Marizomib (Salinosporamide A)

Catalog No.S7504 Batch:S750401

Technical Data

Formula

C₁₅H₂₀ClNO₄

Molecular Weight

313.78

CAS No.

437742-34-2

Solubility (25°C)*

In vitro

DMSO

63 mg/mL (200.77 mM)

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

5.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Marizomib (Salinosporamide A) is a novel marine derived proteasome inhibitor which inhibits CT-L β5, C-L β1, and T-L β2 proteasome activities in human erythrocyte-derived 20S proteasomes with IC50 of 3.5 nM, 430 nM, 28 nM.

Targets

CT-L β5 ^[2] (Cell-free assay)	T-L β2 ^[2] (Cell-free assay)	C-L β1 ^[2] (Cell-free assay)
3.5 nM	28 nM	430 nM

In vitro

Marizomib inhibits the proteasome activity, proliferation, and invasion of glioma cells. Meanwhile, free radical production and apoptosis induced by marizomib can be blocked by antioxidant N-acetyl cysteine.^[1]

In vivo

In animal studies, marizomib distributes into the brain at 30% of blood levels in rats and significantly inhibits (>30%) baseline chymotrypsin-like proteasome activity in brain tissue of monkeys. Encouragingly, the immunocompromised mice, intracranially implanted with glioma xenografts, survives significantly longer than the control animals when treated with marizomib.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines The human glioma cell lines U-251 MG and D-54 MG Concentrations 60 nM Incubation Time 2 h, 24 h Method Proteasome activity is measured in neural stem cells and glioblastoma-derived glioma stem cells at baseline and 2 hours after treatment with marizomib (60 nM). Invasion capability of U-251 MG and D-54 MG cells treated or untreated with 60 nM marizomib for 24 hours is analyzed using Matrigel invasion chambers.
Animal Study:^{^[1]}	Animal Models male Sprague-Dawley rats, 6–8 week old mice Dosages 0.1 mg/kg, 200 µg/kg Administration IV

Cell Assay:^{^[1]}

Cell lines
The human glioma cell lines U-251 MG and D-54 MG
Concentrations
60 nM
Incubation Time
2 h, 24 h
Method
Proteasome activity is measured in neural stem cells and glioblastoma-derived glioma stem cells at baseline and 2 hours after treatment with marizomib (60 nM). Invasion capability of U-251 MG and D-54 MG cells treated or untreated with 60 nM marizomib for 24 hours is analyzed using Matrigel invasion chambers.

Animal Study:^{^[1]}

Animal Models
male Sprague-Dawley rats, 6–8 week old mice
Dosages
0.1 mg/kg, 200 µg/kg
Administration
IV

References

Selleck's Marizomib (Salinosporamide A) has been cited by 6 publications

Targeting mitochondrial energetics reverses panobinostat- and marizomib-induced resistance in pediatric and adult high-grade gliomas [ Mol Oncol, 2023, 17(9):1821-1843]	PubMed: 37014128
Targeting mitochondrial energetics reverses panobinostat- and marizomib-induced resistance in pediatric and adult high-grade gliomas [ Mol Oncol, 2023, 17(9):1821-1843]	PubMed: 37014128
Proteasome inhibition as a therapeutic target for the fungal pathogen Cryptococcus neoformans [ Microbiol Spectr, 2023, 11(5):e0190423]	PubMed: 37750732
Proteasome inhibition as a therapeutic target for the fungal pathogen Cryptococcus neoformans [ Microbiol Spectr, 2023, 10.1128/spectrum.01904-23]	PubMed: 37750732
Collateral deletion of the mitochondrial AAA+ ATPase ATAD1 sensitizes cancer cells to proteasome dysfunction [ Elife, 2022, 11e82860]	PubMed: 36409067
Targeting NAD+ Biosynthesis Overcomes Panobinostat and Bortezomib-Induced Malignant Glioma Resistance [ Mol Cancer Res, 2020, 18(7):1004-1017]	PubMed: 32238439

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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