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VER-246608

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.

Product Specifications

CAS Number

1684386-71-7

Purity

>98% (HPLC)

Solubility

DMSO:100 mg/mL (180.84 mM; Need ultrasonic)

Smiles

O=C (C1=CC=C (O) C=C1O) N (CC2=CC=C (CNC (C (F) F) =O) C=C2) C (C=C3) =CC=C3C4=NC (Cl) =NC=C4C

Molecular Formula

C28H23ClF2N4O4

Molecular Weight

552.96

Storage Conditions

Storage temperature: -20°C. Stability: ≥ 2 years

Notes

For research use only.

Available Sizes

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