M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC 50 =47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC 50 s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC 50 s of 0.6 to 0.9 μM.
In Vitro
M-110 (0.01-10 μM; 72 hours) inhibiting the growth of DU-145 cells with an IC 50 value of 0.9 μM. M-110 has no activity on normal human peripheral blood mononuclear cells up to 40 μM. M-110 (10 μM; 18 hours) inhibits STAT3 Tyr705 phosphorylation. M-110 inhibits the expression of active STAT3 through inhibition of PIM-3. M-110 also inhibits the proliferation of 22Rv1, PC3, and SW480 cells, with IC50 values of 0.6 to 0.8 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: DU-145 cells Concentration: 0.01, 0.1, 1, 10 μM Incubation Time: 72 hours Result: Inhibiting the growth of DU-145 cells with an IC 50 value of 0.9 μM. Western Blot AnalysisCell Line: DU-145 cells Concentration: 10 μM Incubation Time: 18 hours Result: Reduced the expression of p-STAT3 Tyr705 to 23.5%, compared with untreated cells without affecting the expression of STAT3.
