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- CAS号：
668467-91-2
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥159.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥354.0 |
| 规格： | 5mg | 产品价格： | ￥354.0 |
| 规格： | 10mg | 产品价格： | ￥629.0 |
| 规格： | 25mg | 产品价格： | ￥1192.0 |
| 规格： | 50mg | 产品价格： | ￥2016.0 |
| 规格： | 100mg | 产品价格： | ￥3064.0 |
| 规格： | 200mg | 产品价格： | ￥4392.0 |
Product Introduction
Bioactivity
| 名称 | LDN-57444 |
| 描述 | LDN-57444 is a reversible, competitive proteasome Uch-L1 inhibitor(IC50=0.88 μM) . |
| 细胞实验 | MTT assay(Only for Reference) |
| 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. |
| 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。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Corn Oil : 1.5 mg/mL (3.77 mM), Sonication is recommended. DMSO : 19.9 mg/mL (50.05 mM), Sonication is recommended. |
| 关键字 | UCH-L3 | UCH-L1 | LDN-57444 | LDN 57444 | Inhibitor | inhibit | DUBs | Deubiquitinase | Apoptosis |
| 相关产品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Apoptosis Compound Library | Anti-Aging Compound Library | HIF-1 Signaling Pathway Compound Library | NO PAINS Compound Library | Ubiquitination Compound Library | DNA Damage & Repair Compound Library | Endoplasmic Reticulum Stress Compound Library |
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相关实验
网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 LDN-57444【668467-91-2】
￥159 - 4392
