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5-Iodotubercidin is a synthetic purine nucleoside analog and a potent small molecule inhibitor of adenosine kinase (ADK), with an IC50 of approximately 26 nM. It acts as an ATP mimetic and inhibits ADK, leading to increased extracellular adenosine levels. This compound also inhibits other kinases, including casein kinase 1 (CK1), haspin, insulin receptor kinase, and leucine-rich repeat kinase 2 (LRRK2). Mechanistically, it can induce DNA damage and apoptosis in tumor cells by activating the ATM/p53 pathway. Preclinical studies have shown anti-tumor activity in models such as insulinoma. Additionally, radiolabeled forms have been explored for imaging ADK expression in vivo. It is primarily used as a research tool; there are no approved clinical indications[1][4][9].
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