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Staurosporine 星孢菌素

目录号 M2066 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


Staurosporine (AM-2282)是一种有效的PKC抑制剂,作用于PKCα, PKCγ和PKCη时,IC50分别为2 nM, 5 nM和4 nM,对PKCδ(20 nM), PKCε(73 nM)和PKCζ(1086 nM)作用效果稍弱。

Staurosporine结构式

别名:AM-2282

包装 价格 库存状态
2mg 原价 ¥ 980
促销价 ¥ 931
中国库存现货
5mg 原价 ¥ 1680
促销价 ¥ 1596
中国库存现货
10mg 原价 ¥ 2940
促销价 ¥ 2793
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
生物活性

Staurosporine (AM-2282)是一种有效的PKC抑制剂,作用于PKCα, PKCγ和PKCη时,IC50分别为2 nM, 5 nM和4 nM,对PKCδ(20 nM), PKCε(73 nM)和PKCζ(1086 nM)作用效果稍弱。Staurosporine 也强抑制HeLa S3细胞,IC50为4 nM。Staurosporine 也抑制多种其他蛋白激酶,包括PKA, PKG, 磷酸激酶, S6 激酶, 肌球蛋白轻链激酶(MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, 和Syk , IC50分别为 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, 和 16 nM。 Staurosporine (1 μM) 诱导 PC12细胞90%以上凋亡,这种作用可被过量表达的Bcl-2抑制,或者zVAD-fmk, cycloheximide (10 μM) 及actinomycin D (5 μM)处理也可抑制。

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 PC12
方法 Cells are exposed to Staurosporine for ~32 hours. Cells are fixed in 4% paraformaldehyde and stained with the DNA-binding dye Hoechst 33342. Cells are visualized under epifluorescence illumination, and the percentage of apoptotic cells (cells with condensed and fragmented DNA) is determined.
浓度 Dissolved in DMSO, final concentration 1 μM
处理时间 ~32 hours
动物实验
动物模型 Male Mongolian gerbils or male Wistar rats subjected to transient ischemia
配制 Dissolved in DMSO, and diluted in saline
剂量 ~10 ng
给药处理 Stereotaxically administered into the bilateral CAl subfield of the hippocampus
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据
分子量 466.53
分子式 C28H26N4O3
CAS号 62996-74-1
纯度 99.68%
溶解性(25°C) DMSO: ≥ 10 mg/mL
储存和运输条件 固体粉末: -20°C 冷藏长期储存
常温运输及临时存放
储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.1435 mL 10.7174 mL 21.4348 mL
5 mM 0.4287 mL 2.1435 mL 4.287 mL
10 mM 0.2143 mL 1.0717 mL 2.1435 mL
使用AbMole产品发表的文献
客户产品验证及相关生物数据
数据来源 Food Chem (2017). Figure 3. Staurosporine (Abmole Bioscience,Houston, TX, USA)
方法 Measured myofibril fragmentation index
细胞系 Muscles
浓度 0.144 μmol/5 g
处理时间 2 h, 1 d, 2 d, 3 d, 5 d and 7 day
实验结果 During the MFI increased phase (measured at 2 h and 1 d), the MFI values of the low phosphorylation level group (protein kinase inhibited group) were significantly higher (p < 0.05) than those of the control group, while the MFI values of the high phosphorylation level group (phosphatase inhibited group) were significantly lower (p < 0.05) than those of the control group.
数据来源 Food Chem (2017). Figure 2. Staurosporine (Abmole Bioscience,Houston, TX, USA)
方法 Global phosphorylation level of myofibrillar proteins
细胞系 Muscles
浓度 0.144 μmol/5 g
处理时间 2 h, 1 d, 2 d, 3 d, 5 d and 7 day
实验结果 Inhibition of protein kinase by M2066 significantly reduced the phosphorylation level of myofibrillar proteins in muscle compared to control.
数据来源 Food Chemistry (2016).Figure 4. kinase inhibitors (M2066, Abmole, Houston, TX, USA)
方法 Lactic acid concentrations
细胞系
浓度 0.144 μmole per 5 g muscle pieces
处理时间 2h, 24h, 48h, 72h, 120h and 168h
实验结果 No difference was observed in lactic acid content (Fig. 4) between C1 and C2 control groups. In addition, no difference in lactic acid was detected between phosphatase inhibition group and the two control groups at most time points, but the kinase inhibition group had lower lactic acid content than the other three groups (P < 0.05) throughout the entire experimental period.
数据来源 Food Chemistry (2016).Figure 3. kinase inhibitors (M2066, Abmole, Houston, TX, USA)
方法 PH Value
细胞系
浓度 0.144 μmole per 5 g muscle pieces
处理时间 2h, 24h, 48h, 72h, 120h and 168h
实验结果 There was no difference in pH values (Fig. 3) between the phosphatase inhibition group and the two control groups. the pH of the kinase inhibition group declined much slower during the early postmortem stage (P < 0.05) as compared to the other three groups.
数据来源 Food Chemistry (2016).Figure 2. kinase inhibitors (M2066, Abmole, Houston, TX, USA)
方法 protein phosphrylation assay
细胞系
浓度 0.144 μmole per 5 g muscle pieces
处理时间 2h, 24h, 48h, 72h, 120h and 168h
实验结果 The R630/580 values (Fig. 2) were not different between C1 and C2 control groups at any time. However, the R630/580 values of the phosphatase inhibition group were lower than those of all other groups (P < 0.05) except at 2 h. Kinase inhibition group demonstrated greater (P < 0.05) R630/580 values than those of the rest groups except at 2 and 168 h.
数据来源 Food Chemistry (2016).Figure 1. kinase inhibitors (M2066, Abmole, Houston, TX, USA)
方法 Gel electrophoresis and image analyses
细胞系
浓度 0.144 μmole per 5 g muscle pieces
处理时间 2h, 24h, 48h, 3d, 5d and 7d
实验结果 "As expected, the overall phosphorylation of sarcoplasmic proteins in the minced meat with phosphatase inhibitor was significantly higher (P < 0.05) than in control and kinase inhibitor added samples."
参考文献

Triggering of a novel intrinsic apoptosis pathway by the kinase inhibitor staurosporine: activation of caspase-9 in the absence of Apaf-1.
Manns J, et al. FASEB J. 2011 Sep;25(9):3250-61. PMID: 21659556.

Induction of apoptosis by staurosporine involves the inhibition of expression of the major cell cycle proteins at the G(2)/m checkpoint accompanied by alterations in Erk and Akt kinase activities.
Antonsson A, et al. Anticancer Res. 2009 Aug;29(8):2893-8. PMID: 19661292.

Staurosporine induces apoptosis of melanoma by both caspase-dependent and -independent apoptotic pathways.
Zhang XD, et al. Mol Cancer Ther. 2004 Feb;3(2):187-97. PMID: 14985459.

Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase.
Tamaoki T, et al. Biochem Biophys Res Commun. 1986 Mar 13;135(2):397-402. PMID: 3457562.

Staurosporine, a novel protein kinase C inhibitor, prevents postischemic neuronal damage in the gerbil and rat.
Hara H, et al. J Cereb Blood Flow Metab. 1990 Sep;10(5):646-53. PMID: 2384538.

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