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Indirubin-3-monoxime is a cell-permeable derivative of indirubin, a bioactive component of the traditional Chinese medicine Indigo Naturalis (Qing Dai). It is a potent small molecule inhibitor of several cyclin-dependent kinases (CDKs), including CDK1, CDK2, and CDK5, as well as glycogen synthase kinase-3 beta (GSK-3β). Beyond its kinase-inhibitory profile, indirubin-3-monoxime has been identified as a direct binder and inhibitor of STAT3 phosphorylation, which subsequently downregulates downstream targets such as PIM1 kinase. These mechanisms contribute to its anti-proliferative and pro-apoptotic effects in various cancer models, particularly in hematologic malignancies like multiple myeloma. It is widely utilized as a research tool to investigate cell cycle regulation and signaling pathways, and its derivatives are currently being explored for their potential to enhance immune cell-mediated cytotoxicity and overcome immune escape in tumor microenvironments.
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