1. Metabolic Enzyme/Protease
  2. Proteasome
  3. Marizomib

Marizomib (Synonyms: Salinosporamide A; NPI-0052)

Cat. No.: HY-10985
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Marizomib (Salinosporamide A) is second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits 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).

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Marizomib Chemical Structure

Marizomib Chemical Structure

CAS No. : 437742-34-2

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Description

Marizomib (Salinosporamide A) is second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits 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)[1][2][3].

IC50 & Target

IC50: 3.5 nM (CT-L), 28 nM (CT-T-laspase-like), 430 nM (trypsin-like)[1]

In Vitro

Marizomib (Salinosporamide A) (0.1-10000 nM; 72 hours) effectively reduces survival of D-54 and U-251 cells in a dose-dependent manner. The IC50s are ∼52 nM for U-251 and ∼20 nM for D-54[1].
Marizomib (24 hours; 60 nM) induces apoptosis and caspase-3 activation in glioma cells[1].

Cell Proliferation Assay[1]

Cell Line: U-251 and D-54 cells
Concentration: 0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time: 72 hours
Result: Effectively reduced survival of D-54 and U-251 cells in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: D-54 cells
Concentration: 60 nM
Incubation Time: 24 hours
Result: Induces D-54 cells apoptosis.

Western Blot Analysis[1]

Cell Line: D-54 cells
Concentration: 60 nM
Incubation Time: 24 hours
Result: Led to increased activity of caspase-3 in a dose-dependent manner.
In Vivo

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

Animal Model: CB-17 SCID-male mice (4-6 weeks old)[3]
Dosage: 0.15 mg/kg
Administration: i.v; twice a week for three weeks
Result: Significantly decreased tumor growth, and was not associated with any toxicity.
Molecular Weight

313.78

Formula

C₁₅H₂₀ClNO₄

CAS No.

437742-34-2

SMILES
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Keywords:

MarizomibSalinosporamide ANPI-0052NPI0052NPI 0052Proteasomeirreversiblebrain-penetrantpanglioblastomablood-brainbarriercaspasesantitumorInhibitorinhibitorinhibit

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