VS-II-173 is a pan-Pim kinase inhibitor with IC 50 values of 0.07 μM and 0.02 μM for Pim1 and Pim3 , respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2 , PRK2 , RSK1 , DYRK1a and AMPK α1 , selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells ( EC 50 > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694) , MDM2 (S166) , Bad (S112) , and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis . VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin ( HY-13062A ). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations .
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