Chemical Name: N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide
Pan-PDK inhibitor
Molekulargewicht:
552.96
Reinheit:
>98% by HPLC NMR (Conforms)
Formulierung:
White to off-white solid
CAS Nummer:
[1684386-71-7]
Formel:
C28H23ClF2N4O4
Anwendungsbeschreibung:
VER-246608 is a potent (IC50s: 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.
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