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 proliferation In Vitro TM-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:Solid IC50& Target:IC50: 2.97 μM (PDK1), 5.2 μM (PDK2)