JX06
产品说明书
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同义名 : | NSC 402538 |
| CAS号 : | 729-46-4 | |
| 货号 : | A1230676 | |
| 分子式 : | C10H16N2O2S4 | |
| 纯度 : | 99%+ | |
| 分子量 : | 324.51 | |
| MDL号 : | MFCD00072237 | |
| 存储条件： |
Pure form Inert atmosphere, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(154.08 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Pyruvate dehydrogenase kinase PDK1 is a metabolic enzyme responsible for switching glucose metabolism from mitochondrial oxidation to aerobic glycolysis in cancer cells, a general hallmark of malignancy termed the Warburg effect. JX06 is a potent, selective and covalent inhibitor of PDK with IC50s of 49, 101 and 313 nM for PDK1, PDK2 and PDK3, respectively. In A549 cells, JX06 (0-0.6 μM; 72 hours) dose-dependently inhibited the cell growth, and JX06 (0.1-10 μM; 6-24 hours) inhibited PDHA1 phosphorylation in a time- and dose-dependent manner. JX06 (1-10 μM) increased glucose uptake and intracellular ATP level and reduced aerobic glycolysis determined by the lactate production. JX06 (1-10 μM; 24 hours) induced ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR). In A549 xenograft models, JX06 (40-80 mg/kg; i.p. for 21 days) inhibited tumor growth[2]. | ||
| 作用机制 | JX06 forms a disulfide bond with the thiol group of a conserved cysteine residue (C240) based on recognition of a hydrophobic pocket adjacent to the ATP pocket of the PDK1 enzyme[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.08mL 0.62mL 0.31mL |
15.41mL 3.08mL 1.54mL |
30.82mL 6.16mL 3.08mL |
| 参考文献 |
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