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Marizomib

Name: Marizomib
Brand: TargetMol
SKU: T16012
Price: 123 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16012Cas No. 437742-34-2

Alias Salinosporamide A, NPI-0052, ML858

Marizomib is a novel irreversible brain-permeable proteasome inhibitor that inhibits CT-L (β5), CT-T-laspase-like (C-L, β1), and trypsin-like (T-L, β2) 20S proteasomes with IC50s of 3.5, 28, and 430 nM.[3]

Marizomib

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Purity: 99.41%

Catalog No. T16012Alias Salinosporamide A, NPI-0052, ML858Cas No. 437742-34-2

Pack Size	Price	USA Warehouse	Global Warehouse
100 μg	$123	-	In Stock
500 μg	$338	In Stock	In Stock
1 mg	$553	In Stock	In Stock
5 mg	$1,180	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.41%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Marizomib is a novel irreversible brain-permeable proteasome inhibitor that inhibits CT-L (β5), CT-T-laspase-like (C-L, β1), and trypsin-like (T-L, β2) 20S proteasomes with IC50s of 3.5, 28, and 430 nM.[3]
Targets&IC50	Trypsin like:430 nM, CTL laspase-like:28 nM, CTL:3.5 nM
In vitro	METHODS: TNBC (basal), ductal and non-malignant breast epithelial cells were treated with Marizomib (0-500 nM) and cell proliferation was analyzed using the MTS assay after 6 days. RESULTS Marizomib selectively reduced TNBC cell proliferation in a concentration-dependent manner without much effect on non-TNBC and non-malignant mammary epithelial cells (MCF10A and D492), with IC50 values of Marizomib less than 150 nM in TNBC cell lines and greater than 1 µM in non-TNBC cell lines.[1] METHODS: SUM159PT cells were treated with 100 nM Marizomib for 0 and 9 hours (prior to induction of apoptosis) and label-free global proteomics analysis was performed to identify proteins or pathways altered by Marizomib. RESULTS A total of 2547 proteins were identified, of which 425 proteins were downregulated (log2 ≤ 0.6) and 293 proteins were upregulated (log2 ≥ 0.6).Marizomib decreased the levels of 11 proteasome subunits, and 5 proteasome subunits (PSMA5, PSMC2, PSMD2, PSMA1, PSMA7 and PSMA8) were also observed to be Up-regulation. [1] METHODS: Cells were treated with 40 nM or 80 nM marizomib for 4 h. CT-L activity of proteasome in total cell lysates was determined by lysing Suc-LLVY-AMC. RESULTS marizomib effectively inhibited proteasomes in both responsive and non-responsive cells. [2]
In vivo	METHODS: After two weeks of Marizomib (0.15 mg/kg twice/week, IP) treatment of MDA-MB-231 xenografts and patient-derived tumor xenografts (PDX), it was observed whether tumor growth was inhibited in vivo. RESULTS Marizomib treatment significantly reduced tumor volume and tumor weight in MDA-MB-231 xenografts and patient-derived tumor xenografts (PDX). [1]
Synonyms	Salinosporamide A, NPI-0052, ML858

Chemical Properties

Molecular Weight	313.78
Formula	C₁₅H₂₀ClNO₄
Cas No.	437742-34-2
Smiles	[C@@H](O)([C@]12[C@](C)([C@@H](CCCl)C(=O)N1)OC2=O)[C@]3(CCCC=C3)[H]
Relative Density.	1.348 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 31.38 mg/mL (100.01 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.37 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.1869 mL	15.9347 mL	31.8695 mL	159.3473 mL
5 mM	0.6374 mL	3.1869 mL	6.3739 mL	31.8695 mL
10 mM	0.3187 mL	1.5935 mL	3.1869 mL	15.9347 mL
20 mM	0.1593 mL	0.7967 mL	1.5935 mL	7.9674 mL
50 mM	0.0637 mL	0.3187 mL	0.6374 mL	3.1869 mL
100 mM	0.0319 mL	0.1593 mL	0.3187 mL	1.5935 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc