LS-102 (C09-1142-670)

LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC 50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment.In VitroLS-102 inhibits proliferation of RSCs with an IC 50 of 5.4 μM. ?/nLS-102 suppresses proliferation of rheumatoid synovial cells (RSCs) in a Syvn1-dependent manner. LS-102 suppresses polyubiquitination of target proteins of Syvn1, including nuclear factor erythroid 2-related factor 2 (NRF2), V247M α-sarcoglycan mutant, and PGC-1β. LS-102 inhibits E3 ligase activity of Synoviolin (Syvn1). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Rheumatoid synovial cells (RSCs) Concentration: 20, 40, 60 μM Incubation Time: 12 hours Result: Inhibited proliferation of RSCs with an IC 50 of 5.4 µM.In VivoLS-102 (1.3-4 mg/kg; i.p.; daily for 4 weeks) reduces clinical severity scores in a CIA model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 7-week-old DBA/1 male mice (CIA model) Dosage: 1.3, 4.0 mg/kg Administration: I.p.; daily for 4 weeks Result: Reduced the clinical severity scores.Form:Solid. Molecular Formula: C24H36N8O Molecular Weight: 452.6 PubChem CID: 118518043 Isomeric SMILES: CCNCCN(CC)C1=NC(=NC(=N1)N[C@@H](C)C2CCCCC2)NC3=CC4=C(C=C3)N=CO4