In vitro
As a small, cell-permeable dipeptidylboronic acid derivative, bortezomib (Velcade, MG-341, PS-341) can reversibly inhibits the chymotrypsin-like activity of the proteasome by binding tightly to the active sites of the enzyme with Ki of 0.6 nM. PS-341 Induces Apoptosis and IkappaBalpha Degradation and Inhibits p44/42 MAPK Activation in MM Cells. In the NCI-60 cell lines, bortezomib showed growth inhibitory and cytotoxic activity for many human tumor cell types, with an average GI 50 of 3.8 nM across the 60 cell lines. Bortezomib (Velcade, MG-341, PS-341) showed inhibition in multiple myeloma. PS-341 can inhibit U266, IM-9, and Hs Sultan cells with IC50 of 3 mM, 6 mM and 20 nM.
Download Datasheet