Staurosporine

SKU: orb1300561

Description

Staurosporine

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Infectious Disease & Virology, Signal Transduction

Key Properties

• CAS Number: 62996-74-1
• MW: 466.53
• Purity: 99.87%
• Formula: C₂₈H₂₆N₄O₃
• SMILES: CN[C@H]1C[C@@H]2O[C@@](C)([C@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13
• Target: Src,PKA,PKC,Antifungal,Apoptosis,Antibiotic,Antibacterial
• Solubility: DMSO:31.56 mg/mL (67.65 mM);H2O:< 0.1 mg/mL (insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.1 mg/mL (6.64 mM)

Bioactivity

• Target IC50:
  PKA:15 nM|PhK:3 nM|CSK:2000 nM|PhK (Phosphorylase kinase):3 nM|PKCε:73 nM|MLCK:21 nM|IGF-1R:6150 nM|ERK1:1500 nM|PKCα:2 nM|PKCγ:5 nM|S6K:5 nM|CK2:19500 nM|CK1:163500 nM|EGFR:100 nM|PKCη:4 nM|TPK-IIB/Syk:16 nM|IR:61 nM|Ca 2+ /CaM PK-I1:20 nM|v-Src:6 nM|cdc2:9 nM|PKCδ:20 nM|PKCζ:1086 nM
• 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. 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.
• 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. 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. 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PKCα, PKCγ, PKCη, PKC, PKA, Protein kinase A, Protein kinase C, STS, Staurosporine, Bacterial, Apoptosis, Antibiotic AM 2282, Antibiotic AM2282, Antibiotic AM-2282, Antibiotic, AM 2282, AM2282, AM-2282, c-Fgr, CGP 41251, CGP41251, CGP-41251, Inhibitor, Fungal, inhibit

Compound Identifiers

PubChem CID

42610657