L-685458(Synonyms: L-685,458)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

L-685458 (Synonyms: L-685,458) 纯度: 99.33%

L-685458 是一种有效的过渡状态模拟(TSA) γ-分泌酶 (γ-secretase) 抑制剂 (GSI)。L-685458 抑制淀粉样 β-蛋白前体 γ-分泌酶活性,IC50 为 17 nM,选择性高于其他检测的天冬氨酸蛋白酶 50-100 倍。L-685458 抑制 γ-分泌酶介导的 APP-C99 和 Notch-100 的裂解,IC50 分别为 301.3 nM 和 351.3 nM。L-685458 可用于阿尔茨海默病 (AD) 和癌症的研究。

L-685458(Synonyms: L-685,458)

L-685458 Chemical Structure

CAS No. : 292632-98-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥7253 In-stock
1 mg ¥1400 In-stock
5 mg ¥4900 In-stock
10 mg ¥8800 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers[1][2].

体外研究
(In Vitro)

L-685458 reduces both Aβ(40) and Aβ(42) peptide formation in 3 different cells. It against Neuro2A h AβPP695, CHO h AβPP695, and SHSY5 spβA4CTF reduction of Aβ(40) with IC50 values of 402 nM, 113 nM and 48 nM, respectively. And the IC50 values are 775 nM, 248 nM, 67 nM, respectively[1].
L-685458 (5-40 μM; 24 hours) leads to a dramatic downregulation of Hes-1 in 786-O cells[3].
L-685458 has inhibitory effects in hepatoma cell lines, it against Huh7, HepG2, HLE and SKHep1 cells with IC50 of 12.91 μM, 12.69 μM, 21.76 μM and 12.18 μM, respectively[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

L-685458 (percutaneous administration; 5 mg/kg; 2 weeks) has antitumor effects in mouse hepatoma models. L-685458 inhibits EpCAM production except in necrotic areas. And HES1 staining is also diminished in the nucleus[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD-SCID Mouse Hepatoma Model[4]
Dosage: 5 mg/kg
Administration: Percutaneous administration; 5 mg/kg; 2 weeks
Result: Exhibited anti-tumor activities in vivo.

分子量

672.85

Formula

C39H52N4O6

CAS 号

292632-98-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.3 mg/mL (123.80 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4862 mL 7.4311 mL 14.8622 mL
5 mM 0.2972 mL 1.4862 mL 2.9724 mL
10 mM 0.1486 mL 0.7431 mL 1.4862 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Shearman, M.S., Beher, D., Clarke, E.E., Lewis, H.D., Harrison, T., Hunt, P.,

    [2]. Guanghui Yang, et al. Structural basis of γ-secretase inhibition and modulation by small molecule drugs. Cell. 2021 Jan 21;184(2):521-533.e14.

    [3]. Jonas Sjölund, et al. Suppression of renal cell carcinoma growth by inhibition of Notch signaling in vitro and in vivo. J Clin Invest. 2008 Jan;118(1):217-28.

    [4]. Kazunori Kawaguchi, et al. Jagged1 DNA Copy Number Variation Is Associated with Poor Outcome in Liver Cancer. Am J Pathol. 2016 Aug;186(8):2055-2067.

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