LJI308
Unsuitables - unsuitable to be used as a chemical probe
Structure
This is unsuitable as a chemical probe: While this
compound has been used to interrogate specific protein
targets, it is not a chemical probe and should not be used
in assays that depend on a potent and selective modulator
of the protein.
Non selective compound
Intended target: RSKs; In a panel of 442 kinases, 10 uM LJI308 inhibited 60 off-target kinases by >50% and 24 off-target kinases by >80%(BMPR2, DYRK1B, PCACalpha, TIE2, CLK3, CSNK1E, DAPK1, DAPK2, DAPK3, DYRK1A, FLT3(N841I), HIPK1, HIPK2, HIPK3, HIPK4, IRAK1, IRAK3, LOK, MAP3K3, MEK4, PIP5K2C, RPS6KA4, S6K1, TRKC). Aronchik et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res.12, 803-12 (2014).