Product Overview
VER-246608 | T17224 | TargetMol Chemicals
CAS: 1684386-71-7
Smiles: Cc1cnc(Cl)nc1-c1ccc(cc1)N(Cc1ccc(CNC(=O)C(F)F)cc1)C(=O)c1ccc(O)cc1O
Formula: C28H23ClF2N4O4
Pathway: Metabolism|||PI3K/Akt/mTOR signaling
Target: Dehydrogenase|||PDK
Receptor: N/A
Bioactivity: VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Consistent with a PDK mediated MOA, VER-246608 increased pyruvate dehydrogenase complex (PDC) activity, oxygen consumption and attenuated glycolytic activity. VER-246608 was found to potentiate the activity of doxorubicin.
Molecular Weight: 552, 96
