Staurosporine
製品コードS1421 別名：CGP 41251
分子量(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.
カスタマーフィードバック(3)
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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.
J Biomol Screen 2013 18(4), 388-99. Staurosporine purchased from Selleck.
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J Biomol Screen 2013 18(4), 388-99. Staurosporine purchased from Selleck.
製品安全説明書
PKC阻害剤の選択性比較
生物活性
| 製品説明 | 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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| 体外試験 |
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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| 体内試験 | 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] |
お薦めの試験操作（参考用のみ）
| キナーゼ試験： |
+ 展開
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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| 細胞試験： |
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参考
- [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 |
* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。
化学情報
| 分子量 | 466.53 |
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| 化学式 | C28H26N4O3 |
| CAS No. | 62996-74-1 |
| 保管 | 粉 |
| in solvent | |
| 別名 | CGP 41251 |
便利ツール
モル濃度計算器
求めたい質量、体積または濃度を計算してください。
質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)
モル濃度計算器方程式
*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA（製品ページで利用可能な）。
希釈計算器
貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：
開始濃度 x 開始体積 = 最終濃度 x 最終体積
希釈の計算式
この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力 出力 )
常に貯蔵液を準備するとき、小びんラベルとMSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。
分子量计算器
そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：
チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2
モル濃度計算器
臨床試験
| 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 |
技術サポート
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