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Staurosporine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Staurosporine图片
CAS NO:62996-74-1
包装与价格:
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

产品名称
星形孢菌素
Antibiotic AM-2282
STS
AM-2282
产品介绍
Staurosporine 是一种有效,ATP 竞争性的,非选择性蛋白激酶抑制剂,抑制PKCPKAc-Fgr,和Phosphorylase kinaseIC50分别为 6 nM,15 nM,2 nM,3 nM。Staurosporine 也抑制TAOK2,IC50值 3 μM。Staurosporine 是一个凋亡诱导剂。
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]

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)

Ca2+/CaM PK-I1

20 nM (IC50)

MLCK

21 nM (IC50)

IR

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 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
  • Alkaloids
  • Indole Alkaloids
来源

Streptomyces staurosporeus

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1435 mL10.7174 mL21.4348 mL
5 mM0.4287 mL2.1435 mL4.2870 mL
10 mM0.2143 mL1.0717 mL2.1435 mL
*

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
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

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
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.

    请依序添加每种溶剂: 0.5%CMC-Na/saline water

    Solubility: 3.33 mg/mL (7.14 mM); Suspension solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 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 ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin 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 μL20% 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.

    请依序添加每种溶剂: 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。

*以上所有助溶剂都可在本网站选购。