We have earlier shown that ON123300 inhibits both CDK4/CDK6 and ARK5 at low nano-molar concentrations. ARK5, a fifth member of the AMPK family has been identified as a transcriptional target of several tumor cells in which it is overexpressed. Our SAR studies and modifications performed on ON123300 backbone led to the identification of ON123790 which specifically inhibits ARK5 at 14nM without interfering with CDK4/CDK6 activity.<br/><br/>In this presentation we show the synthesis, SAR, kinase profile of ON123790 and the effect of 123790 on glutamine uptake and ATP production in three tumor cell lines.

Design, synthesis and biological evaluation of specific ARK5 inhibitor

253rd National Meeting (2017)

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