For research use only. Not for therapeutic Use.
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].
| Catalog Number | I037356 |
| CAS Number | 921099-13-0 |
| Synonyms | 3-(3,4-dimethoxyphenyl)-7-[2-[4-(2-hydroxyethyl)piperazin-1-yl]ethoxy]-4-methylchromen-2-one |
| Molecular Formula | C26H32N2O6 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H32N2O6/c1-18-21-6-5-20(33-15-13-28-10-8-27(9-11-28)12-14-29)17-23(21)34-26(30)25(18)19-4-7-22(31-2)24(16-19)32-3/h4-7,16-17,29H,8-15H2,1-3H3 |
| InChIKey | FJPOSFVCWXTUDP-UHFFFAOYSA-N |
| SMILES | CC1=C(C(=O)OC2=C1C=CC(=C2)OCCN3CCN(CC3)CCO)C4=CC(=C(C=C4)OC)OC |
| Reference | [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. |
