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

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

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

Staurosporine is a very potent universal inhibitor of protein kinases but showing little selectivity, with IC50 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 $113 In-stock
2 mg $80 In-stock
5 mg $110 In-stock
10 mg $150 In-stock
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Customer Review

    Staurosporine purchased from MCE. Usage Cited in: Int Immunopharmacol. 2017 Jun 14;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: Sci Rep. 2015 Aug 3;5:12728.

    Ganetespib decreases the DYRK1A protein level. 293T cells are transiently transfected with an expression vector for 3xFLAG-DYRK1A. At 24 h after transfection, the cells are treated with Ganetespib (100 nM) and collected 0 and 8 h after treatment. Total cell lysates are subjected to SDS-PAGE followed by Western blot analysis using antibodies against FLAG and GAPDH. In the control group (DMSO), expression of 3xFLAG-DYRK1A increases at 8 h compared to 0 h, and Ganetespib suppresses this increase of

    Staurosporine purchased from MCE. Usage Cited in: Int Immunopharmacol. 2017 Jun 14;50:30-37.

    BV-2 cells are pretreated with or without Bay11-7082 (10 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Staurosporine is a very potent universal inhibitor of protein kinases but showing little selectivity, with IC50 of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase, respectively.

    IC50 & Target

    IC50: 6 nM/15 nM/2 nM/3 nM (PKC/PKA/c-Fgr/Phosphorylase kinase)[1]

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Kinase Assay
    [2]

    MC3T3E-1 cells (2×106 cells/group) are treated with 100 nM Staurosporine for various time periods and lysed in a lysis buffer (EB buffer: 1% Triton X-100, 10 mM Tris, pH 7.6, 50 mM NaCl, 1 mg/mL Aprotinin, 5 mM EDTA, 50 mM NaF, 0.1% 2-mercaptoethanol, and 100 μM sodium orthovanadate). The lysate of the cells is subjected to centrifugation at 12 000 g at 4°C for 30 min. Soluble fraction is collected and incubated with anti-JNK1 antibodies. After incubation on ice for 3 h, 100 μL of a 10% solution of formalin-fixed Staphylococcus aureus is added to the anti-JNK1 immunoprecipitates and further incubated on ice for 1 h. The absorbed immune complex is washed twice with EB buffer and PAN buffer (10 mM PIPES buffer, pH 7.0, 1% aprotinin, 100 mM NaCl). The immunecomplex is mixed with 2 μg of GST-c-Jun NT1-79 proteins as a substrate in 30 μL of the reaction buffer containing 2 μM cold ATP, 2 mM DTT, 20 mM MgCl2, 2 μCi [γ33-P]-ATP, and 20 mM Tris-HCl, pH 7.5 at 30°C for 20 min. The reaction is terminated by adding 15 μL of 3× SDS-PAGE sample buffer and boiling at 98°C for 5 min. The proteins are separated on 12% SDS-PAGE and transferred onto a nitrocellulose membrane via the semi-dry electrotransfer system. The membrane is immunoblotted with rabbit anti-JNK1 antibodies and horse radish peoxidaseconjugated anti-rabbit antibodies to visualize the signals measured by an enhanced chemiluminescence system. The gel is dried under a vacuum, and the phosphotransferase activity is visualized by autoradiography and quantified by a PhosphoImager analyzer[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    Staurosporine is suspended in 0.3% of sodium carboxymethyl cellulose (Rat)[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
    Molecular Weight

    466.53

    Formula

    C₂₈H₂₆N₄O₃

    CAS No.

    62996-74-1

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

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 31 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.98%

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    Cat. No.:
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