921099-13-0

921099-13-0 structure

Name: TM-1
Chemical Name: TM-1
CAS Number: 921099-13-0
Molecular Formula: C₂₆H₃₂N₂O₆
Molecular Weight: 468.54
Catalog: Signaling Pathways Metabolic Enzyme/Protease PDHK
Create Date: 2022-08-31 10:10:44
Modify Date: 2024-01-09 13:02:56
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].

Name	TM-1

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].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> PDHK Research Areas >> Cancer
Target	IC50: 2.97 μM (PDK1), 5.2 μM (PDK2)[1]
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.
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.

Molecular Formula	C₂₆H₃₂N₂O₆
Molecular Weight	468.54