Staurosporine
Catalog No.S1421 Synonyms: CGP 41251
Molecular Weight(MW): 466.53
Staurosporine 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.
4 Customer Reviews
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Caspase-8, 9, 3, 6, PARP, and cleaved PARP were detected in POTEG overexpressed cells and control cells with or without STS treatment.
Mol Carcinog, 2018, 57(7):886-895. Staurosporine purchased from Selleck.
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.
PLoS One 2012 7(6), e39679. Staurosporine purchased from Selleck.
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J Biomol Screen 2013 18(4), 388-99. Staurosporine purchased from Selleck.
J Biomol Screen 2013 18(4), 388-99. Staurosporine purchased from Selleck.
Purity & Quality Control
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Biological Activity
| Description | Staurosporine 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. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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
| Kinase Assay: |
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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. |
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References
- [1] Tamaoki T, et al. Biochem Biophys Res Commun, 1986, 135(2), 397-402.
- [2] Meggio F, et al. Eur J Biochem, 1995, 234(1), 317-322.
- [3] Kruman I, et al. J Neurosci Res, 1998, 51(3), 293-308.
- [4] Tang D, et al. J Biol Chem, 2000, 275(13), 9303-9307.
- [5] Deng X, et al. Proc Natl Acad Sci U S A, 2000, 97(4), 1578-1583.
- [6] Johansson AC, et al. Cell Death Differ, 2003, 10(11), 1253-1259.
- [7] Manns J, et al. FASEB J, 2011, 25(9), 3250-3261.
- [8] Hara H, et al. J Cereb Blood Flow Metab, 1990, 10(5), 646-653.
Solubility (25°C)
| In vitro | DMSO | 4 mg/mL (8.57 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | 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.
Chemical Information
| Molecular Weight | 466.53 |
|---|---|
| Formula | C28H26N4O3 |
| CAS No. | 62996-74-1 |
| Storage | powder |
| in solvent | |
| Synonyms | CGP 41251 |
Bio Calculators
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00082017 | Terminated | Lymphoma Large-Cell Ki-1|Lymphoma T-Cell | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | April 5 2004 | Phase 2 |
| NCT00301938 | Completed | Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Acute Promyelocytic Leukemia (M3)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Myelodysplastic/Myeloproliferative Neoplasms|Previously Treated Myelodysplastic Syndromes|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|T-cell Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Myeloid Leukemia | National Cancer Institute (NCI) | December 2005 | Phase 1 |
| NCT00098956 | Completed | Extensive Stage Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer | National Cancer Institute (NCI) | January 2005 | Phase 2 |
| NCT00031681 | Completed | Advanced Adult Primary Liver Cancer|Carcinoma of the Appendix|Estrogen Receptor-negative Breast Cancer|Extensive Stage Small Cell Lung Cancer|Gastrointestinal Stromal Tumor|HER2-negative Breast Cancer|Metastatic Gastrointestinal Carcinoid Tumor|Ovarian Sarcoma|Ovarian Stromal Cancer|Progesterone Receptor-negative Breast Cancer|Recurrent Adenoid Cystic Carcinoma of the Oral Cavity|Recurrent Adult Primary Liver Cancer|Recurrent Anal Cancer|Recurrent Basal Cell Carcinoma of the Lip|Recurrent Borderline Ovarian Surface Epithelial-stromal Tumor|Recurrent Breast Cancer|Recurrent Cervical Cancer|Recurrent Colon Cancer|Recurrent Endometrial Carcinoma|Recurrent Esophageal Cancer|Recurrent Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity|Recurrent Extrahepatic Bile Duct Cancer|Recurrent Gallbladder Cancer|Recurrent Gastric Cancer|Recurrent Gastrointestinal Carcinoid Tumor|Recurrent Inverted Papilloma of the Paranasal Sinus and Nasal Cavity|Recurrent Lymphoepithelioma of the Nasopharynx|Recurrent Lymphoepithelioma of the Oropharynx|Recurrent Metastatic Squamous Neck Cancer With Occult Primary|Recurrent Midline Lethal Granuloma of the Paranasal Sinus and Nasal Cavity|Recurrent Mucoepidermoid Carcinoma of the Oral Cavity|Recurrent Non-small Cell Lung Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Ovarian Germ Cell Tumor|Recurrent Pancreatic Cancer|Recurrent Prostate Cancer|Recurrent Rectal Cancer|Recurrent Salivary Gland Cancer|Recurrent Small Cell Lung Cancer|Recurrent Small Intestine Cancer|Recurrent Squamous Cell Carcinoma of the Hypopharynx|Recurrent Squamous Cell Carcinoma of the Larynx|Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity|Recurrent Squamous Cell Carcinoma of the Nasopharynx|Recurrent Squamous Cell Carcinoma of the Oropharynx|Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Recurrent Verrucous Carcinoma of the Larynx|Recurrent Verrucous Carcinoma of the Oral Cavity|Small Intestine Adenocarcinoma|Small Intestine Leiomyosarcoma|Small Intestine Lymphoma|Stage IV Adenoid Cystic Carcinoma of the Oral Cavity|Stage IV Anal Cancer|Stage IV Basal Cell Carcinoma of the Lip|Stage IV Borderline Ovarian Surface Epithelial-stromal Tumor|Stage IV Breast Cancer|Stage IV Colon Cancer|Stage IV Endometrial Carcinoma|Stage IV Esophageal Cancer|Stage IV Esthesioneuroblastoma of the Paranasal Sinus and Nasal Cavity|Stage IV Gastric Cancer|Stage IV Inverted Papilloma of the Paranasal Sinus and Nasal Cavity|Stage IV Lymphoepithelioma of the Nasopharynx|Stage IV Lymphoepithelioma of the Oropharynx|Stage IV Midline Lethal Granuloma of the Paranasal Sinus and Nasal Cavity|Stage IV Mucoepidermoid Carcinoma of the Oral Cavity|Stage IV Non-small Cell Lung Cancer|Stage IV Ovarian Epithelial Cancer|Stage IV Ovarian Germ Cell Tumor|Stage IV Pancreatic Cancer|Stage IV Prostate Cancer|Stage IV Rectal Cancer|Stage IV Salivary Gland Cancer|Stage IV Squamous Cell Carcinoma of the Hypopharynx|Stage IV Squamous Cell Carcinoma of the Larynx|Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity|Stage IV Squamous Cell Carcinoma of the Nasopharynx|Stage IV Squamous Cell Carcinoma of the Oropharynx|Stage IV Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Stage IV Verrucous Carcinoma of the Larynx|Stage IV Verrucous Carcinoma of the Oral Cavity|Stage IVA Cervical Cancer|Stage IVB Cervical Cancer|Triple-negative Breast Cancer|Unresectable Extrahepatic Bile Duct Cancer|Unresectable Gallbladder Cancer|Unspecified Adult Solid Tumor Protocol Specific|Untreated Metastatic Squamous Neck Cancer With Occult Primary | National Cancer Institute (NCI)|Washington University Siteman Cancer Center | December 2001 | Phase 1 |
| NCT00012194 | Terminated | Unspecified Adult Solid Tumor Protocol Specific | National Cancer Institute (NCI) | March 2001 | Phase 1 |
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