LJH685 is a potent, ATP-competitive and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50s of 6, 5, 4 nM, respectively.
IC50&Target
IC50: 6 nM (RSK1), 5 nM (RSK1), 4 nM (RSK1)
体外研究
LJH685 (0.01-100 μM; 72 hours) efficiently inhibits the growth of MDA-MB-231 and H358 cells in soft agar with EC50s of 0.73 and 0.79 μM, respectively.
LJH685 (0.1-10 μM; 4 hours) efficiently reduces phosphorylation of YB1 at submicromolar concentrations and causes nearly complete inhibition at higher concentrations.
Cell Proliferation Assay
Cell Line:
MDA-MB-231, H358 cells
Concentration:
0.01, 0.1, 1, 10, 100 μM
Incubation Time:
72 hours
Result:
The growth in soft agar was efficiently inhibited with EC50 values of 0.73 and 0.79 μM in MDA-MB-231 and H358, respectively.
Western Blot Analysis
Cell Line:
MDA-MB-231, H358 cells
Concentration:
0.1, 0.3, 1, 3, 10 μM
Incubation Time:
4 hours
Result:
Efficiently reduced phosphorylation of YB1 at submicromolar concentrations and caused nearly complete inhibition at higher concentrations.
分子量
381.42
CAS号
1627710-50-2
运输条件
Room temperature in continental US; may vary elsewhere.