LS-102 

LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC₅₀ of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment^[1][2].

LS-102 抑制 RSCs 的增殖，IC₅₀ 为 5.4 μM^[1]。
LS-102 抑制类风湿滑膜细胞 (RSCs) 的增殖Syvn1依赖方式。LS-102 抑制 Syvn1 靶蛋白的多泛素化，包括核因子红细胞 2 相关因子 2 (NRF2)、V247M α-肌聚糖突变体和 PGC-1β。LS-102 抑制 Synoviolin (Syvn1) 的 E3 连接酶活性^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

LS-102 (1.3-4 mg/kg；腹腔注射；每日一次，持续 4 周) 可降低 CIA 模型中的临床严重程度评分^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

452.60

C₂₄H₃₆N₈O

1456891-34-1

固体

Pale purple to light pink

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. Yagishita N, et al. RING-finger type E3 ubiquitin ligase inhibitors as novel candidates for the treatment of rheumatoidarthritis. Int J Mol Med. 2012 Dec;30(6):1281-6.  [Content Brief]

  [2]. Fujita H, et al. Identification of the inhibitory activity of walnut extract on the E3 ligase Syvn1. Mol Med Rep. 2018 Dec;18(6):5701-5708.  [Content Brief]