K-252b, c and d, potent inhibitors of protein kinase C from microbial origin.
Nocardiopsis sp. K-290 was found to produce novel metabolites, designated K-252b, c and d, which were structurally related to K-252a. These compounds were isolated from the culture broth and the physico-chemical and biochemical properties were examined. The compounds strongly inhibited protein kinase C. IC50 values (the concentrations causing 50% inhibition) for the effects of K-252b, c and d on the rat brain enzyme were 38.3, 214, and 337 nM, respectively.
D000192:Actinomycetales / Q000378:metabolism; D001419:Bacteria / Q000187:drug effects; D002147:Calmodulin / Q000037:antagonists & inhibitors; D002227:Carbazoles / Q000302:isolation & purification* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D026121:Indole Alkaloids; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*
D002147:Calmodulin; D002227:Carbazoles; D026121:Indole Alkaloids; D010726:Phosphodiesterase Inhibitors; C049985:staurosporine aglycone; D011493:Protein Kinase C