Home Proteases Proteasome inhibitor Marizomib (Salinosporamide A)

research use only

Marizomib (Salinosporamide A) Proteasome inhibitor

Marizomib (Salinosporamide A) is a novel marine derived proteasome inhibitor. It 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.

Marizomib (Salinosporamide A) Proteasome inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 313.78

Purity & Quality Control

Batch: S750401 DMSO]63 mg/mL]false]]]false]]]false Purity: 99.88%
99.88

Related Products

Signaling Pathway

Proteasome Signaling Pathways

Proteasome Signaling Pathway

Cell Culture and Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI 8226 Cytotoxicity assay Cytotoxic activity against RPMI 8226 cells, IC50 = 0.0082 μM. 15916417
NCI60 Cytotoxicity assay Cytotoxicity against human NCI60 cells, GI50 = 0.01 μM. 19022674
HEK293 Function assay Inhibition of NF-kB activation in HEK293 cells, IC50 = 0.011 μM. 15916417
RPMI8226 Cytotoxicity assay 48 hrs Cytotoxicity against human RPMI8226 cells after 48 hrs by resazurin assay, IC50 = 0.011 μM. 19133779
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTS/PMS assay, IC50 = 0.016 μM. 19746976
HCT116 Cytotoxicity assay Cytotoxicity against human HCT116 cells, IC50 = 0.035 μM. 21835627
Click to View More Cell Line Experimental Data

Mechanism of Action

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
In vitro

Marizomib (Salinosporamide A) inhibits the proteasome activity, proliferation, and invasion of glioma cells. Meanwhile, free radical production and apoptosis induced by this compound can be blocked by antioxidant N-acetyl cysteine.[1]
Cell Research 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 (Salinosporamide A) (60 nM). Invasion capability of U-251 MG and D-54 MG cells treated or untreated with 60 nM of this compound for 24 hours is analyzed using Matrigel invasion chambers.

In Vivo
In vivo

In animal studies, marizomib (Salinosporamide A) 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 this compound.[1]
Animal Research Animal Models male Sprague-Dawley rats, 6–8 week old mice
Dosages 0.1 mg/kg, 200 µg/kg
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04341311 Terminated
Diffuse Intrinsic Pontine Glioma|Pediatric Brainstem Glioma|Pediatric Brainstem Gliosarcoma Recurrent|Pediatric Cancer|Pediatric Brain Tumor|Diffuse Glioma
Dana-Farber Cancer Institute|Celgene|Secura Bio Inc.
 August 10 2020 Phase 1
NCT03727841 Terminated
Anaplastic Ependymoma|Ependymoma|Ependymomas
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 January 22 2020 Phase 2
NCT02903069 Completed
Glioblastoma|Malignant Glioma
Celgene|Triphase
 August 17 2016 Phase 1
NCT01501396 Withdrawn
Anorexia
Washington University School of Medicine
 September 2013 Phase 2
NCT00667082 Completed
Non-Small Cell Lung Cancer|Pancreatic Cancer|Melanoma|Lymphoma|Multiple Myeloma
Celgene
 March 2008 Phase 1

References
  • https://pubmed.ncbi.nlm.nih.gov/26681765/
  • https://pubmed.ncbi.nlm.nih.gov/22978849/

Chemical Information

Molecular Weight 313.78 Formula

C15H20ClNO4
CAS No. 437742-34-2 SDF --
Synonyms ML858, MRZ, NPI-0052
Smiles CC12C(C(=O)NC1(C(=O)O2)C(C3CCCC=C3)O)CCCl

Storage and Stability

Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 63 mg/mL ( (200.77 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.