Bisindolylmaleimide II

Tocris Bioscience | Catalog # 4128

Potent PKC inhibitor; also potent nAChR antagonist
Tocris Bioscience
Discontinued Product
4128 has been discontinued. View all Protein Kinase C Inhibitors products.

Key Product Details

Description

Potent PKC inhibitor; also potent nAChR antagonist
View all Protein Kinase C Inhibitors »

Product Description

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).

Product Specifications for Bisindolylmaleimide II

Molecular Weight

438.52

Formula

C27H26N4O2

Storage

Store at -20°C

Purity

≥97% (HPLC)

Chemical Name

3-(1H-Indol-3-yl)-4-[1-[2-(1-methyl-2-pyrrolidinyl)ethyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.28 mL 11.40 mL 22.80 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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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 12 publications citing the usage of this product.

Product Documents for Bisindolylmaleimide II

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for Bisindolylmaleimide II

For research use only

Related Research Areas

Diabetes
Intracellular Kinases

Citations for Bisindolylmaleimide II

Customer Reviews for Bisindolylmaleimide II (1)

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  • BII upregulates GABA-dependent affects of GABA-A receptor
    Name: Anonymous
    Species: Rat
    Assay Type: In Vitro
    Cell Line/Tissue: Hippocampus
    Verified Customer | Posted 07/21/2019
    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.
    Bisindolylmaleimide II 4128

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