LJH685

• CAT Number: I002103
• CAS Number: 1627710-50-2
• Molecular Formula: C₂₂H₂₁F₂N₃O
• Molecular Weight: 381.42
• Purity: ≥95%
• Target: S6 Kinase
• Solubility: DMSO: ≥ 31 mg/mL
• Storage: Store at -20°C
• IC50: 4 to 13 nM
• IUPAC Name: 2,6-difluoro-4-[4-[4-(4-methylpiperazin-1-yl)phenyl]pyridin-3-yl]phenol
• InChI: InChI=1S/C22H21F2N3O/c1-26-8-10-27(11-9-26)17-4-2-15(3-5-17)18-6-7-25-14-19(18)16-12-20(23)22(28)21(24)13-16/h2-7,12-14,28H,8-11H2,1H3
• InChIKey: IKUFKDGKRLMXEX-UHFFFAOYSA-N
• SMILES: CN1CCN(CC1)C2=CC=C(C=C2)C3=C(C=NC=C3)C4=CC(=C(C(=C4)F)O)F

LJH685 is a powerful and selective ATP-competitive inhibitor of RSK (Ribosomal S6 Kinase). It effectively inhibits the biological activity of RSK1, RSK2, and RSK3 with IC50 values of 6, 5, and 4 nM, respectively. By targeting RSK, LJH685 can modulate various cellular processes regulated by RSK signaling pathways. It’s high potency and selectivity make LJH685 a promising candidate for therapeutic interventions aimed at dysregulated RSK activity in diseases such as cancer and neurodegenerative disorders.

Reference

[1]. Aronchik I, 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. 2014 May;12(5):803-12.
[2]. Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015 Aug 21;6(24):20570-7.
[3]. Jain R, et al. Discovery of Potent and Selective RSK Inhibitors as Biological Probes. J Med Chem. 2015 Sep 10;58(17):6766-83.