JX06

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]. IC50 & Target: IC50: 49 nM (PDK1), 101 nM (PDK2), 313 nM (PDK3)^[1] In Vitro: 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]. In Vivo: JX06 (40-80 mg/kg; i.p. for 21 days) inhibits tumor growth in vivo^[1].