VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase ( PDK ) with IC 50 s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1 , PDK-3 , PDK-2 , and PDK-4 , respectively. In Vitro VER-246608 is a novel pan-isoform ATP competitive inhibitor of PDK. VER-246608 demonstrates similar potency across all four PDK isoforms in a DELFIA-based enzyme functional assay in the sub 100 nM range. In terms of cellular biomarker modulation, VER-246608 suppresses the phosphorylation of the Ser 293 residue of E1α (phosphorylated by all four PDK isozymes) with IC 50 values of 266 nM. Treatment of PC-3 cells with 9 μM and 27 μM VER-246608 results in a 21% and 42% reduction, respectively, in media L-lactate levels following a 1 h incubation. VER-246608 also decreases D-glucose consumption at the same concentrations that result in reduced L-lactate production. An approximately 50% reduction in spheroid volume is achieved at concentrations of 10 μM and above, suggesting an increase in VER-246608 potency compared to monolayer growth. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IC50: 35 nM (PDK-1), 40 nM (PDK-3), 84 nM (PDK-2), 91 nM (PDK-4)
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VER-246608
CAS number：1684386-71-7(DMSO) molecular formula：C28H23ClF2N4O4
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1684386-71-7(DMSO) | molecular formula | C28H23ClF2N4O4 |
| molecular weight | 552.96 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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