JX06  ≥98%

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包装规格:5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(100 mg/mL 超声)
产品描述:基本信息 产品编号:J10038 产品名称:JX06 CAS: 729-46-4   储存条件 粉末 -20℃ 四年 分子式: C10H16N2O2S4 溶于液体 -80℃ 六个月 分子量 324.51 -20℃ 一个月 化学名:      Solubility (25°C)   体外 DMSO 65mg/mL (200.3mM) Ethanol Insoluble Water Insoluble 体内(现配现用)     <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.0816mL 15.4078mL 30.8157mL 5mM 0.6163mL 3.0816mL 6.1631mL 10mM 0.3082mL 1.5408mL 3.0816mL 50mM 0.0616mL 0.3082mL 0.6163mL   生物活性 产品描述 一种有效的,选择性的,共价的 PDK 抑制剂。 靶点/IC50 PDK1(Cell-free assay) PDK2(Cell-free assay) PDK3(Cell-free assay) 0.049μM 0.101μM 0.313μM   体外研究 JX06 barely shows inhibitory activity against PDK4 at a concentration of 10μM.JX06 (1-10μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR.JX06 (0-0.6μM; 72 hours) dose-dependently suppresses the growth of A549 cells.JX06 (0.1-10μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner.JX06 (1-10μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells.JX06 (1-10μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) .Apoptosis Analysis Cell Line: A549, EBC-1, HT-29 and H460 cells Concentration: 0, 1, 3, 10μM Incubation Time: 48 hours Result: Induces cell apoptosis in A549 and EBC-1 cells. Cell Viability Assay Cell Line: A549 cells Concentration: 0, 0.2, 0.4, 0.6μM Incubation Time: 72 hours Result: Inhibits the viability of A549 cells in a dose dependent manner. Western Blot Analysis Cell Line: A549 cells Concentration: 0, 0.1, 0.3, 1, 3, 10μM Incubation Time: 0, 6, 12, 24 hours Result: Decreased PDHA1 phosphorylation at both serine 293 and serine 232 (S293 and S232) in a time- and dose-dependent manner. 体内研究 JX06 (40-80mg/kg; i.p. for 21 days) inhibits tumor growth in vivo. Animal Model: A549 subcutaneous xenograft mice Dosage: 40, 80mg/kg Administration: I.p. injections for 21 days Result: Reduced tumor weights and 67.5% tumor volume at the dose of 80mg/kg compared with the vehicle control. Well tolerated at the administration dose.
保存条件:-20℃