VER-246608 is a pan-inhibitor of pyruvate dehydrogenase kinase (PDHK; IC50s = 35, 84, 40, and 91 nM for PDHK1, -2, -3, and -4, respectively). It is selective for PDHKs over heat shock protein 90 (Hsp90; IC50 = >100 µM), as well as a panel of 97 kinases at 10 µM. VER-246608 (10 and 20 µM) decreases the production of L-lactate, a marker of glycolytic activity, in PC3 cells cultured in D-glucose- and L-glutamine-depleted media. It reduces the growth of, and induces cell cycle arrest at the G1 phase in, serum-starved PC3 cells when used at a concentration of 20 µM.
MedKoo Cat#: 407378
Name: VER-246608
CAS#: 1684386-71-7
Chemical Formula: C28H23ClF2N4O4
Exact Mass: 552.1376
Molecular Weight: 552.96
Elemental Analysis: C, 60.82; H, 4.19; Cl, 6.41; F, 6.87; N, 10.13; O, 11.57
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 2.0 | 3.62 | |
| DMSO | 2.0 | 3.62 | |
| DMSO:PBS (pH 7.2) (1:1) | 0.5 | 0.90 |
The following data is based on the product molecular weight 552.96 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
