化合物Bisindolylmaleimide I T6513
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
50 mg | 133052-90-1 | ¥3,730.00 | 询底价 |
1 mg | 133052-90-1 | ¥221.00 | 询底价 |
5 mg | 133052-90-1 | ¥578.00 | 询底价 |
1 mL | 133052-90-1 | ¥638.00 | 询底价 |
100 mg | 133052-90-1 | ¥5,450.00 | 询底价 |
25 mg | 133052-90-1 | ¥1,960.00 | 询底价 |
10 mg | 133052-90-1 | ¥990.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Bisindolylmaleimide I
描述: 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。
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)
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.
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]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 10.3 mg/mL (25 mM)
关键字: Go6850 | PKC | Protein kinase C | Go-6850 | inhibit | Inhibitor | Bisindolylmaleimide I
相关产品: AG-1478 | Avapritinib | Masitinib mesylate | PDGFRα kinase inhibitor 1 | ENMD-2076 | PP58 | Tyrphostin AG1433 | Dovitinib lactate | TAK-593 | Tyrphostin AG1296
相关库: Membrane Protein-targeted Compound Library | Inhibitor Library | Kinase Inhibitor Library | Epigenetics Compound Library | Cytoskeletal Signaling Pathway Compound Library | Tyrosine Kinase Inhibitor Library | Highly Selective Inhibitor Library | Anti-Cancer Active Compound Library | TGF-beta/Smad Compound Library | Reprogramming Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途