LJH685 is a strong, ATP-competitive, and selective inhibitor of RSK (ribosomal S6 kinase), effectively inhibiting the biochemical activities of RSK1, RSK2, and RSK3 with IC50 values of 6, 5, and 4 nM, respectively[1].
体外研究
When applied in concentrations ranging from 0.01 to 100 μM over 72 hours, LJH685 significantly curtails the proliferation of MDA-MB-231 and H358 cells within a soft agar environment, displaying EC50 values of 0.73 and 0.79 μM, correspondingly[1].
Moreover, LJH685 (0.1-10 μM; 4 hours) substantially diminishes phosphorylation of YB1 at submicromolar levels, achieving almost complete suppression at elevated concentrations[1].
LJH685 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HCC1937 cells
10 μM
LJH685 inhibits YB-1 Ser102 phosphorylation, reduces expression of KLF5, FGF-BP1, and Cyclin D1
Cell Death Differ. 2022 Jun;29(6):1283-1295
HCC1806 cells
10 μM
LJH685 inhibits YB-1 Ser102 phosphorylation, reduces expression of KLF5, FGF-BP1, and Cyclin D1
Cell Death Differ. 2022 Jun;29(6):1283-1295
RGC-5 cells
1, 3, and 10 μM
4 hours
Inhibition of RSK3 activity, downregulation of RIP3 phosphorylation, and reduction of necroptosis in RGC-5 cells.
J Anat. 2020 Jul;237(1):29-47
LJH685 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
HCC1806 xenograft model
Intraperitoneal injection
40 mg/kg
Daily for 21 days
LJH685 significantly inhibits tumor growth, reduces expression of YB-1 pS102, KLF5, KRT16, Ly6D, and Cyclin D1, and increases cleaved-PARP1 expression
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