_{Staurosporine，又称星形孢菌素，是一种强效的、ATP竞争性激酶抑制剂，有效抑制PKC活性，在大鼠脑组织实验中，IC50为2.7 nM。Staurosporine强效抑制PKC-α，其抑制活性比PKC-δ高100倍，比PKC-δ和PKC-ζ高1000倍。除此之外，Staurosporine还抑制PKA、PKG、p60v-src酪氨酸蛋白激酶和钙调蛋白激酶II等。Staurosporine抑制多种人癌细胞增殖，主要作用表现为诱导癌细胞G2/M期阻断，调整G1期阻断，并诱导细胞凋亡。另外，Staurosporine具有多种生物学作用，如细胞毒性、松弛平滑肌和调节eNOS基因表达等。目前，Staurosporine 已进入临床Phase 3阶段。}

参考文献

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