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Successful drug repurposing relies on the understanding of molecular mechanisms of the target compound. Cardiac glycosides have demonstrated potent anticancer activities; however, the pharmacological mechanisms underlying their anticancer effects remained elusive, which has restricted their further development in cancer treatment. A bottleneck is the lack of comprehensive understanding about genes and signaling pathways that are altered at the early stage of drug treatment, which is key to understand how they inhibit cancer. To address t