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包装规格:1mg 5mg 25mg in glass bottle
溶解性:溶于DMSO(25mg/ml)和DMF(25mg/ml)
产品描述:基本信息 产品编号:S10103 产品名称:Staurosporine CAS: 62996-74-1   储存条件 粉末 -20℃ 四年     分子式: C28H26N4O3 溶于液体 -80℃ 六个月 分子量: 466.53 -20℃ 一个月 化学名:      Solubility (25°C)   体外 DMSO 46mg/mL (98.6mM) Ethanol Insoluble Water Insoluble 体内(现配现用)     <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.1435mL 10.7174mL 21.4348mL 5mM 0.4287mL 2.1435mL 4.2870mL 10mM 0.2143mL 1.0717mL 2.1435mL 50mM 0.0429mL 0.2143mL 0.4287mL   生物活性 产品描述 一种具有抗真菌活性的微生物碱,抑制多种蛋白激酶,包括PKA(Ki=7.0nM IC50=15nM)、PKG(Ki=8.5nM)、MYLK(MLCK,Ki=1.3nM)、PKC(Ki=0.7nM)、CaMK(IC50=20nM)、CAMKII(Ki=20nM)、酪氨酸激酶(IC50=70nM)和磷酸化酶激酶(IC50=0.5nM)。 靶点/IC50 PKCα(Cell-free assay) c-Fgr (Cell-free assay) phosphorylase kinase (Cell-free assay) PKCη (Cell-free assay) PKCγ(Cell-free assay) 2nM 2nM 3nM 4nM 5nM   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 (100nM) 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 (100nM) 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. 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 10ng 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 0.1mg/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 (0.1mg/kg) partially reversed the decrease of choline acetyltransferase activity in the fronto-parietal cortex induced by basal forebrainlesion.These results suggest that Staurosporine attenuates impairment of learning through reversal of damage to cholinergic neurons induced by basal forebrain-lesion.     推荐实验方法(仅供参考) 细胞实验:   细胞系 PC12 浓度 溶于DMSO,终浓度为1μM 处理时间 ~32小时 方法 使用Staurosporine处理细胞32小时。细胞在4%多聚甲醛中混合,然后使用DNA结合染料Hoechst 33342染色。在荧光照明下观察细胞,测定凋亡细胞百分数。   动物实验:   Mice Female CD-I mice are used. Various amounts of Staurosporine in 10μL of acetone are applied to the ears of 8-wk-old CD-I mice. The extent of irritation is expressed as the minimum dose of the compound causing irritation. Induction of HOC in Mouse Skin Staurosporine in 0.1mL of acetone is applied to the skin of the backs of CD-I mice, and a crude enzyme extract is obtained from the skin 18h later. HDC activity is expressed as pmol of CO2 released per mg of protein per lh of incubation.Induction of ODC in Mouse Skin Staurosporine in 0.2mL of acetone is applied to the skin of the backs of CD-I mice. After 4h,a crude enzyme extract is prepared from the epidermis,and its ODC activity is measured. Enzyme activity is expressed as nmol of CO2 per mg of protein per 30 min of incubation.
保存条件:-20℃