JX06

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JX06 是一种有效的、选择性的共价 PDK 抑制剂，抑制 PDK1、PDK2 和 PDK3，IC50 分别为 49 nM、101 nM 和 313 nM。

JX06, a potent, selective and covalent PDK inhibitor, inhibits PDK1, PDK2 and PDK3 with IC50 of 49 nM, 101 nM and 313 nM respectively.

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) . Apoptosis Analysis Cell Line:A549, EBC-1, HT-29 and H460 cells Concentration:0, 1, 3, 10 μM 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, 0.6 μM 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, 10 μM 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.

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.

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PI3K/Akt/mTOR signaling

PDK

PDK

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729-46-4

324.5

C10H16N2O2S4

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (154.08 mM)

S=C(SSC(=S)N1CCOCC1)N1CCOCC1

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(-20℃)

With Ice Pack

≥ 2 years