购物车
- 全部删除
- 您的购物车当前为空
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。
为众多的药物研发团队赋能,
让新药发现更简单!
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 |
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 |
分子量 | 397.64 |
分子式 | C17H11Cl3N2O3 |
CAS No. | 668467-91-2 |
Smiles | CC(=O)ON=C1C(=O)N(Cc2cc(Cl)ccc2Cl)c2ccc(Cl)cc12 |
密度 | 1.50 g/cm3 (Predicted) |
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 | |||||||||||||||||||||||||||||||
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.
评论内容