Marizomib suppresses the CT-L (β5), CT-T-laspase-like (C-L, β1), and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively). Marizomib is a second-generation, irreversible, brain-penetrant inhibitor of pan-proteasome.

Marizomib (24 hours; 60 nM) causes apoptosis and caspase-3 activation in glioma cells. Marizomib (0.1-10000 nM; 72 hours) potently decreases survival of D-54 and U-251 cells in a dose-dependent manner (IC50s: ～52 nM for U-251 and ～20 nM for D-54)[1].

Marizomib (0.15 mg/kg; i.v; twice a week for three weeks) obviously reduces tumor growth and is not associated with any toxicity[3].

437742-34-2

C15H20ClNO4

313.78

NPI-0052;Salinosporamide A;Marizomib

DMSO:100 mg/mL (318.69 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years