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• 产品描述： 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

• 靶点： γ-secretase；Apoptosis;Apoptosis;Gamma-secretase

• 体内研究：
  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

• 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.

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

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.486 ml	7.431 ml	14.862 ml
  5 mM	0.297 ml	1.486 ml	2.972 ml
  10 mM	0.149 ml	0.743 ml	1.486 ml
  50 mM	0.03 ml	0.149 ml	0.297 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *