Staurosporine 是一种有效，ATP 竞争性的，非选择性蛋白激酶抑制剂，抑制 PKC，PKA，c-Fgr，和 Phosphorylase kinase 的 IC50 分别为 6 nM，15 nM，2 nM，3 nM。Staurosporine 也抑制 TAOK2，IC50 值 3 μM。Staurosporine 是一个凋亡诱导剂。
| CAS No. | 62996-74-1 |
| 生物活性 | Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC50 of 3 μM. Staurosporine is an apoptosis inducer. |
| 分子式 | C28H26N4O3 |
| 分子量 | 466.53 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : 62.5 mg/mL (133.97 mM; Need ultrasonic) |
| 体内研究 | The inhibitory effect of Staurosporine is statistically significant at around Wk 10 of tumor promotion. Although statistically significant inhibition is not obtained with 10 ng of Staurosporine in later weeks of the experiment, a decreasing tendency in the percentages of tumor bearing mice and in average numbers of tumors per mouse is apparent. Thus, Staurosporine slightly inhibits tumor promotion of Teleocidin, even at the dose at which Staurosporine itself induced tumors. Staurosponne (0.05 and 0.1 mg/kg intraperitoneal) attenuates the impaired perlormance of water maze and passive avoidance tasks, even though the drug administration began 2 weeks after the lesion. Moreover, Staurosporine (0.1 mg/kg) partially reversed the decrease of choline acetyltransferase activity in the fronto-parietal cortex induced by basal forebrain-lesion. These results suggest that Staurosporine attenuates impairment of learning through reversal of damage to cholinergic neurons induced by basal forebrain-lesion. |
| 体外研究 | Staurosporine, widely used as a protein kinase C (PKC) inhibitor with a broad spectrum of activity, is an alkaloid isolated from the culture broth of Streptomyces staurospores. MC3T3E-1 osteoblasts, expose to Staurosporine (100 nM) for 12 h, release an amount of LDH (12.4±3.1%) that is similar to that release by the control cells(10.0±2.4%), indicating the relative absence of lytic death, which occurs in necrosis. In addition, treatment with Staurosporine (100 nM) results in morphological changes, characteristic of apoptosis: a brightblue fluorescent condensed nuclei seen through a fluorescence microscope after Hoechst 33258-staining, and a reduction of cell volume. |
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