IU1-47 - USP14 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIU1-47Cat. No.: HY-122243CAS No.: 670270-31-2分式: CHClNO分量: 330.85作靶点: Deubiquitinase作通路: Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 16.67 mg/mL (50.39 mM; Need ult

2、rasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.0225 mL 15.1126 mL 30.2252 mL5 mM 0.6045 mL 3.0225 mL 6.0450 mL10 mM 0.3023 mL 1.5113 mL 3.0225 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保

3、存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1.67 mg/mL (5.05 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1.67 mg/mL (5.05 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 1.67 mg/mL (5.05 mM); C

4、lear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 IU1-47种有效的特异性 USP14 抑制剂，IC50 为 0.6 M。IU1-47 抑制 IsoT/USP5， IC50 为 20 M。IU1-47 在培养的神经元中诱导 tau 蛋降解 1。IC50 & Target IC50: 0.6 M (USP14), 20 M (IsoT/USP5) 1体外研究 IU1-47 is essentially inactive on free USP14 (USP14 that is

5、 not bound to the proteasome). IU1-47 (25 M)antagonizes USP14 deubiquitinating activity and stimulates substrate degradation in vitro 1.IU1-47 stimulates tau degradation principally via the ubiquitin-proteasome system. IU1-47 (3 M, 10 and 30 M; 48 hours) significantly decreases Tau and phosphotau sp

6、ecies Ser-202/Thr-205 levels in murine corticalprimary neurons. The level of USP14 itself does not change 1.Western Blot Analysis 1Cell Line: Murine cortical primary neurons (DIV5) isolated from APPSwe/P301L transgenic animalsConcentration: 3 M, 10 and 30 MIncubation Time: 48 hoursResult: Significan

7、tly decreased Tau and phosphotau species Ser-202/Thr-205 levels.No change in USP14 protein level.REFERENCES1. Boselli M, et al. An inhibitor of the proteasomal deubiquitinating enzyme USP14 induces tau elimination in cultured neurons. J BiolChem. 2017 Nov 24;292(47):19209-19225.McePdfHeightCaution: Product has not been fully validated for medical applications.For research us