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Submit ReviewBisindolylmaleimide II
Description: Potent PKC inhibitor; also potent nAChR antagonist
Chemical Name: 3-(1H-Indol-3-yl)-4-[1-[2-(1-methyl-2-pyrrolidinyl)ethyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Purity: ≥97% (HPLC)
Biological Activity for Bisindolylmaleimide II
Bisindolylmaleimide II is a 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).
Compound Libraries for Bisindolylmaleimide II
Bisindolylmaleimide II is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for Bisindolylmaleimide II
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Bisindolylmaleimide II
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.85 | 100 |
Preparing Stock Solutions for Bisindolylmaleimide II
The following data is based on the product molecular weight 438.52. Batch specific molecular weights may vary from batch to batch due to the degree 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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Product Datasheets for Bisindolylmaleimide II
References for Bisindolylmaleimide II
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Bisindolylmaleimide II, please let us know.
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Keywords: Bisindolylmaleimide II, Bisindolylmaleimide II supplier, protein, kinase, C, PKC, inhibits, inhibitors, nicotinic, cholinergic, acetylcholine, nAChRs, antagonists, antagonism, catecholamines, potent, Protein, Kinase, Nicotinic, Receptors, (Non-selective), 4128, Tocris Bioscience
4 Citations for Bisindolylmaleimide II
Citations are publications that use Tocris products. Selected citations for Bisindolylmaleimide II include:
O'Neill & Sylantyev (2018) Selective modulation of tonically active GABAA receptor functional subgroups by G-proteins and protein kinase C. Exp Biol Med (Maywood) 243 1046 PMID: 30205722
James H et al (2020) Contributing mechanisms underlying desensitization of cholecystokinin-induced activation of primary nodose ganglia neurons. Am J Physiol Cell Physiol 318 C787-C796 PMID: 32073876
John et al (2020) Small Molecule Inhibitor Screen Reveals Calcium Channel Signaling as a Mechanistic Mediator of Clostridium difficile TcdB-Induced Necrosis. ACS Chem Biol 15 1212-1221 PMID: 31909964
Jones et al (2004) Regulation of SHP-1 tyrosine phosphatase in human platelets by serine phosphorylation at its C terminus. PLoS One 279 40475 PMID: 15269224
Do you know of a great paper that uses Bisindolylmaleimide II from Tocris? Please let us know.
Reviews for Bisindolylmaleimide II
Average Rating: 4 (Based on 1 Review.)
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BII upregulates GABA-dependent affects of GABA-A receptor.
By
Anonymous on 07/21/2019
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Hippocampus
Bisindolylmaleimide II (BII) was used to block PKC in hippocampal granule cells. Such a block enhances activity of GABA receptors and, as a sequence, increases effect of competitive antagonists of GABA on root mean square noise (RMS) amplitude of holding current in electrophysiological recording. Figure: changes of RMS after application of SR 95531 and SR 95531 + Picrotoxin. BII makes significant an effect of SR 95531 applied alone.
