LS-102 is a selective inhibitor of E3 ubiquitin ligase synoviolin (Syvn1). LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment.
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描述 | Synoviolin (Syvn1), a RING-type E3 ubiquitin ligase in endoplasmic reticulum associated protein degradation, is involved in rheumatoid arthritis, fibrosis, liver cirrhosis and obesity. LS-102 inhibited the autoubiquitination of synoviolin with an IC50 value of 20 μM. Further evaluation of LS-102 in an in vitro ubiquitination assay showed that the inhibition of synoviolin activity by LS-102 was dose-dependent with an IC50 value of 35 μM. LS-102 inhibited HeLa cell growth at very high concentrations with an IC50 of 32.7 μM. Moreover, treatment of RSCs (rheumatoid synovial cells) with LS-102 suppressed synovial cell growth dose-dependently and with much greater potency than that observed in HeLa cells. In a mouse model of arthritis, intraperitoneal treatment with 1.3 mg/kg or 4.0 mg/kg LS-102 starting on day 21 reduced the clinical severity scores compared to vehicle controls. Finally, histological analysis showed lower histological arthritis scores in mice treated with LS-102 compared with wild-type mice[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.21mL 0.44mL 0.22mL |
11.05mL 2.21mL 1.10mL |
22.09mL 4.42mL 2.21mL |
CAS号 | 1456891-34-1 |
分子式 | C24H36N8O |
分子量 | 452.6 |
SMILES Code | CCNCCN(CC)C1=NC(NC2=CC=C3N=COC3=C2)=NC(N[C@H](C4CCCCC4)C)=N1 |
MDL No. | MFCD32671959 |
别名 | |
运输 | 蓝冰 |
InChI Key | DEDHMXBDEJSZFE-KRWDZBQOSA-N |
Pubchem ID | 118518043 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
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