A new inhibitor of protein kinase C, RK-1409 (7-oxostaurosporine). I. Taxonomy and biological activity.
A novel inhibitor of protein kinase C was found in the fermentation of a soil actinomycete, strain RK-1409. According to the taxonomic studies, the producing strain was designated as Streptomyces platensis subsp. malvinus RK-1409. The protein kinase C inhibitor, RK-1409 (7-oxostaurosporine) inhibited the morphological change of a human chronic erythroleukemia cell, K-562, induced by phorbol 12,13-dibutyrate (PDBu) at the concentration of 10 ng/ml. The concentration of 3 ng/ml inhibited the activity of protein kinase C in vitro. RK-1409 inhibited the cell cycle progression at G2 phase of K-562 cells.
Osada
H
H
RIKEN, Institute of Physical and Chemical Research, Saitama, Japan.
Koshino
H
H
Kudo
T
T
Onose
R
R
Isono
K
K
D000470:Alkaloids / Q000494:pharmacology*; D002227:Carbazoles / Q000494:pharmacology; D016195:G2 Phase / Q000187:drug effects*; D026121:Indole Alkaloids; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D019311:Staurosporine / Q000031:analogs & derivatives; D013302:Streptomyces / Q000145:classification* / Q000302:isolation & purification / Q000378:metabolism
D000470:Alkaloids; D002227:Carbazoles; D026121:Indole Alkaloids; C063438:4'-demethylamino-4'-hydroxystaurosporine; C073929:7-oxostaurosporine; C049985:staurosporine aglycone; D011493:Protein Kinase C; D019311:Staurosporine