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. 2010 Aug 27;430(Pt 3):461–476. doi: 10.1042/BJ20100383

Table 3. Proteasome inhibition in B-cell lymphoma subtypes expressing differing levels of immunoproteasome by β5i- and β5c-selective compounds 5 and 14 respectively compared with bortezomib.

Inhibition of the β5 sites of the constitutive and immunoproteasome was assessed in the indicated B-cell lymphoma lines (20000 cells per well) in situ using the Proteasome-Glo™ assay. Cells were incubated with compound for 1 h and assays were performed with the chymotrypsin-like substrate Suc-LLVY-aminoluciferin as described in the Experimental section. The results are the means±S.E.M. for triplicate determinations.

Proteasome-Glo™ β5 IC50 (nM)
Compound OCI-Ly10 WSU-DLCL2 Karpas-1106P
5 1300±400 320±120 310±150
14 39±7.6 190±76 850±240
Bortezomib 2.9±0.25 2.7±0.26 3.3±0.40