Staurosporine
作者：齐岳
发布时间：2023-09-05
08:51:42
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产品名称：Staurosporine
产品描述：
| 植物来源 | 天然产物 > 其他（植物来源） > 其他 |
| 产品描述 | Staurosporine is a potent PKC inhibitor for PKCα/γ/η (IC50: 2/5/4 nM), less potent to PKCε (73 nM), PKCδ (20 nM) and little action to PKCζ (1086 nM). | ||||||||||||||||
| 靶点活性 | PKCα:2 nM, PKCη:4 nM, PKCε:73 nM, PKCζ:1086 nM, PKCγ:5 nM, PKCδ:20 nM | ||||||||||||||||
| 体外活性 | 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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| 体内活性 | 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]
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| 激酶实验 | 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. | ||||||||||||||||
| 细胞实验 | 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) |
| 别名 | CGP 41251, 星形孢菌素, AM-2282, Antibiotic AM-2282, 星孢菌素 |
| 分子量 | 466.53 |
| 分子式 | C28H26N4O3 |
| CAS No. | 62996-74-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: < 0.1 mg/mL (insoluble)
DMSO: 31 mg/mL (66.45 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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