GF109203X Chemical Properties

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

Hazard Codes 

Xn

Risk Statements 

40-22

Safety Statements 

36/37

WGK Germany 

3

RTECS 

UX9590000

HS Code 

2925199590

MSDS

• Language:English Provider:SigmaAldrich

GF109203X Usage And Synthesis

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.

Uses

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.

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

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