VER-246608 | PDK inhibitor

CAS:1684386-71-7

Catalog Number:10-4224

VER-246608 (1684386-71-7) is a  potent (IC50’s: PDK-1 = 35 nM, PDK-2 = 84 nM, PDK-3 = 40 nM, PDK-4 = 91 nM) 

and selective pan-pyruvate dehydrogenase kinase inhibitor.1 It decreased oxygen consumption and attenuated 

glycolytic activity (Warburg metabolism) under D-glucose/L-glutamine-depleted conditions. VER-246608 treatment of

 four cancer lines (PC-3, SW-1088, UM-22B, and MEF) under depleted D-glucose/L-glutamine conditions resulted in 

almost complete inhibition of cell growth.  It also acted synergistically with doxorubicin in PC-3 and ES-2 cells.

Activity:

PDK inhibitor

Chemical Names:

N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide

Molecular Weight:

552.96

Molecular Formula:

C28H23ClF2N4O4

Solubility:

Soluble in DMSO (>25 mg/ml)

Physical Properties:

White to off-white solid

Purity:

>98% HPLC

NMR: (Conforms)

Storage Temperature:

-20°C

Stability:

Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.

Shipping Code:

RT

References/Citations:

Moore et al. (2014), VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, 

disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells; Oncotarget 5 12862