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Marizomib (Salinosporamide A) Proteasome inhibitor

Name: Marizomib (Salinosporamide A)
Brand: Selleck Chemicals
SKU: S7504
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S7504

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.

Chemical Structure

Molecular Weight: 313.78

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
HPLC
SDS
Datasheet

99.88

Related Targets	HDAC Caspase Secretase MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease Serine Protease
Other Proteasome Products	MG132 Epoxomicin (BU-4061T) Celastrol Oprozomib ONX-0914 (PR-957) Delanzomib VR23 PI-1840 Isoginkgetin S5a/PSMD4 Antibody [L2F5]

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (200.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (15.93mM)	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.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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

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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.

Chemical Information, Storage & Stability

Molecular Weight	313.78	Formula	C₁₅H₂₀ClNO₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	437742-34-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ML858, MRZ, NPI-0052			Smiles	CC12C(C(=O)NC1(C(=O)O2)C(C3CCCC=C3)O)CCCl

Mechanism of Action

Targets/IC₅₀/Ki	CT-L β5 (Cell-free assay) 3.5 nM T-L β2 (Cell-free assay) 28 nM C-L β1 (Cell-free assay) 430 nM
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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26681765/ [2] https://pubmed.ncbi.nlm.nih.gov/22978849/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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