Indirubin is an active ingredient mainly used to treat leukemia in China and is reported to be a leading inhibitor of cyclindependent kinases (CDKs) and glycogen synthase kinase-3 (GSK-3) by competing with ATP binding sites. New findings have indicated that its comprehensive structure may contribute to its polypharmacological activities particularly in cancer and neurodegenerative disease therapy, as both of these diseases are usually accompanied by a common molecular link related to abnormal phosphorylation of CDKs and GSK-3. In the elderly, cancer and neurodegenerative disease are tightly associated common diseases and sometimes unavoidably coexist. In this review, the underlying mechanisms of the dual actions of indirubin and its structurally-related compounds in cancer and neurodegenerative disease therapy are presented.
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