Biochem/physiol Actions
An ATP-competitive, potent pan-PDK inhibitor that efficiently disrupts Warburg metabolism
VER-246608 is a cell-permeable resorcinol amide compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of pan-PDK isoform PDK (IC50 = 35, 84, 40 and 91 nM against PDK1, PDK2, PDK3 and PDK4, respectively) with minimal activity towards HSP-90 (IC50 > 10 µM). VER-246608 effectively enhances PDHA1 (pyruvate dehydrogenase E1-alpha subunit) activity and markedly diminishes PDHA1-Ser293 and -Ser300 phosphorylations without inducing severe cancer cell death. Efficiently disrupts Warburg metabolism and demonstrates cancer cells growth arrest under nutrient-deficient conditions. Also inhibits tumor spheroids growth with a potency that was comparable to cells grown in 2D-culture.
| Quality Segment | 100 |
| assay | ≥98% |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (Warmed) |
| storage temp. | -10 to -25°C |
| SMILES string | O=C(N(CC1=CC=C(CNC(C(F)F)=O)C=C1)C2=CC=C(C3=NC(Cl)=NC=C3C)C=C2)C4=CC=C(C=C4O)O |
