Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SB-743921 hydrochloride (SB743921 HCl) 是一种有效的驱动蛋白纺锤体蛋白 KSP 抑制剂,Ki 值为 0.1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 433 | 现货 | ||
2 mg | ¥ 623 | 现货 | ||
5 mg | ¥ 947 | 现货 | ||
10 mg | ¥ 1,680 | 现货 | ||
25 mg | ¥ 3,130 | 现货 | ||
50 mg | ¥ 4,590 | 现货 | ||
100 mg | ¥ 6,530 | 现货 | ||
500 mg | ¥ 13,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,190 | 现货 |
产品描述 | SB-743921 hydrochloride (SB743921 HCl) is an effective inhibitor of kinesin spindle protein, KSP, (Ki =0.1 nM). |
靶点活性 | KSP:0.1 nM(Ki) |
体外活性 | 对于多种异种移植人的肿瘤,如Colo205,MCF-7, SK-MES, H69, OVCAR-3HT-29, MX-1, MDA-MB-231, A2780,SB-743921均能产生明显的抑制效应,抑制细胞生长的活性. |
体内活性 | SB 743921阻断了有丝分裂纺锤体的产生,因此能将细胞在有丝分裂期积累并产生细胞坏死,对于人的KSP(Ki=0.1 nM)和鼠的KSP(Ki=0.12 nM)。 |
激酶实验 | Biochemistry assay: The motor domains of KSP (amino acids 1–360) is expressed as in Escherichia coli BL21(DE3) as COOH-terminal 6-his fusion proteins. Bacterial pellets are lysed in a microfluidizer with a lysis buffer [50 mM Tris-HCl; 50 mM KCl, 10 mM imidazole, 2 mM MgCl2, 8 mM β-mercaptoethanol, 0.1 mM ATP (pH 7.4)], and proteins are purified using Ni-NTA agarose affinity chromatography, with an elution buffer consisting of 50 mM PIPES, 10% sucrose, 300 mM imidazole, 50 mM KCl, 2 mM MgCl2, mM β-mercaptoethanol, and 0.1 mM ATP (pH 6.8). Steady-state measurements of ATPase activity are performed with a pyruvate kinase–lactate dehydrogenase detection system that coupled the appearance of ADP with oxidation of NADH. Absorbance changes are monitored at 340 nm. All biochemical experiments are performed in PEM25 buffer [25 mM Pipes/KOH (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM SB 743921 for experiments involving microtubules. Rates of ADP release are measured in a stopped-flow apparatus; the decrease in fluorescence of MANT-ATP is monitored. Rates of Pi release are measured in a stopped-flow apparatus, using bacterial phosphate binding protein modified with 7-diethylamino-3-((((2 maleimidyl)ethyl)amino)carbonyl)coumarin (MDCC) dye. Ki estimates of KSP inhibitors are extracted from the dose–response curves, with explicit correction for enzyme concentration. Tubulin polymerization by measuring changes in absorbance at 340 nm is monitored. The assay is performed in 100-μL volumes in 96-well half-area microtiter plates, using a microplate reader with the incubation temperature set at 37 °C. |
细胞实验 | All cells including HeLa cells are cultured in 10% FCS in RPMI 1640 in 5% CO2. We assessed 48-hour growth inhibition by serial dilution of SB 743921 relative to DMSO-treated cells in 96-well microtiter plates, using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium. Cell growth is represented as the ratio of absorbance of treated cells to DMSO control, plotted by concentration and fitted to a four-parameter curve. Concentrations at which cellular growth is inhibited by 50% are extrapolated from the curve fit. The DNA content of HeLa cells cultured in the presence or absence of 1 μM SB 743921 for 24 hours is assessed by propidium iodide staining and flow cytometry. Immunofluorescence images are collected of HeLa cells treated for 24 hours with 1 μM SB 743921, fixed with 2% formaldehyde, permeabilized, and stained with DM1-α, anti-γ-tubulin, and 1 μg/mL 4′,6-diamidino-2-phenylindole, and with Alexa 488 secondary goat antirabbit IgG and Rhodamine-X goat antimouse IgG. Images are collected with a DeltaVision Restoration Microscopy System at a magnification of ×600. Z stacks (0.2 μm) are collected, and out of focus information is removed by constrained iterative deconvolution. Z stacks are then compressed into to a single image plane. (Only for Reference) |
别名 | SB743921 HCl, SB743921 |
分子量 | 553.52 |
分子式 | C31H34Cl2N2O3 |
CAS No. | 940929-33-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55.4 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8066 mL | 9.0331 mL | 18.0662 mL | 45.1655 mL |
5 mM | 0.3613 mL | 1.8066 mL | 3.6132 mL | 9.0331 mL | |
10 mM | 0.1807 mL | 0.9033 mL | 1.8066 mL | 4.5165 mL | |
20 mM | 0.0903 mL | 0.4517 mL | 0.9033 mL | 2.2583 mL | |
50 mM | 0.0361 mL | 0.1807 mL | 0.3613 mL | 0.9033 mL | |
100 mM | 0.0181 mL | 0.0903 mL | 0.1807 mL | 0.4517 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。
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