Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BML-277 (C 3742) 是一种选择性的检测点激酶 2 抑制剂,IC50为 15 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 155 | 现货 | ||
5 mg | ¥ 369 | 现货 | ||
10 mg | ¥ 589 | 现货 | ||
25 mg | ¥ 1,230 | 现货 | ||
50 mg | ¥ 2,450 | 现货 | ||
100 mg | ¥ 3,650 | 现货 | ||
500 mg | ¥ 7,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 397 | 现货 |
产品描述 | BML-277 (C 3742) is a selective checkpoint kinase 2 (Chk2) inhibitor. |
靶点活性 | Chk2:15 nM |
体外活性 | BML-277 is an ATP-competitive inhibitor of Chk2 that dose dependently protects human CD4+ and CD8+ T-cells from apoptosis due to ionizing radiation. BML-277 efficiently rescues both T-cell populations from radiation-induced apoptosis in a dose-dependent manner with an observed EC50 of 3?7.6 μM. The concentration of BML-277 required for radioprotection is consistent with the biochemical measurement of chk2 inhibition. Providing theKm of ATP for Chk2 is determined to be 99 μM and the Ki for BML-277 is 37 nM, and assuming that the intracellular ATP concentration is 10 mM, a 5 μM concentration of BML-277 would be expected to produce 42% inhibition of intracellular chk2[1]. |
激酶实验 | Activity of inhibitors of chk2 is determined by incubating inhibitory compounds with recombinant full-length chk2:? 5 nM recombinant human Chk2, 50 mM HEPES (pH 7.4), 100 mM NaCl, 10 mM MgCl2, 25 μM synthetic peptide substrate (biotin-SGLYRSPSMPENLNRPR, 1 μM ATP, 50 μCi/mL [γ-33P] ATP, and a protease inhibitor mixture. The reaction mixtures are incubated at 37°C for 3 h, and the peptide substrate is captured on streptavidin conjugated to agarose beads. The agarose beads are washed repeatedly with a 0.1% solution of Tween-20 in phosphate-buffered saline, pH 7.4. Enzyme activity at different BML-277 concentrations (6.25, 12.5, 25, 50, 100, and 200 nM) is determined by measuring the amount of radioactive phosphate bound to the substrate peptide by scintillation counting. In kinetic experiments ATP concentration is varied while the ratio between unlabeled and [γ-33P] labeled ATP is kept constant. Reactions are stopped at different time points by addition of 50 mM cold ATP and samples are kept on ice during further processing[1]. |
细胞实验 | BML-277 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. To determine the radioprotective effect of Chk2 inhibitors, purified T-cells are incubated at 100?000 cells per well in BML-277 (102.5 nM, 1 μM, 100.5 μM, 10 μM, and 101.5 μM) or vehicle (DMSO) at varying concentrations in 96-well stripwells for 1 h. Cells are then exposed to a dose of 0 or 10 Gy gamma irradiation from a 137Cs source at a dose rate of 3.65 Gy/min and then returned to the incubator for a further 24 h. Cells are stained with Annexin V-FITC and propidium iodide, according to the manufacturers protocol. Apoptotic and surviving cells are quantitated with a FACSCalibur FACS machine. Data are reported as percent recovery-or the number of survivors from treatment groups minus the number of cells surviving in the irradiated control group divided by the number of surviving cells in the untreated control groups[1]. |
别名 | C 3742, Chk2 Inhibitor II, BML 277 |
分子量 | 363.8 |
分子式 | C20H14ClN3O2 |
CAS No. | 516480-79-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (137.44 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7488 mL | 13.7438 mL | 27.4876 mL | 68.7191 mL |
5 mM | 0.5498 mL | 2.7488 mL | 5.4975 mL | 13.7438 mL | |
10 mM | 0.2749 mL | 1.3744 mL | 2.7488 mL | 6.8719 mL | |
20 mM | 0.1374 mL | 0.6872 mL | 1.3744 mL | 3.436 mL | |
50 mM | 0.055 mL | 0.2749 mL | 0.5498 mL | 1.3744 mL | |
100 mM | 0.0275 mL | 0.1374 mL | 0.2749 mL | 0.6872 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。
BML-277 516480-79-8 Apoptosis Cell Cycle/Checkpoint Chk inhibit C3742 Checkpoint Kinase (Chk) Inhibitor C 3742 BML277 C-3742 Chk2 Inhibitor II BML 277 inhibitor