Biological Activity
Potent, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 0.01 μM). Displays selectivity for PKC over protein kinase A (PKA) and phosphorylase kinase (PK) (IC50 values are 0.75 and 2μM for PK and PKA respectively). Also displays potent, noncompetitive antagonism at nicotinic cholinergic receptors (IC50 ~ 0.03 μM for inhibition of catecholamine secretion in nicotine-stimulated PC-12 cells).
Technical Data
| M. Wt | 438.52 |
| Formula | C27H26N4O2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 137592-45-1 |
| PubChem ID | 2397 |
| InChI Key | LBFDERUQORUFIN-UHFFFAOYSA-N |
| Smiles | O=C(NC3=O)C(C4=CNC5=C4C=CC=C5)=C3C1=CN(CCC6CCCN6C)C2=CC=CC=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.85 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 438.52. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.28 mL | 11.4 mL | 22.8 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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References
References are publications that support the products' biological activity.
Toullec et al (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J.Biol.Chem. 266 15771 PMID: 1874734
Mahata et al (2002) Chromaffin cell catecholamine secretion: bisindolylmaleimide compounds exhibit novel and potent antagonist effects at the nicotinic cholinergic receptor in pheochromocytoma cells. Mol.Pharmacol. 61 1340 PMID: 12021395
Keywords: Bisindolylmaleimide II, supplier, protein, kinase, C, PKC, inhibits, inhibitors, nicotinic, cholinergic, acetylcholine, nAChRs, antagonists, antagonism, catecholamines, potent, Protein, Kinase, C, Nicotinic, Receptors, (Non-selective), Protein, Kinase, C, Tocris Bioscience
