90-1
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 200kg
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| | 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 | | biological source | synthetic | | 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. | | InChIKey | QMGUOJYZJKLOLH-UHFFFAOYSA-N | | SMILES | N1C(=O)C(=C(C1=O)c4c5c([nH]c4)cccc5)c2c3c([n](c2)CCCN(C)C)cccc3 |
| Hazard Codes | Xn | | Risk Statements | 40-22 | | Safety Statements | 36/37 | | WGK Germany | 3 | | RTECS | UX9590000 | | HS Code | 2925199590 | | Storage Class | 10 - Combustible liquids |
| | 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. | | storage | Store at RT | | Background | Bisindolylmaleimide I, also known as GF-109203X, is a potent inhibitor of PKC. In vitro, the IC50 of BIS is 10-20 nM for PKCα/β/γ and 100-200 nM for PKCδ/ε isoforms. The in vitro IC50 for PKCζ is approximately 6 μM, indicating that BIS is a very weak inhibitor for this isoform. In in vivo cellular assays, the IC50 of BIS for PKC is 0.2-2 μM. | | References | [1] D. TOULLEC. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.[J]. The Journal of Biological Chemistry, 1991, 12 1: 15771-15781. DOI:10.1016/s0021-9258(18)98476-0
[2] INGEBORG HERS Richard M D Jeremy M Tavaré. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity[J]. FEBS Letters, 1999, 460 3: 433-436. DOI:10.1016/s0014-5793(99)01389-7 |
| | GF109203X Preparation Products And Raw materials |
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