Staurosporine

SKU: orb1300561

Description

Staurosporine

Research Area

Cell Biology, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 62996-74-1
• MW: 466.5
• Purity: >98%
• Formula: C₂₈H₂₆N₄O₃
• SMILES: C[C@]12N3C=4C5=C(C6=C(C4C=7C3=CC=CC7)CNC6=O)C=8C(N5[C@](O1)(C[C@@H](NC)[C@H]2OC)[H])=CC=CC8
• Target: Kinase
• Solubility: Soluble in DMSO (up to 50 mg/ml)

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
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• 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.
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• 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.
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• 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)
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Storage & Handling

• Storage: -20°C
• 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