Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bioymifi (DR5 Activator) 是一种 TRAIL 受体DR5激活剂,与DR5的胞外结构域结合,Kd 为 1.2 μM,它可诱导 DR5 聚集,导致细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 249 | 现货 | ||
2 mg | ¥ 348 | 现货 | ||
5 mg | ¥ 597 | 现货 | ||
10 mg | ¥ 995 | 现货 | ||
25 mg | ¥ 2,230 | 现货 | ||
50 mg | ¥ 3,990 | 现货 | ||
100 mg | ¥ 5,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 657 | 现货 |
产品描述 | Bioymifi (DR5 Activator) is a novel and potent small-molecule activator of the TRAIL receptor DR5 in human cancer cells. |
靶点活性 | DR5 receptor:1.2 μM(Kd) |
体外活性 | Bioymifi is able to promote cell death without the need for the Smac mimetic in T98 g cells. At a 10 μM concentration, bioymifi induces processing of caspase-3 into smaller fragments. Caspase-8 and the related extrinsic apoptotic pathway are essential for bioymifi-induced cell death. Bioymifi induces DR5-dependent death pathways and is independent of TRAIL. Bioymifi binds the ECD of DR5 with a Kd of 1.2 μM but shows little binding affinity to the DR4 ECD. It has poor solubility in buffer solutions. Bioymifi promotes apoptosis by directly binding to and facilitating aggregation of DR5. When bioymifi reaches micromolar concentration, its capability to aggregate DR5 is strong enough to induce apoptosis in various cancer cells[1]. |
激酶实验 | Solubilized membranes from 3T3 Flk-1 cells are added to polystyrene ELISA plates that has been precoated with a monoclonal antibody that recognizes Flk-1. After an overnight incubation with lysate at 4°C, serial dilutions of SU5416 are added to the immunolocalized receptor. To induce autophosphorylation of the receptor, various concentrations of ATP are added to the ELISA plate wells containing serially diluted solutions of SU5416. The autophosphorylation is allowed to proceed for 60 min at room temperature and then stopped with EDTA. The amount of phosphotyrosine present on the Flk-1 receptors in the individual wells is determined by incubating the immunolocalized receptor with a biotinylated monoclonal antibody directed against phosphotyrosine. After removal of the unbound anti-phosphotyrosine antibody, avidin-conjugated horseradish peroxidase H is added to the wells. A stabilized form of 3,3′,5,5′-tetramethyl benzidine dihydrochloride and Water2 is added to the wells. The color readout of the assay is allowed to develop for 30 min, and the reaction is stopped with H2SO4. Parallel biochemical kinase assays are performed to measure autophosphorylation on EGFR and fibroblast growth factor receptor[1]. |
细胞实验 | Dose-response curves of bioymifi and A2C2 in T98 g cells are plotted as a function of A2C2 or bioymifi concentration. Human glioblastoma (T98 g) cells are treated with various concentrations of A2C2 or bioymifi alone or in combination with 1 μM Smac mimetic (SM) for 48 h. The corresponding cell survival is normalized to the treatment without A2C2 or bioymifi.(Only for Reference) |
别名 | DR5 Activator |
分子量 | 494.32 |
分子式 | C22H12BrN3O4S |
CAS No. | 1420071-30-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7.5 mg/mL (15.17 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.023 mL | 10.1149 mL | 20.2298 mL | 50.5745 mL |
5 mM | 0.4046 mL | 2.023 mL | 4.046 mL | 10.1149 mL | |
10 mM | 0.2023 mL | 1.0115 mL | 2.023 mL | 5.0575 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。
Bioymifi 1420071-30-2 Apoptosis TNF cancer TNF Receptor Inhibitor TNFR extracellular inhibit caspase-8 Tumor Necrosis Factor Receptor DR5 Activator aggregation domain cells inhibitor