GF 109203X is a very 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 (K_i = 29.5 nM). Anti-inflammatory in vivo.

Product Specifications

Molecular Weight

412.49

Formula

C₂₅H₂₄N₄O₂

Storage

Store at RT

Purity

≥98% (HPLC)

Chemical Name

2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl) maleimide

CAS Number

133052-90-1

PubChem ID

2396

InChI Key

QMGUOJYZJKLOLH-UHFFFAOYSA-N

SMILES

CN(C)CCCN1C=C(C2=CC=CC=C12)C1=C(C(=O)NC1=O)C1=CNC2=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
Solubility	DMSO	10.31	25

Preparing Stock Solutions for GF 109203X

The following data is based on the product molecular weight 412.49

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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.25 mM	9.70 mL	48.49 mL	96.97 mL
1.25 mM	1.94 mL	9.70 mL	19.39 mL
2.5 mM	0.97 mL	4.85 mL	9.70 mL
12.5 mM	0.19 mL	0.97 mL	1.94 mL

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Background References

References are publications that support the biological activity of the product.

Jiang Heat shock protein 90-mediated inactivation of nuclear factor-κB switches autophagy to apoptosis through becn1 transcriptional inhibition in selenite-induced NB4 cells. Mol.Biol.Cell. 2011 PMID: 21346199
Toullec The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J.Biol.Chem. 1991 PMID: 1874734
Jacobson Anti-inflammatory properties of Go 6850: a selective inhibitor of protein kinase C. J.Pharmacol.Exp.Ther. 1995 PMID: 7473193
Martiny-Baron Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976. J.Biol.Chem. 1993 PMID: 8486620
Coultrap Competitive antagonism of the mouse 5-hydroxytryptamine3 receptor by bisindolylmaleimide I, a "selective" protein kinase C inhibitor. J.Pharmacol.Exp.Ther. 1999 PMID: 10381762

GF 109203X

Tocris Bioscience, part of Bio-Techne | Catalog # 0741

Key Product Details

Description

Alternative Names

View all Protein Kinase C Inhibitors »

Product Description