Staurosporine

Article number:

5500664

CAS No.:

62996-74-1

Formula:

C28H26N4O3

Chemical description:

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

Synonyms:

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

Molecular weight:

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

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Staurosporine

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