LS-102

1456891-34-1

452.60

DMSO : 31.25 mg/mL (69.05 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

Metabolic Enzyme/Protease

LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC₅₀ of 35 uM. LS-102 has the potential for rheumatoid arthritis treatment^[1][2]. In Vitro: LS-102 inhibits proliferation of RSCs with an IC₅₀ of 5.4 uM^[1].
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 alpha-sarcoglycan mutant, and PGC-1beta. LS-102 inhibits E3 ligase activity of Synoviolin (Syvn1)^[2]. In Vivo: LS-102 (1.3-4 mg/kg; i.p.; daily for 4 weeks) reduces clinical severity scores in a CIA model^[1].