VR23 [Proteasome Inhibitor]

Synthetic. Chemical. CAS: 1624602-30-7. Formula: C19H16ClN5O6S. MW: 477.9. Synthetic. Potent selective and reversible chloroquine derivative 20S proteasome inhibitor (all proteolytic subunits). Targets the trypsin-like beta2 subunit of the constitutive 20S proteasome (IC50=1nM). Cross-reacts and inhibits the chymotrypsin-like beta5 subunit (IC50=50-100nM) and the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) beta1 subunit (IC50=3µM). Anticancer compound effective in cell-based assays and against multiple myeloma and metastatic breast cancer in vivo. In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, as well as in bortezomib-resistent multiple myeloma cells, but with minimal effects on non-cancerous cells.