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SML1788 Sigma-Aldrich

LJI308

≥98% (HPLC)

Synonym: 2,6-Difluoro-4-(4-(4-morpholinophenyl)pyridin-3-yl)phenol, 2,6-Difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]phenol

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Kinase/Phosphatase Biology,
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 5 mg/mL, clear (warmed)
storage temp.   −20°C

Description

Packaging

5, 25 mg in glass bottle

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 μM/RSK1, 4 nM/20 μM/RSK2, 13 nM/10 μM/RSK3), exhibiting similary binding affinity toward RSK1-4, but much reduced inhibitory potency against S6K1 (IC50 = 0.8 μM), MEK4 (IC50 >10 μM), and HIP kinase 1 (IC50 >1 μM). LJI308 effectivelfy reduces cellular Y-box binding protein-1 (YB1) Ser102 (EC50 = 0.2-0.3 μM; 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 μM at 0 and 96 hr).

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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