Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor. In Vitro Capzimin (3027) shows 80-fold selectivity for Rpn11 over Csn5, 10-fold over AMSH and 6-fold over BRCC36 (IC 50 =30 μM, 4.5 μM and 2.3 μM respectively. Capzimin is screened against the NCI panel of 60 cancer cell lines. The median GI 50 is 3.3 μM. Capzimin exhibits promising activity in leukemia cells including the SR and K562 cell lines (GI 50 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; GI 50 = 0.7 μM) and MCF7 (breast cancer; GI 50 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:Target: Rpn11
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Capzimin
CAS number：2084868-04-0(DMSO) molecular formula：C30H24N6O2S4
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| Chinese alias | 卡普西明 | ||
| English alias | - | ||
| CAS number | 2084868-04-0(DMSO) | molecular formula | C30H24N6O2S4 |
| molecular weight | 628.81 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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