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LS-102 {[allProObj[0].p_purity_real_show]}

货号:A1340566

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.

LS-102 化学结构 CAS号:1456891-34-1
LS-102 化学结构
CAS号:1456891-34-1
LS-102 3D分子结构
CAS号:1456891-34-1
LS-102 化学结构 CAS号:1456891-34-1
LS-102 3D分子结构 CAS号:1456891-34-1
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LS-102 纯度/质量文件 产品仅供科研

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LS-102 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].

LS-102 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.

LS-102 实验方案

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

LS-102 技术信息

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

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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