产品
编 号：F440134
分子式：C10H16N2O2S4
分子量：324.51
分子式：C10H16N2O2S4
分子量：324.51
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 729-46-4
产品详情
生物活性：
JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity.
体内研究：
JX06 (40-80?mg/kg; i.p. for 21 days) inhibits tumor growth in vivo.Animal Model:A549 subcutaneous xenograft mice
Dosage:40, 80?mg/kg
Administration:I.p. injections for 21 days
Result:Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control.Well tolerated at the administration dose.
体外研究：
JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM.JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR.JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells.JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner.JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells.JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) .
JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity.
体内研究：
JX06 (40-80?mg/kg; i.p. for 21 days) inhibits tumor growth in vivo.Animal Model:A549 subcutaneous xenograft mice
Dosage:40, 80?mg/kg
Administration:I.p. injections for 21 days
Result:Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control.Well tolerated at the administration dose.
体外研究：
JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM.JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR.JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells.JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner.JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells.JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) .
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