IU1 - Deubiquitinase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIU1Cat. No.: HY-13817CAS No.: 314245-33-5分式: CHFNO分量: 300.37作靶点: Deubiquitinase; Autophagy作通路: Cell Cycle/DNA Damage; Autophagy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 : 60 mg/mL (199.

2、75 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.3292 mL 16.6461 mL 33.2923 mL5 mM 0.6658 mL 3.3292 mL 6.6585 mL10 mM 0.3329 mL 1.6646 mL 3.3292 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，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠

3、性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；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 (5.56 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 (5.56 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn

4、 oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 1.67 mg/mL (5.56 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 IU1种特异性的 Usp14 抑制剂，IC50 为 4-5 M。IC50 & Target IC50: 4-5 M (Usp14) 1体外研究 Usp14, a proteasome-associated deubiquitinating enzyme, can inhibit the degradation of ubiquitin-protein

5、conjugates, in vivo and in vitro. IU1inhibits the catalytic activity of proteasome associated Usp14 in vitro. TheIC50 of IU1 for Usp14 is 4-5 M. IU1 binds specifically to the activated form of Usp14. IU1 can potentiallyinhibit Usp14 by preventing its docking on the proteasome, but direct tests of th

6、is scenario proved negative.Usp14 inhibition is rapidly established upon addition of IU1 and rapidly reversed upon its removal. IU1 alsopromotes degradation of Sic1, a CDK inhibitor from S. cerevisiae 1.REFERENCES1. Lee BH, et al. Enhancement of proteasome activity by a small-molecule inhibitor of USP14. Nature. 2010 Sep 9;467(7312):179-84.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: