Staurosporine.|62996-74-1|(星形孢菌素; Antibiotic AM-2282; STS; AM-2282)-陌孚医药/Medlife

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Staurosporine. (Synonyms: 星形孢菌素; Antibiotic AM-2282; STS; AM-2282)

目录号: PC16063 纯度: ≥98%

CAS No. :62996-74-1

商品编号	规格	价格	会员价
PC16063-1mg	1mg	¥490.00	请登录
PC16063-5mg	5mg	¥1960.00	请登录
PC16063-10mg	10mg	¥3430.00	请登录
PC16063-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥2009.00	请登录

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中文名称

Staurosporine.

中文别名

星孢菌素;链霉菌属十字孢碱;十字孢碱;链霉菌属十字孢碱分子生物学试剂;十字胞碱;星形孢菌素;星胞菌素;Staurosporine 抑制剂;孢菌素标准品;星孢菌素, 来源于链霉菌

英文名称

Staurosporine

英文别名

Staurosporine;STSP;ANTIBIOTIC M 193;ANTIBIOTIC AM-2282;[9S-(9A,10B,11B,13A)]-2,3,10,11,12,13-HEXAHYDRO-10-METHOXY-9-METHYL-11-(METHYLAMINO)-9,13-EPOXY-1H,9H-DIINDOLO[1,2,3-GH:3',2',1'-1M]PYRROLO[3,4-J][1,7]BENZODIAZONIN-1-ONE;2,3,10,11,12,13-HEXAHYDRO-10R-METHOXY-9S-METHYL-11R-METHYLAMINO-9S,13R-EPOXY-1H,9H-DIINDOLO[1,2,3-GH:3',2',1'-LM]PYRROLO[3,4-J][1,7]BENZODIAZONIN-1 ONE;STAUROSPORINE FROM STREPTOMYCES SP.;STAUROSPORINE READY-MADE SOLUTION;STAUROSPORINE FROM STREPTOMYCES SP., PGE WITH 250 UG;Staurosporine from Streptomyces sp;Staurosporin;staurosporine (Antibiotic AM-2282,Stsp);AM-2282;Antibiotic 230;Stauroporine;staurosphorine;STS;protein kinase c inhibitor;Staurosporine, 98%;Kinome_3629

Cas No.

62996-74-1

分子式

C₂₈H₂₆N₄O₃

分子量

466.53

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

IC50 & Target[1][2]

PKC

6 nM (IC₅₀)

PKA

15 nM (IC₅₀)

c-Fgr

2 nM (IC₅₀)

Phosphorylase kinase

3 nM (IC₅₀)

S6 kinase (70 kDa)

5 nM (IC₅₀)

v-Src

6 nM (IC₅₀)

cdc2

9 nM (IC₅₀)

TPK-IIB/Syk

16 nM (IC₅₀)

Ca/CaM PK-I1

20 nM (IC₅₀)

MLCK

21 nM (IC₅₀)

61 nM (IC₅₀)

EGF-R

100 nM (IC₅₀)

ERK-1

1500 nM (IC₅₀)

CSK

2000 nM (IC₅₀)

IGF-IR

6150 nM (IC₅₀)

CK2

19500 nM (IC₅₀)

CK1

163500 nM (IC₅₀)

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 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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. 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

结构分类

来源

Streptomyces staurosporeus

参考文献

[1]. Meggio F, et al. Different susceptibility of protein kinases to staurosporine inhibition. Kinetic studies and molecular bases for the resistance of protein kinase CK2. Eur J Biochem. 1995 Nov 15;234(1):317-22. [Information]

[2]. Chae HJ, et al. Molecular mechanism of staurosporine-induced apoptosis in osteoblasts. Pharmacol Res. 2000 Oct;42(4):373-81. [Information]

[3]. Yoshizawa S, et al. Tumor-promoting activity of staurosporine, a protein kinase inhibitor on mouse skin.Cancer Res. 1990 Aug 15;50(16):4974-8. [Information]

[4]. Nabeshima T, et al. Staurosporine facilitates recovery from the basal forebrain-lesion-induced impairment of learning and deficit of cholinergic neuron in rats. J Pharmacol Exp Ther. 1991 May;257(2):562-6. [Information]

[5]. Yujie Ren, et al. The ORF3a Protein of SARS-CoV-2 Induces Apoptosis in Cells. Cell Mol Immunol. 2020 Jun 18;1-3. [Information]

溶解度数据

体外研究:

DMSO : 62.5 mg/mL (133.97 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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	4.2870 mL
10 mM	0.2143 mL	1.0717 mL	2.1435 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 3.33 mg/mL (7.14 mM); Suspension solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.46 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.46 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (4.46 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.46 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.46 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.46 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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