TM-1 is a potent inhibitor ofpyruvate dehydrogenase kinase(PDHK1). TM-1 inhibitsPDHK1andPDHK2withIC₅₀s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation^[1].

IC50: 2.97 μM (PDK1), 5.2 μM (PDK2)^[1]

TM-1 (0-10 μM) inhibits PDHK1 activity with the inhibition rate of 80.5% (dosage at 10 μM) and an IC₅₀value of 2.97 μM^[1].
TM-1 (0-2.1 μM; 12 h) shows anti-osteosarcoma activity and inhibits MG-63 cells with an EC₅₀value of 14.5 μM^[1].
TM-1 (3, 6, 12 μM; 24 h) decreases PDHC phosphorylation of both Ser293 and Ser232 sites in a dose-dependent manner^[1].

468.54

Solid

C₂₆H₃₂N₂O₆

921099-13-0

Room temperature in continental US; may vary elsewhere.