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 Vitro LS-102 inhibits proliferation of RSCs with an IC 50 of 5.4 μM. ? LS-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 Vivo LS-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
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LS-102
CAS number:1456891-34-1 molecular formula:C24H36N8O
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1456891-34-1 | molecular formula | C24H36N8O |
| molecular weight | 452.6 g/mol | Exact mass | - |
| PSA | - | logp | - |
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