Powder: -20°C for 3 years | In solvent: -80°C for 1 year
IU1 是一种可逆的特异性人类 USP14 蛋白酶体抑制剂,可以穿透细胞,IC50为 4.7 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 396 | 现货 | ||
10 mg | ¥ 537 | 现货 | ||
25 mg | ¥ 996 | 现货 | ||
50 mg | ¥ 1,837 | 现货 | ||
100 mg | ¥ 2,698 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 438 | 现货 |
产品描述 | IU1(IC50=4.7 μ M), a reversible, specific human USP14 proteasome inhibitor, can penetrate the cell. |
靶点活性 | USP14:4.7 μM |
体外活性 | IU1 binds specifically to the activated form of USP14. IU1 can potentially inhibit USP14 by preventing its docking on the proteasome, exhibiting little or no activity toward 8 other DUBs, IsoT, UCH37, BAP1, UCH-L1, UCH-L3, USP15, USP2, USP7. USP14 inhibition is rapidly established upon addition of IU1 and rapidly reversed upon its removal. IU1 inhibits USP14 induced chain trimming and decreases electrophoretic mobility of Ub-CCNB species. IU1 enhances proteasomal degradation of Ub-CCNB in the presence of USP14. IU1 promots degradation of tau and depletes TDP-43, ATXN3, and glial fibrillary acidic protein (GFAP) in proteotoxic mechanisms. [1] |
激酶实验 | High-throughput screening: Screening is conducted at the ICCB-Longwood screening facility. 10 μL of recombinant USP14 protein are dispensed into each well of a 384-well low volume plate in duplicate, using a Wellmate plate dispenser. 33.3?nL of compound from the library are pin-transferred into the wells using a Seiko pin transfer robotic system, followed by pre-incubation for about 30?min. The last two columns of each plate are used for positive and negative controls for the assay. To initiate the enzyme reaction, 10?μL of VS-proteasome plus Ub-AMC mixture are added to each well, using a Wellmate dispenser. Samples are then incubated for another 45?min. Ub-AMC hydrolysis is measured at Ex355/Em460 using an Envision plate reader. The final concentrations of USP14, VS-proteasome and Ub-AMC are 15?nM, 1?nM and 0.8 μM, respectively. The final concentration of test compound is approximately 17?μM. Enzymes and substrates are prepared in Ub-AMC assay buffer (50?mM Tris-HCl (pH?7.5), 1?mM EDTA, 1?mM ATP, 5 mM MgCl2, 1?mM DTT, and 1 mg/Ml ovalbumin). |
细胞实验 | MTT(Only for Reference) |
分子量 | 300.37 |
分子式 | C18H21FN2O |
CAS No. | 314245-33-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (100 mM)
Ethanol: 15 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 3.3292 mL | 16.6461 mL | 33.2923 mL | 83.2307 mL |
5 mM | 0.6658 mL | 3.3292 mL | 6.6585 mL | 16.6461 mL | |
10 mM | 0.3329 mL | 1.6646 mL | 3.3292 mL | 8.3231 mL | |
20 mM | 0.1665 mL | 0.8323 mL | 1.6646 mL | 4.1615 mL | |
50 mM | 0.0666 mL | 0.3329 mL | 0.6658 mL | 1.6646 mL | |
DMSO | 100 mM | 0.0333 mL | 0.1665 mL | 0.3329 mL | 0.8323 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。
IU1 314245-33-5 Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB inhibit DUBs IU 1 Inhibitor Deubiquitinase IU-1 inhibitor