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VS-II-173 is a small molecule inhibitor of the Pim-1 kinase, characterized by a pyrazolo[4,3-a]phenanthridine scaffold. Developed by researchers at the University of Caen Normandy (CERMN), it is an antineoplastic agent specifically investigated for the treatment of acute myeloid leukemia (AML). Pim-1 is a serine/threonine kinase that promotes cell survival and proliferation; its overexpression is a hallmark of several hematological malignancies and is associated with resistance to chemotherapy. VS-II-173 acts as an ATP-competitive inhibitor, binding to the orthosteric site of the Pim-1 kinase to block its signaling pathways, thereby inducing apoptosis and inhibiting the growth of AML cells such as the MOLM-13 line. It has served as a structural template for the synthesis of subsequent generations of Pim inhibitors.
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