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Tocris/GF 109203X/0741/1/1 mg

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货号: 0741/1

品牌: Tocris

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Description: Protein kinase C inhibitor

Alternative Names: Gö 6850, Bisindolylmaleimide I

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

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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.

Compound Libraries

GF 109203X is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	412.49
Formula	C₂₅H₂₄N₄O₂
Storage	Store at RT
Purity	≥98% (HPLC)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	10.31	25

Preparing Stock Solutions

The following data is based on the product molecular weight 412.49. 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	2.42 mL	12.12 mL	24.24 mL
5 mM	0.48 mL	2.42 mL	4.85 mL
10 mM	0.24 mL	1.21 mL	2.42 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Coultrap et al (1999) Competitive antagonism of the mouse 5-hydroxytryptamine3 receptor by bisindolylmaleimide I, a "selective" protein kinase C inhibitor. J.Pharmacol.Exp.Ther. 290 76 PMID: 10381762

Jacobson et al (1995) Anti-inflammatory properties of Go 6850: a selective inhibitor of protein kinase C. J.Pharmacol.Exp.Ther. 275 995 PMID: 7473193

Martiny-Baron et al (1993) Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976. J.Biol.Chem. 268 9194 PMID: 8486620

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

Jiang et al (2011) 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. 22 1167 PMID: 21346199

Keywords: GF 109203X, supplier, Protein, kinase, C, inhibitors, inhibits, PKC, PKM, Kinase, Kinases, alpha, beta, α, β, GF109203X, Go6850, Go, 6850, Gö, 6850, Bisindolylmaleimide, I, Protein, Kinase, C, Autophagy, Protein, Kinase, C, Tocris Bioscience

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