| Description |
TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK1). TM-1 inhibits PDHK1 and PDHK2 with IC50s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation[1].
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| Related Catalog |
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| Target |
IC50: 2.97 μM (PDK1), 5.2 μM (PDK2)[1]
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| In Vitro |
TM-1 (0-10 μM) inhibits PDHK1 activity with the inhibition rate of 80.5% (dosage at 10 μM) and an IC50 value of 2.97 μM[1]. TM-1 (0-2.1 μM; 12 h) shows anti-osteosarcoma activity and inhibits MG-63 cells with an EC50 value 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]. Cell Viability Assay[1] Cell 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.
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| References |
[1]. Fang A, et al. Identification of pyruvate dehydrogenase kinase 1 inhibitors with anti-osteosarcoma activity. Bioorg Med Chem Lett. 2017 Dec 15;27(24):5450-5453.
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