LJI308
Chemical Name: 2,6-Difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]phenol
Purity: ≥98%
Biological Activity
LJI308 is a potent pan-ribosomal S6 protein kinase (RSK) inhibitor (IC50 values are 4 to 13 nM). Displays selectivity for RSK isoforms over other kinases. Inhibits RSK-dependent Y-box binding protein 1 (YB-1) phosphorylation in vitro. Suppresses growth of triple negative breast cancer cell lines.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Discovery of potent and selective RSK inhibitors as biological probes.
Jain et al.
J.Med.Chem., 2015;58:6766 -
Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers.
Aronchik et al.
Mol.Cancer Res., 2014;12:803 -
Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells.
Davies et al.
Oncotarget., 2015;6:20570
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