1. Epigenetics
    TGF-beta/Smad
    Protein Tyrosine Kinase/RTK
    Stem Cell/Wnt
  2. PKC
    PKA
  3. Staurosporine

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

Cat. No.: HY-15141 Purity: 99.98%
Handling Instructions

Staurosporine is a potent 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.

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

Staurosporine Chemical Structure

Staurosporine Chemical Structure

CAS No. : 62996-74-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 135 In-stock
Estimated Time of Arrival: December 31
2 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 28 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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: Cancer Res. 2013 Apr 15;73(8):2574-86.

    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.

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

    PMA markedly reduces the protein level of GLT-1.

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

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

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Staurosporine is a potent 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.

    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 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].

    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].

    Molecular Weight

    466.53

    Formula

    C₂₈H₂₆N₄O₃

    CAS No.

    62996-74-1

    SMILES

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

    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 : ≥ 31 mg/mL (66.45 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.2143 mL 1.0717 mL 2.1435 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.98%

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    Staurosporine
    Cat. No.:
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