VER-246608 | PDK inhibitor

CAS:
 1684386-71-7
Catalog Number:
 10-4224

Available Options

Size:PriceQuantity 
5 mg$100.00
25 mg$375.00

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.

References/Citations:

  1. 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

 

1684386-71-7, pan-PDK inhibitor, PDK inhibitor, pyruvate dehydrogenase kinase inhibitor, VER-246608, VER-246608 supplier, VER246608
CAS:
1684386-71-7
Catalog Number:
10-4224
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

Safety Data Sheet:

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee