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  3. Staurosporine

Staurosporine  (Synonyms: Antibiotic AM-2282; STS; AM-2282)

Cat. No.: HY-15141 Purity: 99.81%
COA Handling Instructions

Staurosporine est un inhibiteur puissant et non sélectif des protéines kinases avec des IC50s de 6 nM, 15 nM, 2 nM et 3 nM pour PKC, PKA, c-Fgr et Phosphorylase kinase respectivement.

Staurosporin ist ein wirksamer und nicht selektiver Inhibitor von Proteinkinasen mit IC50-Werten von 6 nM, 15 nM, 2 nM und 3 nM für PKC-, PKA-, c-Fgr- bzw. Phosphorylase-Kinase.

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.

For research use only. We do not sell to patients.

Staurosporine Chemical Structure

Staurosporine Chemical Structure

CAS No. : 62996-74-1

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5 mg USD 132 In-stock
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Customer Review

Based on 114 publication(s) in Google Scholar

Top Publications Citing Use of Products

110 Publications Citing Use of MCE Staurosporine

WB

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

    PMA markedly reduces the protein level of GLT-1.

    Staurosporine purchased from MedChemExpress. 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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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)

    In Vitro

    Staurosporine, widely used as a protein kinase C (PKC) inhibitor with a broad spectrum of activity, is an alkaloid which can be 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[2].

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

    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].

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

    Molecular Weight

    466.53

    Formula

    C28H26N4O3

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(NC1)C2=C1C3=C(C4=C2C5=C(C=CC=C5)N4[C@H]6C[C@@H](NC)[C@@H](OC)[C@]7(C)O6)N7C8=CC=CC=C83

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 62.5 mg/mL (133.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent 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 4.2870 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.46 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.46 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
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    %
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    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.98%

    References
    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.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 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
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    • 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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