Staurosporine (AM-2282) 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。

别名：AM-2282; STS; CGP 41251

规格	价格	库存状态
2mg	¥ 750	中国库存现货
5mg	¥ 1300	中国库存现货
10mg	¥ 2180	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： 99.24%
COA
MSDS
H-NMR
HPLC

产品信息

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。

使用AbMole产品发表的文献

Inflamm Regen. 2023 Jun 20;43(1):31.

Promotion of axon regeneration and protection on injured retinal ganglion cells by rCXCL2
Biomaterials. 2021 Aug;275:120958.

Tumor progress intercept by intervening in Caveolin-1 related intercellular communication via ROS-sensitive c-Myc targeting therapy
Pak Vet J. 2021 Mar.

Evaluation of the PBMC Proliferation, Apoptosis and Cytokines Profiling in Cattle Infected with Mycoplasma bovis Strain 07801
PLoS One. 2019 Oct 10;14(10):e0223096.

Optimized bioluminescence analysis of adenosine triphosphate (ATP) released by platelets and its application in the high throughput screening of platelet inhibitors.
Food Chem. 2017 Mar 15;219:304-310.

Effects of protein phosphorylation on color stability of ground meat
Food Chem. 2017 Sep 20.

Dephosphorylation enhances postmortem degradation of myofibrillar proteins

产品使用成果展示

	数据来源	Food Chem (2017). Figure 3. Staurosporine (Abmole Bioscience,Houston, TX, USA)
	方法	Measured myofibril fragmentation index
	细胞系/动物模型	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/动物模型	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/动物模型
	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/动物模型
	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/动物模型
	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/动物模型
	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."

实验参考

体外实验*
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

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
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

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	466.53
分子式	C28H26N4O3
CAS号	62996-74-1
溶解性（25°C）	DMSO ≥ 50 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

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

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
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
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Manns J, et al. FASEB J. Triggering of a novel intrinsic apoptosis pathway by the kinase inhibitor staurosporine: activation of caspase-9 in the absence of Apaf-1.

[2] Antonsson A, et al. Anticancer Res. 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.

[3] Zhang XD, et al. Mol Cancer Ther. Staurosporine induces apoptosis of melanoma by both caspase-dependent and -independent apoptotic pathways.

[4] Tamaoki T, et al. Biochem Biophys Res Commun. Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase.

[5] Hara H, et al. J Cereb Blood Flow Metab. Staurosporine, a novel protein kinase C inhibitor, prevents postischemic neuronal damage in the gerbil and rat.

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