Table 3.
Inhibitors of non-20S UPS components.
| Name | Target | IC50/Kd | Mechanism |
|---|---|---|---|
| Capzimin | Rpn11 | 0.3 µM (In vitro Rpn11 assay); 0.6 µM (UbG76V-GFP degradation assay in cells) |
Chelating the zinc ion in Rpn11, inactivating its DUB activity [40] |
| Ubistatin B | polyUb | 10 µM (CFTR ubiquitination assay in cells) |
Binding to the polyUb chain and blocking the substrate/Ub receptor interaction [151,152] |
| RA190 | Rpn13 | Not Applicable | Covalently binding to cysteine residue 88 (Cys88) of Rpn13 when it is not bound to the proteasome and Uch37 at the proteasome [158,159,160] |
| RA183 | |||
| KDT-11 | Rpn13 | 1.7 µM (Kd) | Peptoid ligand binding to Rpn13 [161] |
| RIP-1 | Rpt4 | 3.0 µM (proteasome-mediated stripping of the Gal4-VP16 protein from DNA in vitro) |
Inhibiting the protein unfolding activity of the 19S RP [167,168] |