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
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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].
| 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]. |
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| Related Catalog | |
| 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 |
| Molecular Formula | C26H32N2O6 |
|---|---|
| Molecular Weight | 468.54 |