Human embryonic kidney (HEK293) cells were obtained from the American Type Culture Collection (ATCC, Manassas, VA). HEK293 cells stably transfected with mouse OCT1 (mOCT1) or human OCT1 (hOCT1) were cultured in Dulbecco’s Modified Eagle Media (DMEM) media supplemented with 10% fetal bovine serum (FBS) and grown at 37°C in a humidified incubator containing 5% CO2. Radiolabeled [14C] TEA and [14C] metformin were obtained from American Radiochemicals (St. Louis, MO). Cellular uptake assays were performed 48 h following transient transfection by Lipofectamine 3000 Transfection Reagent (Thermo Fisher Scientific, Waltham, MA). ON-TARGETplus Human YES1 siRNA was obtained from Dharmacon (Lafayette, CO). RNA extraction kits were obtained from Omega Bio-tek (Norcross, GA). Reference standards of decynium22, a positive control inhibitor, as well as the TKIs bosutinib, dasatinib, gilteritinib, ibrutinib, lapatinib, sunitinib, vandetanib, and CH6953755 were obtained from MedChemExpress (Monmouth Junction, NJ).

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