| Bioactivity | 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[1]. | |||||||||
| Invitro | JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM[1].JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR[1].JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells[1].JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner[1].JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells[1].JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) [1]. Apoptosis Analysis[1] Cell Line: | |||||||||
| Name | JX06 | |||||||||
| CAS | 729-46-4 | |||||||||
| Formula | C10H16N2O2S4 | |||||||||
| Molar Mass | 324.51 | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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