[CAS NO. 921099-13-0] TM-1
PRODUCTS SPECIFICATIONS [921099-13-0]
DESCRIPTION [921099-13-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 468.54 |
| Molecular Formula | C26H32N2O6 |
| SMILES | O=C1C(C2=CC=C(OC)C(OC)=C2)=C(C)C3=CC=C(OCCN4CCN(CCO)CC4)C=C3O1 |
Summary
TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase ( PDHK1 ). TM-1 inhibits PDHK1 and PDHK2 with IC 50 s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation [1] .
IC50 & 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 IC
50
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 EC
50
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |