Staurosporine (STS)

Catalog No.S1421 Batch:S142109

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Technical Data

Formula

C28H26N4O3
Molecular Weight 466.53 CAS No. 62996-74-1
Solubility (25°C)* In vitro DMSO 93 mg/mL (199.34 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (10.72mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

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. This compound 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 (STS), a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. It also displays strong inhibitory effect against HeLa S3 cells with IC50 of 4 nM. [1] This compound 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] At 1 μM, it induces >90% apoptosis in PC12 cells. Consistently, this 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 STS can be enhanced by the expression of functional caspase-3 via caspase-8 activation and Bid cleavage. [4] Treatment at 1 μM only partially inhibits IL-3-stimulated Bcl2 phosphorylation but completely blocks PKC-mediated Bcl2 phosphorylation. [5] It 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, STS 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, pretreatment with Staurosporine (STS) (0.1–10 ng) before ischemia prevents neuronal damage in a dose-dependent manner, suggesting the involvement of PKC in CA1 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 μmol of Tris/malate, pH 6.8, 20 μmol of KCl, 30 nmol of CaCl2, 20 μg of phosphatidylserine, 5 μg of partially purified protein kinase C, 0.5% (final concentration) of DMSO, 10 pmol of [3H]PDBu (1-3 × 104 cpm/pmol) and 10 μL of various amounts of Staurosporine (STS).
Cell Assay:

[3]
  • Cell lines

    PC12

  • Concentrations

    Dissolved in DMSO, final concentration 1 μM

  • Incubation Time

    ~32 hours

  • Method

    Cells are exposed to Staurosporine (STS) for ~32 hours, after which they are fixed in 4% paraformaldehyde and stained with the DNA-binding dye Hoechst 33342. Under epifluorescence illumination, 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

References

  • https://pubmed.ncbi.nlm.nih.gov/3457562/
  • https://pubmed.ncbi.nlm.nih.gov/8529658/
  • https://pubmed.ncbi.nlm.nih.gov/9486765/
  • https://pubmed.ncbi.nlm.nih.gov/10734071/
  • https://pubmed.ncbi.nlm.nih.gov/10677502/
  • https://pubmed.ncbi.nlm.nih.gov/14576777/
  • https://pubmed.ncbi.nlm.nih.gov/21659556/
  • https://pubmed.ncbi.nlm.nih.gov/2384538/

Customer Product Validation

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

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

Intracellular concentration of HSF1-phosphoserine 326, total HSF1, S6 kinase-phosphothreonine-389, total S6 kinase and β-actin, without or with heat shock in HeLa cells pretreated with mTOR inhibitors rapamycin (30 nM) and KU0063794 (2 uM) and kinase inhibitor staurosporine (100 nM) for 2 hr. Relative levels of HSF1-phosphoserine 326 in cells after the various treatments were determined by densitometric analysis of X-ray films, normalized to untreated cells (lane 1), and are indicated below the representation of the immunoblots.

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

Caspase-8, 9, 3, 6, PARP, and cleaved PARP were detected in POTEG overexpressed cells and control cells with or without STS treatment.

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

Selleck's Staurosporine (STS) Has Been Cited by 199 Publications

Cytosolic cytochrome c represses ferroptosis [ Cell Metab, 2025, S1550-4131(25)00149-4] PubMed: 40233758
A Leishmania virulence factor harnesses an allosteric kinase switch to regulate its ubiquitin ligase activity [ Mol Cell, 2025, 85(19):3711-3728.e11] PubMed: 40997810
Targeting SUMO2 reverses aberrant epigenetic rewiring driven by SS18::SSX fusion oncoproteins and impairs sarcomagenesis [ EMBO J, 2025, 10.1038/s44318-025-00526-w] PubMed: 40804185
Deep transfer learning approach for automated cell death classification reveals novel ferroptosis-inducing agents in subsets of B-ALL [ Cell Death Dis, 2025, 16(1):396] PubMed: 40382332
Deep transfer learning approach for automated cell death classification reveals novel ferroptosis-inducing agents in subsets of B-ALL [ Cell Death Dis, 2025, 16(1):396] PubMed: 40382332
Exploiting dysregulated iron homeostasis to eradicate persistent high-grade serous ovarian cancer [ Cell Death Discov, 2025, 11(1):423] PubMed: 40998801
EGFR-mediated crosstalk between vascular endothelial cells and hepatocytes promotes Piezo1-dependent liver regeneration [ Genes Dis, 2025, 12(3):101321] PubMed: 40083329
Real-time nanomechanical visualization and profiling for rapid discrimination of early-stage regulated cell death modalities [ Talanta, 2025, 298(Pt B):129001] PubMed: 41106246
Capturing the Heterogeneity of the PDAC Tumor Microenvironment: Novel Triple Co-Culture Spheroids for Drug Screening and Angiogenic Evaluation [ Cells, 2025, 14(6)450] PubMed: 40136699
Macrophages with different origins proliferate ex vivo and do not lose their core intrinsic features [ iScience, 2025, 28(6):112635] PubMed: 40510129

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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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