Staurosporine
目录号：S1421 别名： CGP 41251
Molecular Weight(MW): 466.53
Staurosporine是一种有效的PKC抑制剂，在无细胞试验中作用于PKCα，PKCγ 和PKCη，IC50分别为2 nM，5 nM 和 4 nM，对PKCδ(20 nM)和PKCε(73 nM作用较弱，对PKCζ (1086 nM)的活性很低。同时 对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。Phase 3。
客户使用该产品的4个实验数据：
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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.
产品安全说明书
PKC抑制剂选择性比较
生物活性
| 产品描述 | Staurosporine是一种有效的PKC抑制剂，在无细胞试验中作用于PKCα，PKCγ 和PKCη，IC50分别为2 nM，5 nM 和 4 nM，对PKCδ(20 nM)和PKCε(73 nM作用较弱，对PKCζ (1086 nM)的活性很低。同时 对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。Phase 3。 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 靶点 |
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| 体外研究 |
Staurosporine 也强抑制HeLa S3细胞，IC50为4 nM。[1]Staurosporine 也抑制多种其他蛋白激酶，包括PKA, PKG, 磷酸激酶, S6 激酶, 肌球蛋白轻链激酶(MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, 和Syk ， IC50分别为 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, 和 16 nM。[3] Staurosporine (1 μM) 诱导 PC12细胞90%以上凋亡,这种作用可被过量表达的Bcl-2抑制,或者zVAD-fmk, cycloheximide (10 μM) 及actinomycin D (5 μM)处理也可抑制。相应地, Staurosporine处理，诱导细胞内游离钙水平 [Ca2+]i快速且持久的提升，线粒体活性氧（ROS）的积累,及 随后的线粒体功能障碍。[4]通过caspase-8激活和Bid 分裂，功能性caspase-3的表达可增强Staurosporine诱导MCF7细胞死亡。[5] 1 μM Staurosporine处理，只部分抑制IL-3刺激的Bcl2 磷酸化，而完全阻断PKC调节的 Bcl2磷酸化。[6] Staurosporine 诱导人类包皮成纤维细胞AG-1518凋亡,根据溶酶体组织蛋白酶D调节的 细胞色素 c释放和 caspase 激活。[7] 除了激活传统线粒体凋亡通路, Staurosporine触发一种新型内在凋亡通路, 依赖Apaf-1存在时对caspase-9的激活。[8] |
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| Cell Data |
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| 体内研究 | 在局部贫血前，使用Staurosporine(0.1-10 ng)预处理局部贫血沙鼠和大鼠模型，可防止神经元损伤，这种作用存在剂量依赖性，说明CAl锥体细胞死亡涉及PKC。[2] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 激酶实验： |
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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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| 细胞实验：[4] |
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| 动物实验：[2] |
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参考文献
- [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.
溶解度 (25°C)
| 体外 | DMSO | 4 mg/mL (8.57 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 466.53 |
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| 化学式 | C28H26N4O3 |
| CAS号 | 62996-74-1 |
| 稳定性 | powder |
| in solvent | |
| 别名 | CGP 41251 |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| 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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