Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 246 | 现货 | ||
5 mg | ¥ 443 | 现货 | ||
10 mg | ¥ 788 | 现货 | ||
25 mg | ¥ 1,490 | 现货 | ||
50 mg | ¥ 2,660 | 现货 | ||
100 mg | ¥ 3,830 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 443 | 现货 |
产品描述 | LDN-57444 is a reversible, competitive proteasome Uch-L1 inhibitor(IC50=0.88 μM) . |
靶点活性 | UCH-L1:0.88 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 |
分子量 | 397.64 |
分子式 | C17H11Cl3N2O3 |
CAS No. | 668467-91-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 19.9 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5148 mL | 12.5742 mL | 25.1484 mL | 62.8709 mL |
5 mM | 0.503 mL | 2.5148 mL | 5.0297 mL | 12.5742 mL | |
10 mM | 0.2515 mL | 1.2574 mL | 2.5148 mL | 6.2871 mL | |
20 mM | 0.1257 mL | 0.6287 mL | 1.2574 mL | 3.1435 mL | |
50 mM | 0.0503 mL | 0.2515 mL | 0.503 mL | 1.2574 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
LDN-57444 668467-91-2 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB Inhibitor inhibit Deubiquitinase LDN 57444 LDN57444 DUBs inhibitor