LS-102

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Chemical Structure| 1456891-34-1 同义名 : -
CAS号 : 1456891-34-1
货号 : A1340566
分子式 : C24H36N8O
纯度 : 98%+
分子量 : 452.6
MDL号 : MFCD32671959
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(232 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
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].
实验方案
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
参考文献

[1]Yagishita N, Aratani S, Leach C, et al. RING-finger type E3 ubiquitin ligase inhibitors as novel candidates for the treatment of rheumatoid arthritis. Int J Mol Med. 2012;30(6):1281-1286.

[2]Yagishita N, Aratani S, et al. RING-finger type E3 ubiquitin ligase inhibitors as novel candidates for the treatment of rheumatoid arthritis. Int J Mol Med. 2012 Dec;30(6):1281-6.