星形孢菌素，一种磷脂/钙离子依赖性蛋白激酶的强效抑制剂。
Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase.
作者信息
Tamaoki T, Nomoto H, Takahashi I, Kato Y, Morimoto M, Tomita F
出版信息
Biochem Biophys Res Commun. 1986 Mar 13;135(2):397-402. doi: 10.1016/0006-291x(86)90008-2.
Staurosporine, microbial alkaloid which has been known to have antifungal activity was found to inhibit markedly phospholipid/Ca++dependent protein kinase (protein kinase C) from rat brain, with an IC50 value of 2.7 nM. However, it had little effect on the binding of 3H-phorbol-12, 13-dibutyrate (PDBu) to protein kinase C. The inhibition of protein kinase C was not competitive with phospholipid. This compound also showed the strong cytotoxic effect on the growth of HeLa S3 cells, with an IC50 value of 4 X 10(-12)M under the condition of 72 hr-exposure.
星形孢菌素是一种已知具有抗真菌活性的微生物生物碱，它被发现能显著抑制大鼠脑中的磷脂/钙离子依赖性蛋白激酶（蛋白激酶C），半数抑制浓度（IC50）值为2.7纳摩尔。然而，它对3H-佛波醇-12,13-二丁酸酯（PDBu）与蛋白激酶C的结合影响很小。对蛋白激酶C的抑制作用与磷脂不存在竞争性。该化合物对HeLa S3细胞的生长也表现出强烈的细胞毒性作用，在72小时暴露条件下，IC50值为4×10⁻¹²摩尔。
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