| 名稱 | Staurosporine |
| 描述 | Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis. |
| 細胞實驗 | 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) |
| 激酶實驗 | 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. |
| 體外活性 | 方法：人宮頸癌細胞 HeLa 用 Staurosporine (1-10 nM) 處理 72 h，使用 MTT 方法檢測細胞活力。
結(jié)果：Staurosporine 對 Hela 細胞增殖具有劑量依賴性抑制作用，IC50 約為 10 nM。[1]
方法：人胰腺癌細胞 PaTu 8988t、Panc-1 用 Staurosporine (1 μM) 處理 3-24 h，使用 Flow Cytometry 方法檢測細胞死亡情況。
結(jié)果：PaTu 8988t 細胞，Staurosporine 孵育 3-24 h 顯著增加了細胞凋亡率，并顯著減少了生命細胞的數(shù)量；培養(yǎng) 6-16 h 后，壞死率增加。Panc-1 細胞，Staurosporine 處理在 9-24 h 后顯著增加細胞凋亡并顯著減少生命細胞的數(shù)量。[2]
方法：人肝癌細胞 HepG2 用 Staurosporine (20? nmol/L) 處理 6-24 h，使用 Western Blot 方法檢測靶點蛋白表達水平。
結(jié)果：Staurosporine 顯著抑制 mTOR 磷酸化并增加自噬標記蛋白 LC3-II 的表達，表明 Staurosporine 通過抑制 mTOR 有效激活自噬。[3] |
| 體內(nèi)活性 | 方法：為檢測體內(nèi)抗腫瘤活性，將 Staurosporine (3 mg/kg) 和 Lapatinib (50 mg/kg) 灌胃給藥給攜帶人乳腺癌腫瘤 JIMT-1 的 Nu/J-Foxn1 Nu/Nu 小鼠，每周兩次，持續(xù)兩周。
結(jié)果：Staurosporine 和 Lapatinib 的組合以統(tǒng)計學(xué)顯著的方式抑制了腫瘤生長。[4]
方法：為檢測對胰島 β 細胞功能的影響，將 Staurosporine (0.4 mg/kg in 0.5% sodium carboxymethyl cellulose) 腹腔注射給 iPLA2β-/-的 C57BL6 小鼠，每天一次，持續(xù)兩周。
結(jié)果：Staurosporine 會損害動物的糖耐量和胰島的葡萄糖刺激的胰島素分泌。[5] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 0.1 mg/mL (insoluble)
DMSO : 13.75 mg/mL (29.47 mM)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.1 mg/mL (6.64 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
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| 關(guān)鍵字 | Antibiotic | Apoptosis | PKC | Protein kinase A | Staurosporine | Antibiotic AM2282 | Antibiotic AM 2282 | Bacterial | Protein kinase C | AM 2282 | inhibit | Inhibitor | Fungal | STS | CGP-41251 | PKA | AM2282 | CGP41251 |
| 相關(guān)產(chǎn)品 | Dehydroacetic acid sodium | Doxycycline | Methyl anthranilate | Neomycin sulfate | Geraniol | Dimethyl sulfoxide | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Ampicillin sodium | Sulfamethoxazole sodium | Kanamycin sulfate | Sodium 4-phenylbutyrate |
| 相關(guān)庫 | 微生物天然產(chǎn)物庫 | 抑制劑庫 | 抗癌活性化合物庫 | 經(jīng)典已知活性庫 | 抗真菌庫 | 生物堿類天然產(chǎn)物庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | 酪氨酸激酶分子庫 | 抗感染天然產(chǎn)物庫 |