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. 2010 Oct 11;285(51):40125–40134. doi: 10.1074/jbc.M110.160606

TABLE 1.

Effect of inhibitors on the purified immunoproteasomes

26 S proteasomes, purified from rabbit spleens, were incubated with different concentrations of inhibitors for 30 min at 37 °C followed by measurements by activities as described under “Experimental Procedures.” Residual activity was plotted against concentration on semi-log plots (supplemental Fig. S1), which were used to determine IC50 values. (To allow for easy comparison with data on Fig. 2, IC50 values are provided instead of Ki and k2.)

Active sites
IC50 ratio
β5i β2i β1i β2i/β5i β1i/β5i
IC50 (μm) -fold
NC-005 0.044 4.6 10 105 225
NC-005-mvs 1.5 ∼140 ∼140 ∼93 ∼93
YU-101 0.26 1.9 4.5 7.3 17.3
YU-101-mvs 1.9 ≫100a ≫100b
PR-171 0.00028 0.62 2.42 2321 8643
PR-171-mvs 0.011 5.3 22.5 481 2045
PR-957 0.0102 1.04 6.4 102 627
PR-957-mvs 1.0 53 78 53 78

a 21 ± 1% inhibition was at 81 μm.

b 16 ± 2% inhibition was at 81 μm (values are mean ± S.E. of two independent measurements).