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簡要描述：Staurosporine是一種有效的PKC抑制劑，在無細(xì)胞試驗(yàn)中作用于PKCα，PKCγ 和PKCη，IC50分別為2nM，5nM 和 4nM，對(duì)PKCδ(20nM)和PKCε(73nM作用較弱，對(duì)PKCζ (1086nM)的活性很低。同時(shí) 對(duì)其他的激酶PKA，PKG，S6K，CaMKII，等也顯示抑制活性。
產(chǎn)品型號(hào)：abs810006廠商性質(zhì)：生產(chǎn)廠家更新時(shí)間：2025-11-11訪 問 量：949產(chǎn)品分類
Product Category詳細(xì)介紹
| 品牌 | absin | CAS | 62996-74-1 |
|---|---|---|---|
| 分子式 | C28H26N4O3 | 純度 | >98 % |
| 分子量 | 466.54 | 貨號(hào) | abs810006 |
| 規(guī)格 | 5mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | 對(duì)其他的激酶PKA,PKG，S6K，CaMKII，等也顯示抑制活性。 | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
| 產(chǎn)品描述 | |
| 描述 | Staurosporine是一種有效的PKC抑制劑，在無細(xì)胞試驗(yàn)中作用于PKCα，PKCγ 和PKCη，IC50分別為2nM，5nM 和 4nM，對(duì)PKCδ(20nM)和PKCε(73nM作用較弱，對(duì)PKCζ (1086nM)的活性很低。同時(shí) 對(duì)其他的激酶PKA，PKG，S6K，CaMKII，等也顯示抑制活性。 |
| 純度 | >98 % |
| 儲(chǔ)存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | 星形孢菌素，Antibiotic AM-2282; STS; AM-2282;CGP 41251 |
| 外觀 | Lyophilized powder |
| 可溶性/溶解性 | DMSO：4 mg/mL (8.57 mM) |
| 生物活性 | |
| 靶點(diǎn) | PKCα,c-Fgr,phosphorylase kinase,PKCη,PKCγ… |
| In vitro(體外研究) | 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. 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. Staurosporine (1 μM) induces >90% apoptosis in PC12 cells. Consistently, Staurosporine treatment induces a rapid and prolonged elevation of intracellular free calcium levels i, accumulation of mitochondrial reactive oxygen species (ROS), and subsequent mitochondrial dysfunction. 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. Staurosporine treatment at 1 μM only partially inhibits IL-3-stimulated Bcl2 phosphorylation but completely blocks PKC-mediated Bcl2 phosphorylation. Staurosporine induces apoptosis of human foreskin fibroblasts AG-1518, depending on the lysosomal cathepsins D mediated cytochrome c release and caspase activation. 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. |
| In vivo(體內(nèi)研究) | 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. |
| 參考文獻(xiàn) | |
| 參考文獻(xiàn) | [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. |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Cell CycleKinases/PhosphatasesCdks EpigeneticsCell cycleKinases/PhosphatasesCdks NeuroscienceNeurology processNeural Signal Transduction NeuroscienceNeurology processNeurodegenerative diseaseOther Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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