Capzimin is an effective and moderately specific inhibitor of proteasome isopeptidase Rpn11.

Capzimin 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). Capzimin is screened against the NCI panel of 60 cancer cell lines (median GI50: 3.3 μM). Capzimin exhibits promising activity in leukemia cells including the SR and K562 cell lines (GI50s: 0.67 μM and 1 μM), 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.

2084868-04-0

C30H24N6O2S4

628.81

Capzimin

DMSO:55.67 mg/mL (88.53 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years