CAS NO: | 62996-74-1 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases withIC50s of 6 nM, 15 nM, 2 nM, and 3 nM forPKC,PKA,c-Fgr, andPhosphorylase kinaserespectively. Staurosporine also inhibitsTAOK2with an IC50of 3 μM. Staurosporine is anapoptosisinducer[1][2][3][4][5]. | |||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Staurosporine, widely used as a protein kinase C (PKC) inhibitor with a broad spectrum of activity, is an alkaloid isolated from the culture broth ofStreptomyces 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[2]. | |||||||||||||||||
体内研究 (In Vivo) | 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[3]. 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[4]. | |||||||||||||||||
分子量 | 466.53 | |||||||||||||||||
性状 | Solid | |||||||||||||||||
Formula | C28H26N4O3 | |||||||||||||||||
CAS 号 | 62996-74-1 | |||||||||||||||||
中文名称 | 星形孢菌素 | |||||||||||||||||
结构分类 |
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来源 | Streptomyces staurosporeus | |||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | |||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(133.97 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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