Staurosporine

Catalog No.S1421

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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Staurosporine Chemical Structure

Staurosporine Chemical Structure
Molecular Weight: 466.53

Validation & Quality Control

Customer Product Validation(3)

Quality Control & MSDS

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Staurosporine is available in the following compound libraries:

Product Information

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  • Research Area
  • Staurosporine Mechanism
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    Combination Therapy

Product Description

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.
Targets PKCα [1]
(Cell-free assay)
c-Fgr [2] phosphorylase kinase [2] PKCη [1]
(Cell-free assay)

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IC50 2 nM 2 nM 3 nM 4 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]
Features

Protocol(Only for 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
Formulation Dissolved in DMSO, and diluted in saline
Dosages ~10 ng
Administration Stereotaxically administered into the bilateral CAl subfield of the hippocampus

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

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.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT00301938 Completed Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0  ...more 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
NCT00082017 Completed Lymphoma, Large-Cell, Ki-1|Lymphoma, T-Cell National Cancer Institute (NCI)|National Institutes of He  ...more National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 2004 Phase 2
NCT00072189 Terminated Recurrent Melanoma|Stage IV Melanoma National Cancer Institute (NCI) November 2003 Phase 2
NCT00036777 Completed Unspecified Adult Solid Tumor, Protocol Specific National Cancer Institute (NCI) March 2002 Phase 1

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Chemical Information

Download Staurosporine SDF
Molecular Weight (MW) 466.53
Formula

C28H26N4O3

CAS No. 62996-74-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms CGP 41251
Solubility (25°C) * In vitro DMSO 4 mg/mL (8.57 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo
* <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.
Chemical Name 9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-11-(methylamino)-, [9S-(9α,10β,11β,13α)]-

Customer Product Validation (3)


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Rating
Source PLoS One 2012 7(6), e39679. Staurosporine purchased from Selleck
Method Western blot
Cell Lines HeLa cells
Concentrations 100 nM
Incubation Time 2 h
Results It examined the effect on HSF1-S326 phosphorylation of drugs that have been shown to inhibit mTOR activity, including rapamycin, KUOO6379 and staurosporine. Heat shock led to phosphorylation of HSF1 on S326. Staurosporine inhibited the stress-induced activation of HSF1-S326 phosphorylation while abolishing the phosphorylation on T389 of ribosomal S6 kinase, a well-characterized substrate for mTOR. Inhibition of HSF1 phosphorylation on S326 by rapamycin suggests that this site in HSF1 is a target for the TORC1 complex.

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Rating
Source J Biomol Screen 2013 18(4), 388-99. Staurosporine purchased from Selleck
Method Binding and activity assays
Cell Lines baculovirus-infected insect cells
Concentrations 0.001-10000 uM
Incubation Time
Results Staurosporine binds preferentially to npMEK1 in the presence of ATP.

Click to enlarge
Rating
Source J Biomol Screen 2013 18(4), 388-99. Staurosporine purchased from Selleck
Method enzyme activity analysis
Cell Lines
Concentrations
Incubation Time 75 min
Results Staurosporine, sunitinib, dasatinib and VX-680 were able to completely inhibit the enzyme activity.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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