Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 56.00 | |
2 mg | In stock | $ 79.00 | |
5 mg | In stock | $ 98.00 | |
10 mg | In stock | $ 148.00 | |
25 mg | In stock | $ 259.00 | |
50 mg | In stock | $ 423.00 | |
100 mg | In stock | $ 628.00 | |
500 mg | In stock | $ 1,350.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 111.00 |
Description | Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis. |
Targets&IC50 | PKCε:73 nM, PKCζ:1086 nM, PKCγ:5 nM, PKCδ:20 nM, PKCη:4 nM, PKCα:2 nM |
In vitro |
METHODS: Human cervical cancer cells HeLa were treated with Staurosporine (1-10 nM) for 72 h, and cell viability was measured by MTT. RESULTS: Staurosporine inhibited the proliferation of Hela cells in a dose-dependent manner, with an IC50 of about 10 nM. [1] METHODS: Human pancreatic cancer cells PaTu 8988t and Panc-1 were treated with Staurosporine (1 μM) for 3-24 h, and cell death was detected by Flow Cytometry. RESULTS: For PaTu 8988t cells, incubation with Staurosporine for 3-24 h significantly increased apoptosis and significantly decreased the number of viable cells; necrosis increased after 6-16 h. For Panc-1 cells, Staurosporine treatment significantly increased apoptosis and significantly decreased the number of viable cells after 9-24 h. The RESULTS were summarized as follows. [2] METHODS: Human hepatocellular carcinoma cells HepG2 were treated with Staurosporine (20 nmol/L) for 6-24 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Staurosporine significantly inhibited the phosphorylation of mTOR and increased the expression of LC3-II, an autophagy marker protein, suggesting that Staurosporine activates autophagy effectively by inhibiting mTOR. [3] |
In vivo |
METHODS: To assay anti-tumor activity in vivo, Staurosporine (3 mg/kg) and Lapatinib (50 mg/kg) were administered by gavage twice a week for two weeks to Nu/J-Foxn1 Nu/Nu mice harboring human mammary carcinoma tumors JIMT-1. RESULTS: The combination of Staurosporine and Lapatinib inhibited tumor growth in a statistically significant manner. [4] METHODS: To examine the effects on islet β-cell function, Staurosporine (0.4 mg/kg in 0.5% sodium carboxymethyl cellulose) was administered intraperitoneally to iPLA2β-/- C57BL6 mice once daily for two weeks. for two weeks. RESULTS: Staurosporine impairs glucose tolerance and glucose-stimulated insulin secretion in pancreatic islets. [5] |
Kinase Assay | Enzyme assay and binding assay: Protein kinase C is assayed in a reaction mixture (0.25 mL) containing 5 μmol of Tris/HCl, pH 7.5, 2.5 μmol of magnesium acetate, 50 μg of histone II S, 20 μg of phosphatidylserine, 0.88 μg of diolein, 125 nmol of CaCl2, 1.25 nmol of [γ-32]ATP (5-10 × 104 cpm/nmol) and 5 μg of partially purified enzyme. The binding of [3H]PDBu to protein kinase C is determined: Reaction mixture (200 μL contained 4 μmo1 of Tris/malate, pH 6.8, 20 μmol of KCl, 30 nmol of CaC12, 20 μg of phosphatidylserine, 5 μg of partially purified protein kinase C, 0.5% (final concentration) of DMSO,10 pmol of [3H]PDBu (l-3 × 104 cpm/pmol) and 10 μL of various amounts of Staurosporine. |
Cell Research | Cells are exposed to Staurosporine for ~32 hours. Cells are fixed in 4% paraformaldehyde and stained with the DNA-binding dye Hoechst 33342. Cells are visualized under epifluorescence illumination, and the percentage of apoptotic cells (cells with condensed and fragmented DNA) is determined. (Only for Reference) |
Synonyms | Antibiotic AM-2282, AM-2282, CGP 41251 |
Molecular Weight | 466.53 |
Formula | C28H26N4O3 |
CAS No. | 62996-74-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 0.1 mg/mL (insoluble)
DMSO: 31 mg/mL (66.45 mM)
You can also refer to dose conversion for different animals. More
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Staurosporine 62996-74-1 Angiogenesis Apoptosis Chromatin/Epigenetic Cytoskeletal Signaling Microbiology/Virology Tyrosine Kinase/Adaptors Antibacterial Antibiotic Antifungal PKA Src PKC Antibiotic AM-2282 AM-2282 Protein kinase A Antibiotic AM2282 Antibiotic AM 2282 Bacterial Protein kinase C AM 2282 inhibit Inhibitor Fungal STS CGP 41251 CGP-41251 AM2282 CGP41251 inhibitor