VS-II-173 is a pan-Pim kinase inhibitor with IC50 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 AMPKalpha1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC50 > 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 [1][2].
Molekulargewicht:
264.24
CAS Nummer:
[1627962-21-3]
Formel:
C14H8N4O2
Target-Kategorie:
AMPK,Apoptosis,DYRK,MDM-2/p53,Pim,STAT
Anwendungsbeschreibung:
MCE Product type: Reference compound
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