| 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(xì)胞實(shí)驗(yàn) | 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(shí)驗(yàn) | 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(xì)胞 HeLa 用 Staurosporine (1-10 nM) 處理 72 h，使用 MTT 方法檢測(cè)細(xì)胞活力。
結(jié)果：Staurosporine 對(duì) Hela 細(xì)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(xì)胞 PaTu 8988t、Panc-1 用 Staurosporine (1 μM) 處理 3-24 h，使用 Flow Cytometry 方法檢測(cè)細(xì)胞死亡情況。
結(jié)果：PaTu 8988t 細(xì)胞，Staurosporine 孵育 3-24 h 顯著增加了細(xì)胞凋亡率，并顯著減少了生命細(xì)胞的數(shù)量；培養(yǎng) 6-16 h 后，壞死率增加。Panc-1 細(xì)胞，Staurosporine 處理在 9-24 h 后顯著增加細(xì)胞凋亡并顯著減少生命細(xì)胞的數(shù)量。[2]
方法：人肝癌細(xì)胞 HepG2 用 Staurosporine (20? nmol/L) 處理 6-24 h，使用 Western Blot 方法檢測(cè)靶點(diǎn)蛋白表達(dá)水平。
結(jié)果：Staurosporine 顯著抑制 mTOR 磷酸化并增加自噬標(biāo)記蛋白 LC3-II 的表達(dá)，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(cè)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(jì)學(xué)顯著的方式抑制了腫瘤生長。[4]
方法：為檢測(cè)對(duì)胰島 β 細(xì)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(huì)損害動(dòng)物的糖耐量和胰島的葡萄糖刺激的胰島素分泌。[5] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : < 0.1 mg/mL (insoluble)
DMSO : 31.56 mg/mL (67.65 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.1 mg/mL (6.64 mM), Solution.
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| 關(guān)鍵字 | STS | Staurosporine | Protein kinase C | Protein kinase A | PKCη | PKCγ | PKCα | PKC | PKA | Inhibitor | inhibit | Fungal | CGP-41251 | CGP41251 | c-Fgr | Bacterial | Apoptosis | Antibiotic AM2282 | Antibiotic AM 2282 | Antibiotic | AM2282 | AM 2282 |
| 相關(guān)產(chǎn)品 | Formamide | Aceglutamide | Calcium Propionate | Benzyl propionate | Neomycin sulfate | Terbinafine hydrochloride | Dimethyl sulfoxide | Sodium bicarbonate | Hyaluronic acid sodium (MW 20 kDa) | Sodium diacetate | Sulfamethoxazole sodium | D(+)-Raffinose pentahydrate |
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