tcsc0042403 Capzimin

Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.

IC50 & Target: Target: Rpn11^[1]

In Vitro: Capzimin (3027) shows 80-fold selectivity for Rpn11 over Csn5, 10-fold over AMSH and 6-fold over BRCC36 (IC₅₀=30 μM, 4.5 μM and 2.3 μM respectively. Capzimin is screened against the NCI panel of 60 cancer cell lines. The median GI₅₀ is 3.3 μM. Capzimin exhibits promising activity in leukemia cells including the SR and K562 cell lines (GI₅₀ values of 0.67 μM and 1 μM respectively), as well as several solid tumor cell lines including NCI-H460 (non-small cell lung cancer; GI₅₀= 0.7 μM) and MCF7 (breast cancer; GI₅₀=1.0 μM). Immunoblotting for the processed form of caspase 3 and caspase-cleaved poly ADP-ribose polymerase in HCT116 cells confirm that Capzimin not only blocks cell growth, but also induces apoptosis^[1].