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Staurosporine (AM-2282) 是一种蛋白激酶抑制剂,对 PKC、PKA、c-Fgr、Phosphorylase kinase 和 TAOK2 均有抑制活性 (IC50=6/15/2/3/3000 nM),具有 ATP 竞争性和非选择性。Staurosporine 也可以诱导凋亡。
Staurosporine (AM-2282) 是一种蛋白激酶抑制剂,对 PKC、PKA、c-Fgr、Phosphorylase kinase 和 TAOK2 均有抑制活性 (IC50=6/15/2/3/3000 nM),具有 ATP 竞争性和非选择性。Staurosporine 也可以诱导凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 452 | 现货 | |
2 mg | ¥ 659 | 现货 | |
5 mg | ¥ 1,190 | 现货 | |
10 mg | ¥ 1,880 | 现货 | |
25 mg | ¥ 3,660 | 现货 | |
50 mg | ¥ 4,990 | 现货 | |
100 mg | ¥ 7,160 | 现货 | |
500 mg | ¥ 14,300 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,380 | 现货 |
产品描述 | 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. |
靶点活性 | PKCα:2 nM, PKCη:4 nM, PKCδ:20 nM, PKCγ:5 nM, PKCζ:1086 nM, PKCε:73 nM |
体外活性 | 方法:人宫颈癌细胞 HeLa 用 Staurosporine (1-10 nM) 处理 72 h,使用 MTT 方法检测细胞活力。 结果:Staurosporine 对 Hela 细胞增殖具有剂量依赖性抑制作用,IC50 约为 10 nM。[1] 方法:人胰腺癌细胞 PaTu 8988t、Panc-1 用 Staurosporine (1 μM) 处理 3-24 h,使用 Flow Cytometry 方法检测细胞死亡情况。 结果:PaTu 8988t 细胞,Staurosporine 孵育 3-24 h 显著增加了细胞凋亡率,并显著减少了生命细胞的数量;培养 6-16 h 后,坏死率增加。Panc-1 细胞,Staurosporine 处理在 9-24 h 后显著增加细胞凋亡并显著减少生命细胞的数量。[2] 方法:人肝癌细胞 HepG2 用 Staurosporine (20 nmol/L) 处理 6-24 h,使用 Western Blot 方法检测靶点蛋白表达水平。 结果:Staurosporine 显著抑制 mTOR 磷酸化并增加自噬标记蛋白 LC3-II 的表达,表明 Staurosporine 通过抑制 mTOR 有效激活自噬。[3] |
体内活性 | 方法:为检测体内抗肿瘤活性,将 Staurosporine (3 mg/kg) 和 Lapatinib (50 mg/kg) 灌胃给药给携带人乳腺癌肿瘤 JIMT-1 的 Nu/J-Foxn1 Nu/Nu 小鼠,每周两次,持续两周。 结果:Staurosporine 和 Lapatinib 的组合以统计学显著的方式抑制了肿瘤生长。[4] 方法:为检测对胰岛 β 细胞功能的影响,将 Staurosporine (0.4 mg/kg in 0.5% sodium carboxymethyl cellulose) 腹腔注射给 iPLA2β-/-的 C57BL6 小鼠,每天一次,持续两周。 结果:Staurosporine 会损害动物的糖耐量和胰岛的葡萄糖刺激的胰岛素分泌。[5] |
激酶实验 | 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. |
细胞实验 | 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) |
别名 | Antibiotic AM-2282, AM-2282, 星形孢菌素, CGP 41251, 星孢菌素 |
分子量 | 466.53 |
分子式 | C28H26N4O3 |
CAS No. | 62996-74-1 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | 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. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
10% DMSO+40% PEG300+5% Tween 80+45% Saline/DMSO
DMSO
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