GF109203X

Bezeichnung:GF109203X

CAS-Nr133052-90-1

Englisch Name:GF109203X

CBNumberCB2103079

SummenformelC25H24N4O2

Molgewicht412.48

MOL-Datei133052-90-1.mol

GF109203X physikalisch-chemischer Eigenschaften

Schmelzpunkt	280℃ (decomposition)
Siedepunkt	685.6±55.0 °C(Predicted)
Dichte	1.30±0.1 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: ~1 mg/mlsoluble
Aggregatzustand	Liquid
pka	8.13±0.60(Predicted)
Farbe	Orange
Wasserlöslichkeit	Insoluble in water.
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 6 months.

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	40-22
S-Sätze:	36/37
WGK Germany	3
RTECS-Nr.	UX9590000
HS Code	2925199590

Gefahreninformationscode (GHS)

GF109203X Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R40:Verdacht auf krebserzeugende Wirkung.
S-Sätze Betriebsanweisung:
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
Beschreibung
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.
Verwenden
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.
Biologische Aktivität
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.
Lager
Store at RT
Einzelnachweise
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

GF109203X Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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