Staurosporine (STS)

Catalog No.S1421 Batch:S142106

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Technical Data

Formula

C28H26N4O3
Molecular Weight 466.53 CAS No. 62996-74-1
Solubility (25°C)* In vitro DMSO 46 mg/mL (98.6 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
Targets
PKCα [1]
(Cell-free assay)		 c-Fgr [2]
(Cell-free assay)		 phosphorylase kinase [2]
(Cell-free assay)		 PKCη [1]
(Cell-free assay)		 PKCγ [1]
(Cell-free assay)		 View More
2 nM 2 nM 3 nM 4 nM 5 nM
In vitro Staurosporine, a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. Staurosporine displays strong inhibitory effect against HeLa S3 cells with IC50 of 4 nM. [1] Staurosporine also inhibits a variety of other protein kinases, including PKA, PKG, phosphorylase kinase, S6 kinase, Myosin light chain kinase (MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, and Syk with IC50 of 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, and 16 nM, respectively. [2] Staurosporine (1 μM) induces >90% apoptosis in PC12 cells. Consistently, Staurosporine treatment induces a rapid and prolonged elevation of intracellular free calcium levels [Ca2+]i, accumulation of mitochondrial reactive oxygen species (ROS), and subsequent mitochondrial dysfunction. [3] The apoptosis of MCF7 cells induced by Staurosporine can be enhanced by the expression of functional caspase-3 via caspase-8 activation and Bid cleavage. [4] Staurosporine treatment at 1 μM only partially inhibits IL-3-stimulated Bcl2 phosphorylation but completely blocks PKC-mediated Bcl2 phosphorylation. [5] Staurosporine induces apoptosis of human foreskin fibroblasts AG-1518, depending on the lysosomal cathepsins D mediated cytochrome c release and caspase activation. [6] In addition to activating the classical mitochondrial apoptosis pathway, Staurosporine triggers a novel intrinsic apoptosis pathway, relying on the activation of caspase-9 in the absence of Apaf-1. [7]
In vivo In the gerbil and rat ischemia models, Staurosporine pretreatment (0.1-10 ng) before ischemia prevents neuronal damage in a dose-dependent manner, suggesting the involvement of PKC in CAl pyramidal cell death after ischemia. [8]

Protocol (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[3]
  • Cell lines

    PC12

  • Concentrations

    Dissolved in DMSO, final concentration 1 μM

  • Incubation Time

    ~32 hours

  • Method

    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.
Animal Study:

[8]
  • Animal Models

    Male Mongolian gerbils or male Wistar rats subjected to transient ischemia

  • Dosages

    ~10 ng

  • Administration

    Stereotaxically administered into the bilateral CAl subfield of the hippocampus

Customer Product Validation

Data from [J Biomol Screen, 2013, 18(4), 388-99]

Data from [J Biomol Screen, 2013, 18(4), 388-99]

Data from [Data independently produced by PLoS One, 2012, 7(6), e39679]

Data from [Data independently produced by , , Mol Carcinog, 2018, 57(7):886-895]

Selleck's Staurosporine (STS) has been cited by 168 publications

Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists [ Nat Commun, 2024, 15(1):489] PubMed: 38216578
Fatal COVID-19 pulmonary disease involves ferroptosis [ Nat Commun, 2024, 15(1):3816] PubMed: 38769293
Fatal COVID-19 pulmonary disease involves ferroptosis [ Nat Commun, 2024, 15(1):3816] PubMed: 38769293
Kisspeptin-10 binding to Gpr54 in osteoclasts prevents bone loss by activating Dusp18-mediated dephosphorylation of Src [ Nat Commun, 2024, 15(1):1300] PubMed: 38346942
Oncogenic KEAP1 mutations activate TRAF2-NFκB signaling to prevent apoptosis in lung cancer cells [ Redox Biol, 2024, 69:103031] PubMed: 38184997
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics [ Mol Syst Biol, 2024, 20(1):28-55] PubMed: 38177929
Lytic bacteriophages induce the secretion of antiviral and proinflammatory cytokines from human respiratory epithelial cells [ PLoS Biol, 2024, 22(4):e3002566] PubMed: 38652717
Synergy of retinoic acid and BH3 mimetics in MYC(N)-driven embryonal nervous system tumours [ Br J Cancer, 2024, 10.1038/s41416-024-02740-5] PubMed: 38942989
SUMOylation controls Hu antigen R posttranscriptional activity in liver cancer [ Cell Rep, 2024, 43(3):113924] PubMed: 38507413
Identification and characterization of a potent and selective HUNK inhibitor for treatment of HER2+ breast cancer [ Cell Chem Biol, 2024, S2451-9456(24)00037-0] PubMed: 38307028

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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