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Biological Activity
GF 109203X is a potent and selective inhibitor of protein kinase C, selective for the α and β1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC50 values are 0.6, 4.6, and 33 μM respectively). Potent antagonist at the 5-HT3 receptor (Ki = 29.5 nM).
Targets
| Target | Value |
|---|---|
| PKCβ2 | IC50: 16nM |
| PKCβ1 | IC50: 17nM |
| PKCα | IC50: 20nM |
| PKCγ | IC50: 20nM |
| PDGFR | IC50: 65μM |
| EGFR | IC50: >100μM |
| Insulin Receptor | IC50: >100μM |
| In vitro | DMSO | 70 mg/mL (169.7 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 24.24 mL | 121.22 mL | 242.43 mL |
| 0.5 mM | 4.85 mL | 24.24 mL | 48.49 mL |
| 1 mM | 2.42 mL | 12.12 mL | 24.24 mL |
| 5 mM | 0.48 mL | 2.42 mL | 4.85 mL |
*The above data is based on the productmolecular weight 412.49. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A13197 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 133052-90-1 |
| Formula | C25H24N4O2 |
| M. Wt | 412.49 |
| Purity | >98% |
| Synonyms | GF-109203X, GF109203X, GO6850, GO-6850, Bisindolylmaleimide I |
| SMILES | CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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