Synonyms: 2,6-Difluoro-4-(4-(4-morpholinophenyl)pyridin-3-yl)phenol; 2,6-Difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]phenol
Molecular Formula: C21H18F2N2O2
Molecular Weight: 368.38
Linear Structural Formula: C21H18F2N2O2
MDL Number: MFCD29905461
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: LJI308 is potent pan-RSK inhibitor that targets RSK N-terminal kinase domain (NTKD) ATP-binding site (IC50/[ATP] = 6 nM/5 muM/RSK1, 4 nM/20 muM/RSK2, 13 nM/10 muM/RSK3), exhibiting similary binding affinity toward RSK1-4, but much reduced inhibitory potency against S6K1 (IC50 = 0.8 muM), MEK4 (IC50 >10 muM), and HIP kinase 1 (IC50 >1 muM). LJI308 effectivelfy reduces cellular Y-box binding protein-1 (YB1) Ser102 (EC50 = 0.2-0.3 muM; MDA-MB-231 and H358 cells), but not ribosomal S6 protein (S6RP) S235/236, phosphorylation level and selectively inhibits the growth of YB1-overpressing HTRY-LT triple-negative breast cancer (TNBC) cells, but not the parental non-tumorigenic human mammary epithelial cell (HMEC) line HTRZ (% inhibition = 6.8%/HTRZ, 88%/HTRY-LT1, 66%/HTRY-LT2 in 8 days; 5 muM at 0 and 96 hr).