LS-102
目录号: PL03514 纯度: ≥96%
CAS No. :1456891-34-1
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中文名称
LS-102
英文名称
LS-102
英文别名
(S)-N2-(Benzo[d]oxazol-6-yl)-N4-(1-cyclohexylethyl)-N6-ethyl-N6-(2-(ethylamino)ethyl)-1,3,5-triazine;LS-102;(S)-N2-(Benzo[d]oxazol-6-yl)-N4-(1-cyclohexylethyl)-N6-ethyl-N6-(2-(ethylamino)ethyl)-1,3,5-triazine-2,4,6-triamine;6-N-(1,3-Benzoxazol-6-yl)-4-N-[(1S)-1-cyclohexylethyl]-2-N-ethyl-2-N-[2-(ethylamino)ethyl]-1,3,5-triazine-2,4,6-triamine
Cas No.
1456891-34-1
分子式
C24H36N8O
分子量
452.60
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
LS 102 是一种选择性的 E3 连接酶 synoviolin (Syvn1) 抑制剂。LS-102 抑制 Syvn1 自泛素化,IC50 约为 35 μM,有研究类风湿关节炎的潜力。
生物活性
LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC 50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment.
性状
Solid
体外研究(In Vitro)
LS-102 inhibits proliferation of RSCs with an IC50 of 5.4 μM.
LS-102 suppresses proliferation of rheumatoid synovial cells (RSCs) in a Syvn1-dependent manner. LS-102 suppresses polyubiquitination of target proteins of Syvn1, including nuclear factor erythroid 2-related factor 2 (NRF2), V247M α-sarcoglycan mutant, and PGC-1β. LS-102 inhibits E3 ligase activity of Synoviolin (Syvn1). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
LS-102 (1.3-4 mg/kg; i.p.; daily for 4 weeks) reduces clinical severity scores in a CIA model. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 7-week-old DBA/1 male mice (CIA model)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[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.
[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.
溶解度数据
In Vitro: DMSO : 31.25 mg/mL (69.05 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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