Extended Data Table 2.
Enzyme inhibition IC50 values of bortezomib and GNF6702 on three proteolytic activities of wild type T. cruzi, PSMB4I29M T. cruzi, and H. sapiens proteasomes
| GNF6702 IC50 [μM]* | bortezomib IC50 [μM]* | ||
|---|---|---|---|
| wild type T. cruzi proteasome | chymotrypsin | 0.035 ± 0.0013 | 0.091 ± 0.0075 |
| caspase | >10 | 0.37 ± 0.012 | |
| trypsin | >10 | 1.7 ± 0.088 | |
| PSMB4I29M T. cruzi proteasome | chymotrypsin | >10 | 0.26 ± 0.040 |
| caspase | >10 | 0.54 ± 0.012 | |
| trypsin | >10 | 1.6 ± 0.058 | |
| H. sapiens constitutive proteasome | chymotrypsin | >10 | 0.030 ± 0.0070 |
| caspase | >10 | 0.16 ± 0.007 | |
| trypsin | >10 | 7.9 ± 0.15 |
*
mean ± s.e.m.; n= 3 technical replicates