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General description
A cell-permeable pyrrolylpyrrolidinyl-ethanone that inhibits the proteasome association-dependent USP14 deubiquitinase (DUB) activity in a reversible manner (IC50 = 4.7 µM against Ub-AMC hydrolysis), exhibiting little or no activity toward 8 other DUBs. Shown to downregulate tau, TDP-43, ATXN3, GFAP, and free Ub levels in MEF cultures in a dose- (25 to 100 µM), time-, and USP14-dependent manner. USP14-catalyzed trimming of protein surface polyubiquitin chains rescues proteasome-bound proteins from proteolytic degradation and thereby prevents the depletion of free ubiquitin pool in cells. Comparing to b-AP15 (Cat. No. 662140), IU1 does not inhibit UCH37/UCH-L5 (IC50 = 700 µM).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Lee, B.H., et al. 2010. Nature467, 179.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
| Quality Segment | 100 |
| assay | ≥90% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | beige |
| solubility | DMSO: 50 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | Fc1ccc(cc1)[n]2c(c(cc2C)C(=O)CN3CCCC3)C |
| InChI | 1S/C18H21FN2O/c1-13-11-17(18(22)12-20-9-3-4-10-20)14(2)21(13)16-7-5-15(19)6-8-16/h5-8,11H,3-4,9-10,12H2,1-2H3 |
| InChI key | JUWDSDKJBMFLHE-UHFFFAOYSA-N |
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瓶顶过滤器-500ml容量,MF75TM系列，聚苯乙烯外壳，75mmSFCA滤膜，孔径0.2um,适合瓶颈尺寸45mm，12/箱，291-4520，Nalgene，Thermofisher，赛默飞世尔¥ 2856.42
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