Description
TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase ( PDHK1 ). TM-1 inhibits PDHK1 and PDHK2 with IC 50 s of 2.97 µM and 5.2 µM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferationIn VitroTM-1 (0-10 µM) inhibits PDHK1 activity with the inhibition rate of 80.5% (dosage at 10 µM) and an IC 50 value of 2.97 µM. TM-1 (0-2.1 µM; 12 h) shows anti-osteosarcoma activity and inhibits MG-63 cells with an EC 50 value of 14.5 µM. TM-1 (3, 6, 12 µM; 24 h) decreases PDHC phosphorylation of both Ser293 and Ser232 sites in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MG-63 cells Concentration: 3, 6, 12 µM Incubation Time: 24 hours Result: Dramatically reduced the PDHK phosphorylation of both Ser293 and Ser232 sites at 6 or 12 µM.Form:SolidIC50& Target:IC50: 2.97 µM (PDK1), 5.2 µM (PDK2)