Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PR-619 (2,6-Diamino-3,5-dithiocyanopyridine) 是一种 DUB 抑制剂,可诱导内质网应激和内质网应激相关的凋亡,对 USP4、USP8、USP7、USP2和 USP5的 EC50分别为 3.93、4.9、6.86、7.2 和 8.61 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 159 | 现货 | ||
5 mg | ¥ 351 | 现货 | ||
10 mg | ¥ 567 | 现货 | ||
25 mg | ¥ 883 | 现货 | ||
50 mg | ¥ 1,230 | 现货 | ||
100 mg | ¥ 1,990 | 现货 | ||
200 mg | ¥ 2,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 623 | 现货 |
产品描述 | PR-619 (2,6-Diamino-3,5-dithiocyanopyridine) is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs). |
靶点活性 | USP4:3.93 μM(EC50), JOSD2:1.17 μM(EC50), UCH-L3:2.95 μM(EC50), SENP6 core:2.37 μM(EC50), USP8:4.90 μM(EC50) |
体内活性 | PR-619以剂量和时间依赖性方式(20至150 μM,0.5至20 h)在HEK293T细胞中增加总体蛋白质多聚泛素化。PR619处理导致K48和K63连接的polyUb链上调。PR-619诱导HCT116细胞死亡,EC50为6.3 μM。 |
激酶实验 | Ub-PLA2 assay: Recombinant enzymes in 20 mM Tris-HCl, pH 8.0, 2 mM CaCl2 and 2 mM β-mercaptoethanol (DUB assay buffer) are preincubated with single doses or dose ranges of PR-619 or P22077 for 30 minutes in a 96 well plate before the addition of Ub-PLA2 and NBD C6-HPC. The liberation of a fluorescent product within the linear range of the assay is monitored at room temperature using a fluorescence plate reader. Vehicle (2%(v/v) DMSO) and 10 mM N-ethylmaleimide are included as controls. Where ≥60% inhibition is observed, EC50 values are determined using a sigmoidal dose response equation. |
细胞实验 | 72 h hours later, 0.2 mg/mL resazurin prepared in phosphate-buffered saline is added to each well and the cells are incubated for an additional 3-6 h. The fluorescence of the resazurin reduction product is measured using Ex=535 nm and Em=590 nm filters on a fluorimeter. The EC50 values are calculated in Prism.(Only for Reference) |
别名 | PR 619, 2,6-Diamino-3,5-dithiocyanopyridine |
分子量 | 223.28 |
分子式 | C7H5N5S2 |
CAS No. | 2645-32-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 201.5 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.4787 mL | 22.3934 mL | 44.7868 mL | 111.967 mL |
5 mM | 0.8957 mL | 4.4787 mL | 8.9574 mL | 22.3934 mL | |
10 mM | 0.4479 mL | 2.2393 mL | 4.4787 mL | 11.1967 mL | |
20 mM | 0.2239 mL | 1.1197 mL | 2.2393 mL | 5.5984 mL | |
50 mM | 0.0896 mL | 0.4479 mL | 0.8957 mL | 2.2393 mL | |
100 mM | 0.0448 mL | 0.2239 mL | 0.4479 mL | 1.1197 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。
PR-619 2645-32-1 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB DUBs PR619 tau G0/G1 Deubiquitinase PR 619 ER-stress 2,6-Diamino-3,5-dithiocyanopyridine ubiquitination inhibit Inhibitor arrest inhibitor