M-110 是一种高选择性的,ATP 竞争性的 PIM 激酶抑制剂,M-110 对 PIM-3 抑制作用最好,IC50=47 nM。M-110 抑制 PIM-1 和 PIM-2 的IC50 为 2.5 μM。M-110 抑制前列腺癌细胞的增殖,IC50 为 0.6-0.9 μM。
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.
Cell Viability Assay
Cell Line:
|
DU-145 cells
|
Concentration:
|
0.01, 0.1, 1, 10 μM
|
Incubation Time:
|
72 hours
|
Result:
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Inhibiting the growth of DU-145 cells with an IC
50
value of 0.9 μM.
|
Western Blot Analysis
Cell 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.
|