Then, we selected PDK4‐IN‐1 hydrochloride, an anthraquinone derivative and a potent and orally active PDH kinase 4 inhibitor; VER‐246608, a potent and ATP‐competitive inhibitor of PDH kinases (PDK1, PDK2, PDK3, and PDK4); and DCA, a metabolic regulator in cancer cells' mitochondria with anticancer activity by inhibiting PDK activity; and examined the effect of these agents on cellular response. This evidence concerns the gene PDK3 and cancer.