Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bisindolylmaleimide I (GF109203X) 是一种有效且高度选择性的蛋白激酶 C(PKC) 抑制剂,Ki 值为 14 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 221 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 990 | 现货 | ||
25 mg | ¥ 1,960 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,450 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 638 | 现货 |
产品描述 | Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor with a Ki of 14 nM. |
靶点活性 | PKC:14 nM |
体外活性 | GF109203X, as an ATP-competitive PKC inhibitor, prevents platelet aggregation induced by stimuli that activate PKC, and has the potential as a tool for studying the involvement of PKC in signal transduction pathways. [1] GF 109203X produces reversal activity on P-glycoprotein and MRP -mediated multidrug resistance. [2] [3] PKC inhibition by GF109203X significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells. [4] |
体内活性 | GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats. [5] |
激酶实验 | Assay of protein kinase C: Protein kinase C is arrayed by measuring 32PI transferred from [gamma-32PI] ATP to lysine-rich histone type Ill-s. The reaction mixture (80 μL) contained 50 mM Tris-HCI. pH 7.4, 100 μM CaCl2, 10 mM MgCI2, 37.5 μL/mL histone type Ill-s, 10 μM [gamma-32PI] ATP (1250 cpm/pmol), 31 μM bovine brain phosphatidylserine and 0.5 μM 1,2 sn-dioleylglycerol. Fifteen μL of purified PKC (final concentration in assay 0.38 μg/mL) is added to the incubation mixture. After 10 min at 30°C, the reaction is stopped by addition of 30 μL of casein 30 mg/mL and 0.9 ml of 12% trichloroacetic acid. The acid precipitable material is collected by centrifugation, dissolved in 1N NaOH (100μL) and precipitated again with 1 ml of 12% trichloroacetic acid. The pellet is dissolved in 1N NaOH (100μL) and 32P incorporation is measured by scintillation counting in Aquasol. |
细胞实验 | Cell proliferation is monitored by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Cells are seeded in 96-well plates and allowed to grow overnight. The cells are serum-starved for 18–24 hours and then treated with 1 mM carbachol for 48 hours in 100 μL serum-free RPMI 1640. Inhibitors are added 30 min prior to carbachol treatment. Following the treatment, 10 μL of MTT solution (5 mg/ml) is applied to each well, and the plates were incubated for 3 h at 37 °C. After the medium is removed, the formazan crystals formed are solubilized in 100 μL DMSO. The absorbance at 570 nm is measured using a microplate reader and the background absorbance at 690 nm is subtracted. Each assay is performed in triplicate. (Only for Reference) |
别名 | GF109203X, Go 6850, 3-[1-[3-(二甲氨基)丙基]1H-吲哚-3-基]-4-(吲哚-3-基)1H-吡咯-2,5二酮 |
分子量 | 412.48 |
分子式 | C25H24N4O2 |
CAS No. | 133052-90-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10.3 mg/mL (25 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4244 mL | 12.1218 mL | 24.2436 mL | 60.609 mL |
5 mM | 0.4849 mL | 2.4244 mL | 4.8487 mL | 12.1218 mL | |
10 mM | 0.2424 mL | 1.2122 mL | 2.4244 mL | 6.0609 mL | |
20 mM | 0.1212 mL | 0.6061 mL | 1.2122 mL | 3.0304 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Bisindolylmaleimide I 133052-90-1 Angiogenesis Chromatin/Epigenetic Cytoskeletal Signaling Tyrosine Kinase/Adaptors PDGFR PKC Go6850 Protein kinase C Go-6850 GF109203X inhibit Go 6850 3-[1-[3-(二甲氨基)丙基]1H-吲哚-3-基]-4-(吲哚-3-基)1H-吡咯-2,5二酮 Inhibitor inhibitor