Marizomib

SKU: orb1707013

Description

Marizomib is a brain-penetrant, irreversible proteasome inhibitor that potently targets the β5 (IC50=3.5 nM), β1 (28 nM), and β2 (430 nM) subunits of the 20S proteasome. It is widely used in preclinical research, including in vitro cell studies and in vivo models, for investigating cancer, neurodegenerative diseases, and proteasome biology.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 437742-34-2
• MW: 313.78
• Purity: 99.41% (May vary between batches)
• Formula: C₁₅H₂₀ClNO₄
• SMILES: [C@@H](O)([C@]12[C@](C)([C@@H](CCCl)C(=O)N1)OC2=O)[C@]3(CCCC=C3)[H]
• Target: Proteasome
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.37 mM);DMSO:31.38 mg/mL (100.01 mM)

Bioactivity

• Target IC50:
  Trypsin like:430 nM|CTL:3.5 nM|CTL laspase-like:28 nM
• In Vivo:
  METHODS: After two weeks of Marizomib (0.15 mg/kg twice/week, IP) treatment of MDA-MB-231 xenografts and patient-derived tumor xenografts (PDX), it was observed whether tumor growth was inhibited in vivo. RESULTS Marizomib treatment significantly reduced tumor volume and tumor weight in MDA-MB-231 xenografts and patient-derived tumor xenografts (PDX).
  Read more...
• In Vitro:
  METHODS: TNBC (basal), ductal and non-malignant breast epithelial cells were treated with Marizomib (0-500 nM) and cell proliferation was analyzed using the MTS assay after 6 days. RESULTS Marizomib selectively reduced TNBC cell proliferation in a concentration-dependent manner without much effect on non-TNBC and non-malignant mammary epithelial cells (MCF10A and D492), with IC50 values of Marizomib less than 150 nM in TNBC cell lines and greater than 1 µM in non-TNBC cell lines. METHODS: SUM159PT cells were treated with 100 nM Marizomib for 0 and 9 hours (prior to induction of apoptosis) and label-free global proteomics analysis was performed to identify proteins or pathways altered by Marizomib. RESULTS A total of 2547 proteins were identified, of which 425 proteins were downregulated (log2 ≤ 0.6) and 293 proteins were upregulated (log2 ≥ 0.6).Marizomib decreased the levels of 11 proteasome subunits, and 5 proteasome subunits (PSMA5, PSMC2, PSMD2, PSMA1, PSMA7 and PSMA8) were also observed to be Up-regulation. METHODS: Cells were treated with 40 nM or 80 nM marizomib for 4 h. CT-L activity of proteasome in total cell lysates was determined by lysing Suc-LLVY-AMC. RESULTS marizomib effectively inhibited proteasomes in both responsive and non-responsive cells.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Salinosporamide A, trypsin-like, CT-T-laspase-like, CT-L, 20S proteasome, Marizomib, NPI 0052, NPI0052, NPI-0052, ML858, ML-858, ML 858

Compound Identifiers

PubChem CID

11347535