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CAS No.: 1456891-34-1

LS-102 Catalog No. CSN27287

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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400-920-2911

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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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2095 mL
- 11.0474 mL
- 22.0948 mL
- 5 mM
- 0.4419 mL
- 2.2095 mL
- 4.4190 mL
- 10 mM
- 0.2209 mL
- 1.1047 mL
- 2.2095 mL

技术信息

CAS号	1456891-34-1	储存条件	粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C24H36N8O	运输	蓝冰
分子量	452.60	别名

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