Bisindolylmaleimide II

Pricing Availability Delivery Time Qty
Cat.No. 4128 - Bisindolylmaleimide II | C27H26N4O2 | CAS No. 137592-45-1
Description: Potent PKC inhibitor and nicotinic receptor 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)
Datasheet
Citations (1)
Literature

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.

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 11.4 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

Safety Datasheet

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


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View Related Products by Product Action

View all Protein Kinase C Inhibitors

Keywords: protein kinase C PKC inhibits inhibitors nicotinic cholinergic acetylcholine nAChRs antagonists antagonism catecholamines potent Protein Kinase C

1 Citation for Bisindolylmaleimide II

Citations are publications that use Tocris products. Selected citations for Bisindolylmaleimide II include:

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? If so please let us know.

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