Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HA14-1 是一种 Bcl-2/Bcl-xL 拮抗剂,与 Bcl-2 上的特定口袋结合,IC50约为 9 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 188 | 现货 | ||
10 mg | ¥ 325 | 现货 | ||
25 mg | ¥ 552 | 现货 | ||
50 mg | ¥ 828 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 213 | 现货 |
产品描述 | HA14-1, a Bcl-2/Bcl-XL antagonist, is a non-peptidic ligand of a Bcl-2 surface pocket (IC50: ~9 μM). |
靶点活性 | BCL2:9 μM |
体外活性 | 在免疫缺陷小鼠体内,HA14-1(400 nM)对胶质母细胞瘤的生长无明显作用.但在体内HA14-1(400 nM)可增强DNA损伤剂依托泊苷(2.5 mg/kg)对胶质母细胞瘤生长的作用效果. |
体内活性 | 作用于滤泡性淋巴瘤细胞系HF1A3, HF4.9和HF28RA时,HA14-1具有细胞毒性,LC50为4.5/12.6/8.1 μM。通过激活caspase,HA14-1剂量依赖性诱导HL-60细胞凋亡。HA14-1经caspase和ROS诱导HF4.9,HF1A3和HF28RA细胞凋亡。 |
激酶实验 | Affinity determination: The binding affinity of organic compounds to Bcl-2 protein in vitro is determined by a competitive binding assay based on fluorescence polarization. For this assay, 5-carboxyfluorecein is coupled to the N terminus of a peptide, GQVGRQLAIIGDDINR, derived from the BH3 domain of Bak (Flu-BakBH3), which has been shown to bind to the surface pocket of the Bcl-xL protein with high-affinity. According to our molecular modeling studies and binding measurement using fluorescence polarization, the Flu-BakBH3 peptide binds the surface pocket of Bcl-2 with a similar affinity. Bcl-2 used in this assay is a recombinant GST-fused soluble protein. Flu-BakBH3 and Bcl-2 protein are mixed in the presence or absence of organic compounds under standard buffer conditions and are incubated for 30 min. The binding of Flu-BakBH3 to Bcl-2 protein is measured on a LS-50 luminescence spectrometer equipped with polarizers using a dual path length quartz cell (500 μl). The fluorophore is excited with vertical polarized light at 480 nm (excitation slit width 15 nm), and the polarization value of the emitted light is observed through vertical and horizontal polarizers at 530 nm (emission slit width 15 nm). The binding affinity of each compound for Bcl-2 protein is assessed by determining the ability of different concentrations of the compound to inhibit Flu-BakBH3 binding to Bcl-2. |
细胞实验 | The cytotoxic effects of HA14-1 against different FL cell lines are determined by the MTT assay. Briefly, the cells (5000/well) are incubated in triplicate in 96-well plate in the presence or absence of HA14-1 for 20 h at 37 °C. Thereafter, the MTT solution is added to each well. After 4 h incubation at 37 °C, the optical density (OD) is measured by means of 96-well plate reader, with the extraction buffer as a blank. The following formula is used: percentage cell viability = (OD of the experiment samples/OD of the control) × 100. Sigmoidal dose-response curves are fitted to the mean cell viability plotted against log HA14-1 dose and lethal concentration 50% (LC50) values are calculated from the resulting curves using Prism 4.0 softw(Only for Reference) |
分子量 | 409.23 |
分子式 | C17H17BrN2O5 |
CAS No. | 65673-63-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 40.9 mg/mL (100 mM)
DMSO: 40.9 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.4436 mL | 12.2181 mL | 24.4361 mL | 61.0903 mL |
5 mM | 0.4887 mL | 2.4436 mL | 4.8872 mL | 12.2181 mL | |
10 mM | 0.2444 mL | 1.2218 mL | 2.4436 mL | 6.109 mL | |
20 mM | 0.1222 mL | 0.6109 mL | 1.2218 mL | 3.0545 mL | |
50 mM | 0.0489 mL | 0.2444 mL | 0.4887 mL | 1.2218 mL | |
100 mM | 0.0244 mL | 0.1222 mL | 0.2444 mL | 0.6109 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。
HA14-1 65673-63-4 Apoptosis BCL Bcl-2 Family HA141 HA14 1 HA-14-1 inhibit Inhibitor inhibitor