Salinosporamide A (NPI-0052)

For research use only.

Catalog No.S7504 Synonyms: ML858, Marizomib, MRZ

1 publication

Salinosporamide A (NPI-0052) Chemical Structure

CAS No. 437742-34-2

Salinosporamide A (NPI-0052, ML858, Marizomib, MRZ) 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.

Selleck's Salinosporamide A (NPI-0052) has been cited by 1 publication

Purity & Quality Control

Choose Selective Proteasome Inhibitors

Biological Activity

Description Salinosporamide A (NPI-0052, ML858, Marizomib, MRZ) 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI 8226 Mk\KR5l1d3SxeHnjbZR6KGG|c3H5 M2jtVGN6fG:2b4jpZ{Bi[3Srdnn0fUBi\2GrboP0JHJRVUliOEKyOkBk\WyuczygTWM2OCB;IECuNFA5OiEQvF2u NYXBe4tURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW5NVY1OTdpPkG1PVE3PDF5PD;hQi=>
NCI60 MYDDfZRwfG:6aXPpeJkh[XO|YYm= NIjFOVBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0l4MDDj[YxteyxiR1m1NEA:KDBwMEGg{txONg>? MlvZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlyMkK2O|QoRjF7MEKyOlc1RC:jPh?=
HEK293 M{T4RWZ2dmO2aX;uJIF{e2G7 MoPoTY5pcWKrdHnvckBw\iCQRj3rRkBi[3SrdnH0bY9vKGmwIFjFT|I6OyClZXzsd{whUUN3MDC9JFAvODFzIN88UU4> M1LPVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OUG2OFE4Lz5zNUmxOlQyPzxxYU6=
RPMI8226 NUT3c3BXS3m2b4TvfIlkcXS7IHHzd4F6 M3\mVFQ5KGi{cx?= NILJ[VhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTWE2LOEKyOkBk\WyuczDh[pRmeiB2ODDodpMh[nlicnXzZZp2emmwIHHzd4F6NCCLQ{WwJF0hOC5yMUGg{txONg>? NXrkbZVvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxN|M4PzlpPkG5NVM{Pzd7PD;hQi=>
HCT116 NYD4d4hzS3m2b4TvfIlkcXS7IHHzd4F6 MlXtO|IhcHK| NYS4folpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGOvVG1UKGG|c3H5MEBKSzVyIE2gNE4xOTZizszNMi=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd2Nkm3Okc,OTl5NE[5O|Y9N2F-
HCT116 NHLmOIFEgXSxdH;4bYNqfHliYYPzZZk> Mm\hR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{NCCLQ{WwJF0hOC5yM{Wg{txONg>? M4fQXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOEO1OlI4Lz5{MUizOVYzPzxxYU6=

... Click to View More Cell Line Experimental Data

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

Cell Research:

[1]

- Collapse
  • 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.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: male Sprague-Dawley rats, 6–8 week old mice
  • Dosages: 0.1 mg/kg, 200 µg/kg
  • Administration: IV
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (200.77 mM)

* 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.

Chemical Information

Molecular Weight 313.78
Formula

C15H20ClNO4

CAS No. 437742-34-2
Storage powder
in solvent
Synonyms ML858, Marizomib, MRZ
Smiles CC12C(C(=O)NC1(C(=O)O2)C(C3CCCC=C3)O)CCCl

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 ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04341311 Active not recruiting Drug: Marizomib|Drug: Panobinostat 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
NCT02903069 Completed Drug: MRZ|Drug: TMZ|Radiation: RT|Device: Optune Glioblastoma|Malignant Glioma Celgene|Triphase August 17 2016 Phase 1
NCT02330562 Active not recruiting Drug: MRZ|Drug: BEV Malignant Glioma|Glioblastoma Celgene|Triphase April 15 2015 Phase 1|Phase 2
NCT01501396 Withdrawn Drug: Megestrol Acetate|Drug: Mirtazapine Anorexia Washington University School of Medicine September 2013 Phase 2
NCT00667082 Completed Drug: NPI-0052 (marizomib) + vorinostat Non-Small Cell Lung Cancer|Pancreatic Cancer|Melanoma|Lymphoma|Multiple Myeloma Celgene March 2008 Phase 1

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

Proteasome Signaling Pathway Map

Related Proteasome Products

Tags: buy Salinosporamide A (NPI-0052) | Salinosporamide A (NPI-0052) supplier | purchase Salinosporamide A (NPI-0052) | Salinosporamide A (NPI-0052) cost | Salinosporamide A (NPI-0052) manufacturer | order Salinosporamide A (NPI-0052) | Salinosporamide A (NPI-0052) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID