TM-1 |
| Katalog-Nr.GC65502 |
TM-1 ist ein potenter Inhibitor der Pyruvat-Dehydrogenase-Kinase (PDHK1). TM-1 hemmt PDHK1 und PDHK2 mit IC50-Werten von 2,97 μM bzw. 5,2 μM. TM-1 blockiert die Phosphorylierung des Pyruvat-Dehydrogenase-Komplexes (PDHC) und hemmt die Zellproliferation.
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Cas No.: 921099-13-0
Sample solution is provided at 25 µL, 10mM.
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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].
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].
[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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