Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PYR-41 是一种选择性,可透过细胞的泛素活化酶 E1抑制剂,IC50值小于10 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 288 | 现货 | ||
5 mg | ¥ 496 | 现货 | ||
10 mg | ¥ 828 | 现货 | ||
25 mg | ¥ 1,460 | 现货 | ||
50 mg | ¥ 2,370 | 现货 | ||
100 mg | ¥ 3,530 | 现货 | ||
200 mg | ¥ 5,120 | 现货 | ||
500 mg | ¥ 7,830 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 552 | 现货 |
产品描述 | PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2. |
靶点活性 | E1:< 10 μM |
体外活性 | PYR-41 (50 μM) inhibits activity of ubiquitin-activating enzyme E1 by over 90%. PYR-41 could be a target for nucleophilic attack and potentially reacts with the active site cysteine of E1. PYR-41 efficiently blocks cyclin E degradation. PYR-41 decreases the level of E1fUb thioesters in cells with a IC50 of between 10 and 25 μM, and prevents proteasome inhibitor–induced accumulation of ubiquitylated proteins. PYR-41 increases total sumoylation in cells and in cell harboring temperature-sensitive E1. PYR-41 is able to inhibit both proteasome-dependent and proteasome-independent activities of ubiquitylation. PYR-41 (50 μM) attenuates 1 ng/mL IL-1α-mediated nuclear factor-κB activation by >60% through preventing the downstream ubiquitylation and proteasomal degradation of IκBα. PYR-41 inhibits degradation of p53 and activates the transcriptional activity of p53, which enable its differentially killing transformed p53-expressing cells. [1] PYR-41 blocks ubiquitination reactions but paradoxically leads to the accumulation of high MW ubiquitinated proteins. PYR-41 also has equal or greater inhibitory activity against several deubiquitinases (DUBs) in intact cells and purified USP5 in vitro. PYR-41 also mediates cross-linking of specific protein kinases (Bcr-Abl, Jak2) to inhibit their signaling activity. [1] |
激酶实验 | Rabbit or mouse E1 (apper 250 ng) is incubated with 32P-ubiquitin in 1× reaction buffer [50 mM Tris (pH 7.4), 0.2 mM ATP, 0.5 mM MgCl2] at room temperature for 15 min. In some experiments, the His-tagged mouse E1 is bound to TALON cobalt affinity resin before carrying out incubations and reactions. Mouse E1 and 32P-ubiquitin are added to the beads in 1× reaction buffer and incubated as for E1 reactions. Samples are heated in nonreducing SDS-PAGE sample buffer and resolved by SDS-PAGE. Thioesters with ubiquitin are visualized by Storm PhosphoImager. |
别名 | PYR41, PYR 41 |
分子量 | 371.3 |
分子式 | C17H13N3O7 |
CAS No. | 418805-02-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 37.1 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6932 mL | 13.4662 mL | 26.9324 mL | 67.331 mL |
5 mM | 0.5386 mL | 2.6932 mL | 5.3865 mL | 13.4662 mL | |
10 mM | 0.2693 mL | 1.3466 mL | 2.6932 mL | 6.7331 mL | |
20 mM | 0.1347 mL | 0.6733 mL | 1.3466 mL | 3.3665 mL | |
50 mM | 0.0539 mL | 0.2693 mL | 0.5386 mL | 1.3466 mL | |
100 mM | 0.0269 mL | 0.1347 mL | 0.2693 mL | 0.6733 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。
PYR-41 418805-02-4 Apoptosis Ubiquitination E1/E2/E3 Enzyme E3 ligating enzyme PYR41 E1 activating enzyme PYR 41 Inhibitor Ubiquitin conjugating enzyme E2 conjugating enzyme Ubiquitin activating enzyme Ubiquitin ligase inhibit inhibitor