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IU1

IU1

产品编号 T6107   CAS 314245-33-5

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。

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IU1 Chemical Structure
IU1, CAS 314245-33-5
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
产品目录号及名称: IU1 (T6107)
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纯度: 99.11%
纯度: 98.77%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 30 mg/mL (100 mM)

Ethanol: 15 mg/mL (50 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Byung-Hoon L, et al. Nature, 2010, 467(7312), 179-184.

文献引用

1. Wu W, Xu H, Liao C, et al. Blockade of USP14 potentiates type I interferon signaling and radiation-induced antitumor immunity via preventing IRF3 deubiquitination. Cellular Oncology. 2022: 1-15 2. Yue X, Liu T, Wang X, et al.Pharmacological inhibition of BAP1 recruits HERC2 to competitively dissociate BRCA1–BARD1, suppresses DNA repair and sensitizes CRC to radiotherapy.Acta Pharmaceutica Sinica B.2023
GNE-6776 XL177A IU1-248 USP7-IN-6 LDN-91946 DUB-IN-2 OTUB1/USP8-IN-1 HCl KSQ-4279

相关化合物库

该产品包含在如下化合物库中:
泛素化化合物库 抑制剂库 含氟化合物库 DNA 损伤和修复分子库 抗衰老化合物库 自噬库 HIF-1化合物库 抗癌化合物库 细胞周期化合物库 经典已知活性库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

IU1 314245-33-5 Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB inhibit DUBs IU 1 Inhibitor Deubiquitinase IU-1 inhibitor

 

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