Molecular Formula | C18H21FN2O |
Molar Mass | 300.37 |
Density | 1.16±0.1 g/cm3(Predicted) |
Boling Point | 437.0±45.0 °C(Predicted) |
Solubility | DMSO: >10mg/mL |
Appearance | powder |
Color | off-white to light brown |
pKa | 8.20±0.20(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month. |
In vitro study | IU1 specifically binds to the active form of usp14. IU1 inhibits USP14 by inhibiting its docking to the proteasome, whereas it inhibits the binding of USP14 to 8 other DUBs, IsoT, UCH37, BAP1, UCH-L1, UCH-L3, USP15, USP2, USP7 had little or no inhibitory activity. USP14 was rapidly inhibited by the addition of IU1 and the inhibition was rapidly reversed after removal. IU1 inhibits usp14-induced chain modification and reduces the electrophoretic mobility of types by Ub-CCNB. IU1 enhances Ub-CCNB degradation of the proteasome in the presence of usp14. In the study of protein toxicity mechanism, IU1 promotes the degeneration of tau and reduces by TDP-43, ATXN3, and glial fibrillary acidic protein (GFAP). |
Hazard Symbols | Xi - Irritant |
Risk Codes | 41 - Risk of serious damage to eyes |
Safety Description | 61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.329 ml | 16.646 ml | 33.292 ml |
5 mM | 0.666 ml | 3.329 ml | 6.658 ml |
10 mM | 0.333 ml | 1.665 ml | 3.329 ml |
5 mM | 0.067 ml | 0.333 ml | 0.666 ml |
biological activity | IU1 is a cell-permeable, reversible proteasome (proteasome) selective inhibitor. when acting on USP14, IC50 is 4.7 μM, and the selectivity when acting on IsoT is 25 times higher. IU1 can induce autophagy. |
target | TargetValue USP14 (cell-free say) 4.7 μM |
Target | Value |
USP14 (cell-free assay) | 4.7 μM |
in vitro study | IU1 specifically binds to the active form of USP14. IU1 inhibits USP14 by inhibiting its attachment to the proteasome, while 8 other DUBs, IsoT, UCH37, BAP1, UCH-L1, UCH-L3, USP15, USP2, USP7 have little or no inhibitory activity. IU1 was added to quickly inhibit USP14. After removal, the inhibition was quickly reversed. IU1 inhibits USP14-induced chain modification and reduces electrophoretic mobility of Ub-CCNB types. In the presence of USP14, IU1 enhances the Ub-CCNB degradation of the proteasome. In the study of protein toxicity mechanism, IU1 promotes the degradation of tau and reduces TDP-43, ATXN3, and glial fibrillary acidic protein (GFAP). |