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LDN-57444

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产品编号 T1924Cas号 668467-91-2
别名 LDN57444

LDN-57444 是一种可逆的,竞争性的,定向位点的泛素 C 末端水解酶 L1 抑制剂,IC50和Ki 值分别为 0.88 μM 和 0.40 μM。它还可抑制 UCH-L3 的活性,IC50值为 25 μM。

LDN-57444
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LDN-57444

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纯度: 99.87%
产品编号 T1924 别名 LDN57444Cas号 668467-91-2

LDN-57444 是一种可逆的,竞争性的,定向位点的泛素 C 末端水解酶 L1 抑制剂,IC50和Ki 值分别为 0.88 μM 和 0.40 μM。它还可抑制 UCH-L3 的活性,IC50值为 25 μM。

规格价格库存数量
1 mg¥ 179现货
5 mg¥ 443现货
10 mg¥ 787现货
25 mg¥ 1,490现货
50 mg¥ 2,520现货
100 mg¥ 3,830现货
200 mg¥ 5,490期货
1 mL x 10 mM (in DMSO)¥ 443现货
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产品介绍

生物活性
产品描述
LDN-57444 is a reversible, competitive proteasome Uch-L1 inhibitor(IC50=0.88 μM) .
靶点活性
UCHL1:0.88 μM
体外活性
在体内,LDN-57444使突触蛋白分布和脊柱形态发生明显改变.LDN-57444导致UCH-L1活性下降,但对于cAMP水平的蛋白酶抑制没有效果.
体内活性
LDN-57444(25-50 μM)以剂量依赖的方式,通过细胞凋亡途径能够通过降低泛素蛋白酶体系统的活性,并增加高度泛素化蛋白的水平,降低细胞的存活率。
激酶实验
HTS screen: To start an assay, 0.5 μL of 5 mg/mL test compound (about 50 μM final reaction concentration) or DMSO control is aliquoted into each well. Both enzyme and substrate are prepared in UCH reaction buffer (50 mM Tris-HCl [pH 7.6], 0.5 mM EDTA, 5 mM DTT, and 0.5 mg/mL ovalbumin). 25 μL of 0.6 nM UCH-L1 is then added to each well except substrate control wells, followed by plate shaking for 45–60 s on an automatic shaker. The enzyme/compound mixture is incubated at room temperature for 30 min before 25 μL of 200 nM Ub-AMC is added to initiate the enzyme reaction. The reaction mixture (300 pM UCH-L1, 100 nM Ubiquitin-AMC with 2.5 μg test compound) is incubated at room temperature for 30 additional minutes prior to quenching the reaction by the addition of 10 μL 500 mM acetic acid per well. The fluorescence emission intensity is measured on a LJL Analyst using a coumarin filter set (ex = 365 nm, em = 450 nm) and is subtracted by the intrinsic compound fluorescence to reveal the enzyme activity. A DMSO control (0.5 μL of DMSO, 25 μL of UCH-L1, 25 μL of ubiquitin-AMC, 10 μL of acetic acid), enzyme control (25 μL of UCH-L1, 25 μL of buffer, 10 μL of acetic acid), substrate control (25 μL of buffer, 25 μL of ubiquitin-AMC, 10 μL of acetic acid), and inhibitor control (0.5 μL of ubiquitin aldehyde [100 nM stock], 25 μL of UCH-L1, 25 μL of ubiquitin-AMC, 10 μL of acetic acid) are also performed in each assay plate to ensure quality and reproducibility. Potential UCH-L1 inhibitors are selected if the compounds demonstrated greater than 60% inhibition compared to the controls. The UCH-L1 enzymatic reactions are manually repeated twice using the same protocol to confirm the results for the hit compounds from the primary robot-assisted screen.
细胞实验
MTT assay(Only for Reference)
别名LDN57444
化学信息
分子量397.64
分子式C17H11Cl3N2O3
CAS No.668467-91-2
SmilesCC(=O)ON=C1C(=O)N(Cc2cc(Cl)ccc2Cl)c2ccc(Cl)cc12
密度1.50 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 19.9 mg/mL (50 mM)
溶液配制表
1mg5mg10mg50mg
1 mM2.5148 mL12.5742 mL25.1484 mL125.7419 mL
5 mM0.5030 mL2.5148 mL5.0297 mL25.1484 mL
10 mM0.2515 mL1.2574 mL2.5148 mL12.5742 mL
20 mM0.1257 mL0.6287 mL1.2574 mL6.2871 mL
50 mM0.0503 mL0.2515 mL0.5030 mL2.5148 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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