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 |