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Soluble in DMSO (10mg/ml) or DMF. Poorly soluble in aqueous solutions.
Identity
Determined by 1H-NMR.
Other Product Data
Note: Warming and sonication may be required when dissolving the compound in the solvent of choice. Stock solutions are stable for at least 1 month when stored at -20°C.
Targets the trypsin-like β2 subunit of the constitutive 20S proteasome (IC50=1nM). Cross-reacts and inhibits the chymotrypsin-like β5 subunit (IC50=50-100nM) and the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) β1 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.
Product References
VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification: S. Pundir, et al.; Cancer Res. 75, 4164 (2015)