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HomeProduct name listGF109203X

GF109203X

Synonym(s):Bisindolylmaleimide I;Bisindolylmaleimide I hydrochloride;InSolution ;3-(N-[Dimethylamino]propyl-3-indolyl)-4-(3-indolyl)maleimide;3-[1-(Dimethylaminopropyl)indol-3-yl]-4-(indol-3-yl)maleimide hydrochloride

GF109203X Structural

What is GF109203X?

Description

GF-109203X (133052-90-1) is a potent and selective protein kinase C inhibitor (IC50 = 10 nM; cAMP-dependent protein kinase IC50 = 2 μM and phosphorylase kinase IC50 = 0.7 μM). Inactive against the tyrosine kinases EGFR, PGDFR and Insulin receptor. Potent inhibitor of GSK-3β in cell lysates (IC50 = 360nM) and GSK-3β immunoprecipitates (IC50 = 170nM) derived from rat epididymal adipocytes.2 Cell permeable.

The Uses of GF109203X

Bisindolylmaleimide is used as a highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3, used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals, very potent and selective inhibitor of protein kinase C.

What are the applications of Application

Bisindolylmaleimide I (GF 109203X) is a highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3

Biological Activity

Very potent and selective inhibitor of protein kinase C, selective for the α and β 1 isoforms (IC 50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μ M for α , β 1, δ , ε , and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC 50 values are 0.6, 4.6, and 33 μ M respectively). Potent antagonist at the 5-HT 3 receptor (K i = 29.5 nM). Anti-inflammatory in vivo . Also available as part of the Mixed Kinase Inhibitor Tocriset™ .

Biochem/physiol Actions

A potent and selective competitive inhibitor of protein kinase C (PKC) and of glycogen synthase kinase-3 (GSK-3). Inhibits parathyroid hormone-induced Ca2+ resorption from isolated bone tissue, Staurosporine, another protein kinase inhibitor, actually enhanced Ca2+ resorption elicited by a number of agents, but GF109203X counteracted that enhancement.

storage

Store at RT

References

1) Toullec, et al. (1991), The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C; J. Biol .Chem. 266 15771 2) Hers, et al. (1999) The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity; FEBS Lett. 460 433

Properties of GF109203X

Melting point: 280℃ (decomposition)
Boiling point: 685.6±55.0 °C(Predicted)
Density  1.30±0.1 g/cm3(Predicted)
storage temp.  2-8°C
solubility  DMSO: ~1 mg/mlsoluble
pka 8.13±0.60(Predicted)
form  Liquid
color  Orange
Water Solubility  Insoluble in water.
Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 6 months.

Safety information for GF109203X

Signal word Danger
Pictogram(s)
ghs
Health Hazard
GHS08
GHS Hazard Statements H350:Carcinogenicity
Precautionary Statement Codes P201:Obtain special instructions before use.
P202:Do not handle until all safety precautions have been read and understood.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P308+P313:IF exposed or concerned: Get medical advice/attention.
P405:Store locked up.
P501:Dispose of contents/container to..…

Computed Descriptors for GF109203X

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