Staurosporine

Artikelnummer:

5500664

CAS Nr.:

62996-74-1

Formel:

C28H26N4O3

Chemische Beschreibung:

3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one

Synonyme:

(+)-Staurosporine, AM-2282, Alkaloid AM-2282 from Streptomyces, Antibiotic 230, Antibiotic AM 2282, CCRIS 3272, Staurosporin Free Base

Molekulargewicht:

466,54 g/mol

Staurosporine is a natural antibiotic, first isolated in 1977 from Streptomyces staurosporeus (Omura et al, 1977). Staurosporine is a potent inhibitor of many kinases including protein kinase C (IC50 = 0.7 nM), protein kinase A (IC50 = 7 nM), and protein kinase G (IC50 = 8.5 nM). Matsumoto, H. and Sasaki, Y. "Staurosporine, a protein kinase C inhibitor, interferes with proliferation of arterial smooth muscle cells." Biochem. Biophys. Res. Commun. 158: 105-109 (1989). Tamaoki, T., et al. "Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase." Biochem. Biophys. Res. Commun. 135: 397-402 (1986).Staurosporine induces apoptosis in human neuroblastoma cell lines and chick embryonic neurons. Boix, J., et al. "Characterization of the cell death process induced by staurosporine in human neuroblastoma cell lines." Neuropharmacology 36: 811-821 (1997). Wiesner, D.A. and Dawson, G., "Staurosporine induces programmed cell death in embryonic neurons and activation of the ceramide pathway." J. Neurochem. 66: 1418-1425 (1996). In addition, Staurosporine and its analogues exhibit antifungul, antibacterial and immunosuppressive activities. Due to its strong inhibitory effect, Staurosporine is widely used as a PKC inhibitor in the research laboratory. During the last decades, some analogues of Staurosporine were isolated or synthesized in order to improve the its selectivity. An important analogue is K252a, isolated from culture of Nocardiopsis sp. Other semisynthetic analogues are K252b, K252c, KT5823, KT5555, KT5720 and PKC 412. The different analogues share a common structural component, display inhibitory effect on protein kinases, but differ at their inhibition's strength and enzyme's affinity. Origin: Streptomyces staurosporeus

Informieren Sie sich über
Staurosporine

ADCs

Cfm Oskar Tropitzsch GmbH ist bekannt dafür, ausgefallene Forschungsreagenzien zu liefern – in diesem Falle Cytoxoxins für Antikörper. Bei diesen „Warheads“ handelt es sich um hoch toxische Substanzen, wie z.B. ...

Mehr erfahren

Fermentationsprodukte

Allgemein ist Fermentation (von lat. fermentare = gären) definiert als Stoffumwandlung unter aeroben oder anaeroben Bedingungen durch Einwirkung von Mikroorganismen."Mikroorganismus" ist eine Sammelbezeichnung für gewöhnlich mikroskopisch kleine, überwiegend einzellige Organismen ...

Mehr erfahren

Protein Kinase Inhibitoren

Proteinkinasen sind Enzyme, die Phosphatgruppen von hochenergetischen Donoren (meist Nukleosidtriphosphate) auf oberflächenexponierte Serin-, Threonin- oder Tyrosinseitenketten anderer Proteine übertragen und so deren biologische Eigenschaften verändern. Das menschliche Proteom umfasst mehr ...

Mehr erfahren