LJH685

• CAT Number: I002103
• CAS Number: 1627710-50-2
• Molecular Formula: C₂₂H₂₁F₂N₃O
• Molecular Weight: 381.42
• Purity: ≥95%
• Synonyms: 2,6-difluoro-4-(4-(4-(4-methylpiperazin-1-yl)phenyl)pyridin-3-yl)phenol
• Target: Apoptosis
• 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（Cat No.:I002103）is a selective inhibitor of Salt-Inducible Kinases (SIKs), specifically targeting SIK1, SIK2, and SIK3. These kinases are involved in regulating gene transcription, metabolism, and inflammation by modulating key pathways, including CREB-regulated gene expression. By inhibiting SIK activity, LJH685 affects processes like glucose metabolism and inflammatory responses, making it a valuable tool for studying SIK-related mechanisms in metabolic diseases and inflammation. It has shown potential for modulating immune responses, improving insulin sensitivity, and providing neuroprotective effects, offering insights into the development of novel therapeutic strategies for metabolic and inflammatory 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.