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CW-069 是一种微管运动蛋白 HSET 的变构选择性抑制剂,IC50值为 75 μM,对 KSP 具有显着的特异性。
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CW-069 是一种微管运动蛋白 HSET 的变构选择性抑制剂,IC50值为 75 μM,对 KSP 具有显着的特异性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 346 | 现货 | |
5 mg | ¥ 825 | 现货 | |
10 mg | ¥ 1,260 | 现货 | |
25 mg | ¥ 2,270 | 现货 | |
50 mg | ¥ 3,170 | 现货 | |
100 mg | ¥ 4,450 | 现货 | |
500 mg | ¥ 9,290 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 889 | 现货 |
产品描述 | CW-069 (IC50=75 μM), an allosteric selective inhibitor of microtubule motor protein HSET, exhibits remarkable specificity over KSP. |
靶点活性 | HSET:75 μM |
体外活性 | CW069在具有多余中心体的N1E-115细胞中增加多极纺锤体,但不改变正常人类真皮成纤维细胞的双极纺锤体形态。同时,CW069对N1E-115癌细胞的生长具有抑制作用,IC50为10 μM。[1] |
激酶实验 | In Vitro Enzymatic ATPase Assay: The protocol is optimized for use with full-length, N-terminal, 6His-tagged HSET and KSP, and measured the MT-stimulated activity of the proteins. Inhibition of the Gsp synthetase activity of HSET/KSP is observed spectrophotometrically by coupling the hydrolysis of ATP to oxidation of NADH via pyruvate kinase/lactate dehydrogenase reactions. The assay is initiated by adding purified Gsp synthetase/amidase (12.8 nM) to an assay mixture containing the following components (final concentration): 6 nM protein, 0.07 mg/ml MTs (University Biologicals), 1.56 mM glutathione, 10 mM spermidine, 2 mM ATP, 2.7 mM MgCl2, 1 mM phospho(enol)-pyruvate, 0.2 mM NADH, 50 μg/ml lactate dehydrogenase, 100 μg/ml pyruvate kinase, and various concentrations of inhibitor all in 50 mM Na PIPES (pH 6.8) at 37°C. The ADP-Glo detection assay (Promega) is performed as described in the manufacturer's instructions. All compound additions were performed using a multidrop BioMek Nxp. Plates were read using a Pherastar microplate reader. |
细胞实验 | Cells are cultured in DMEM supplemented with 10% fetal calf serum (FCS) at 37°C and 5% CO2. All compounds used in the Sulforhodamine B colorimetric (SRB) assay are dissolved in DMSO and diluted in culture medium to a final concentration of 0.2% DMSO. For the SRB assay and live-cell imaging, cells are seeded in 96-well plates at a density of 2,500 cells per well. After 24 hr, the cells are treated with compound for 72 hr, with triplicate wells for each concentration. For the SRB assay, the cells are then fixed with trichloroacetic acid (TCA) and stained with SRB. Fluorescence is quantified using an Infinite 200 PRO plate-reader at a wavelength of 545 nm. Compound-treated wells are compared with solvent control wells and the concentration of compound that results in 50% of the solvent-control cell growth is designated as the IC50 concentration, calculated using Graphpad PRISM 6. At least three biological replicates are performed for each assay.(Only for Reference) |
别名 | CW069 |
分子量 | 500.33 |
分子式 | C23H21IN2O3 |
CAS No. | 1594094-64-0 |
Smiles | OC(=O)c1cc(I)ccc1NC(=O)[C@H](Cc1ccccc1)NCc1ccccc1 |
密度 | 1.559 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 4 mg/mL (7.99 mM) DMSO: 93 mg/mL (185.9 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||||||||||||||||||||||
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