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  2. PKC PKA Apoptosis Bacterial Fungal Antibiotic
  3. Staurosporine

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

目录号: HY-15141 纯度: 99.81%
COA 产品使用指南

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。

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Staurosporine Chemical Structure

Staurosporine Chemical Structure

CAS No. : 62996-74-1

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10 mM * 1 mL in DMSO ¥1673
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Customer Review

MCE 顾客使用本产品发表的 89 篇科研文献

WB

    Staurosporine purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2018 Aug;1864(8):2600-2609.  [Abstract]

    Expression of Nogo-B and apoptosis-related proteins determined by Western blot analysis.

    Staurosporine purchased from MCE. Usage Cited in: Int Immunopharmacol. 2017 Sep;50:30-37.  [Abstract]

    BV-2 cells are pretreated with or without Staurosporine (1 μM) for 30 min, and then incubated with 20 μM Aβ1–42 for 24 h. The protein expression of TNF-α, IL-1β, and IL-6 are detected by western blot.

    Staurosporine purchased from MCE. Usage Cited in: Neuroscience. 2017 Dec 4;365:217-225.  [Abstract]

    PMA markedly reduces the protein level of GLT-1.

    Staurosporine purchased from MCE. Usage Cited in: Cancer Res. 2013 Apr 15;73(8):2574-86.  [Abstract]

    Cells are treated with the indicated concentrations of AZD8055, Torin2 or staurosporin overnight and analyzed by western blot using antibodies specific for the indicated proteins.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    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[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 是一种能够从 Streptomyces staurospores 培养液中分离出来的生物碱,广泛用作蛋白激酶 C (PKC) 抑制剂,具有广谱活性。MC3T3E-1 成骨细胞暴露于 Staurosporine (100 nM) 12 小时后,释放出与对照细胞 (10.0±2.4%) 相似的 LDH 量 (12.4±3.1%),表明相对缺乏裂解细胞死亡,发生在坏死。此外,用 Staurosporine (100 nM) 处理会导致形态学变化,这是细胞凋亡的特征:在 Hoechst 33258 染色后通过荧光显微镜观察到亮蓝色荧光浓缩核,细胞体积减小[2]

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

    体内研究
    (In Vivo)

    Staurosporine 的抑制作用在肿瘤促进的第 10 周左右具有统计学意义。尽管在实验的后几周使用 10 ng Staurosporine 没有获得统计学上显著的抑制作用,但荷瘤小鼠的百分比和每只小鼠的平均肿瘤数明显呈下降趋势。因此,即使在 Staurosporine 本身诱导肿瘤的剂量下,Staurosporine 也会轻微抑制 Teleocidin 的肿瘤促进作用[3]。Staurosponne (0.05 和 0.1 mg/kg 腹膜内注射) 可减轻水迷宫和被动回避任务的受损性能,即使给药是在损伤后 2 周开始的。此外,Staurosporine (0.1 mg/kg) 部分逆转了由基底前脑损伤引起的额顶叶皮层中胆碱乙酰转移酶活性的降低。这些结果表明 Staurosporine 通过逆转由基底前脑损伤引起的胆碱能神经元损伤来减轻学习障碍[4]

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

    分子量

    466.53

    Formula

    C28H26N4O3

    CAS 号
    性状

    固体

    颜色

    White to yellow

    中文名称

    星形孢菌素

    结构分类
    初始来源

    Streptomyces staurosporeus

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 62.5 mg/mL (133.97 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    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
    查看完整储备液配制表

    * 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    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

    • 方案 一

      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); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.46 mM); 悬浊液; 超声助溶

      此方案可获得 2.08 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      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。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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。

    • 方案 一

      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; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.98%

    参考文献
    Animal Administration
    [3][4]

    Mice[3]
    Female CD-I mice are used. Various amounts of Staurosporine in 10 μL 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 0.1 mL of acetone is applied to the skin of the backs of CD-I mice, and a crude enzyme extract is obtained from the skin 18 h later. HDC activity is expressed as pmol of CO2 released per mg of protein per l h of incubation. Induction of ODC in Mouse Skin Staurosporine in 0.2 mL of acetone is applied to the skin of the backs of CD-I mice. After 4 h, 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.
    Rats[4]
    Male Kbl Wistar rats(weighing 270 to 310 g) are used. In the group which is given Staurosporine for 2 weeks, the water maze task and Staurosporine administration are started 2 weeks after the BF-lesion, and the passive avoidance task is carried out 4 weeks after the BFlesion. The rat received Staurosporine at doses of 0.01, 0.03, 0.1, and 0.3 mg/kg (i.p., N=10 in each group for 2 weeks) 30 mm prior to the water maze training sessions and the passive avoidance task acquisitiontrial. In the group which is given Staurosporine for 4 weeks, the drug is first given 2 weeks after the BF-lesion. The water maze task is carried out 4 weeks after the BF-lesion. The passive avoidance task is carried out 6 weeks after the BF-lesion. The rat received Staurosporine at 0.05, 0.1, and 0.2 mg/kg (i.p., N=10 in each group) once a day for 2 weeks before training, and for 2 weeks after the water maze training sessions and the passive avoidance task acquisition trial. Staurosporine is suspended in 0.3% of sodium carboxymethyl cellulose. The vehicle is administered to the non-lesioned controls and the lesioned controls on the same schedule as the Staurosporine-treated animals.

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

    参考文献

    完整储备液配制表

    * 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1435 mL 10.7174 mL 21.4348 mL 53.5871 mL
    5 mM 0.4287 mL 2.1435 mL 4.2870 mL 10.7174 mL
    10 mM 0.2143 mL 1.0717 mL 2.1435 mL 5.3587 mL
    15 mM 0.1429 mL 0.7145 mL 1.4290 mL 3.5725 mL
    20 mM 0.1072 mL 0.5359 mL 1.0717 mL 2.6794 mL
    25 mM 0.0857 mL 0.4287 mL 0.8574 mL 2.1435 mL
    30 mM 0.0714 mL 0.3572 mL 0.7145 mL 1.7862 mL
    40 mM 0.0536 mL 0.2679 mL 0.5359 mL 1.3397 mL
    50 mM 0.0429 mL 0.2143 mL 0.4287 mL 1.0717 mL
    60 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8931 mL
    80 mM 0.0268 mL 0.1340 mL 0.2679 mL 0.6698 mL
    100 mM 0.0214 mL 0.1072 mL 0.2143 mL 0.5359 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    目录号:
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