Products/Services Used | Details | Operation |
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Proteins, Expression, Isolation and Analysis | … Micro Beads and the Auto MACS magnetic cell sorter (Miltenyi Biotech, Bergisch Gladbach, Germany) … panel assay (GenScript, Nanjing, China) as previously described [32] … 551024, BD Bioscience Pharmingen, San Diego, CA, USA), p53 (sc-47698, Santa Cruz Biotechnology … | Get A Quote |
A series of novel dipeptidyl boronic acid inhibitors of 20S proteasome were designed and synthesized. Aliphatic groups at R position were designed for the first time to fully understand the SAR (structure-activity relationship). Among the screened compounds, novel inhibitor 5c inhibited the CT-L (chymotrypsin-like) activity with IC of 8.21 nM and the MM (multiple myeloma) cells RPMI8226, U266B and ARH77 proliferations with the IC of 8.99, 6.75 and 9.10 nM, respectively, which showed similar in vitro activities compared with the compound MLN2238 (biologically active form of marketed MLN9708). To investigate the oral availability, compound 5c was esterified to its prodrug 6a with the enzymatic IC of 6.74 nM... More