Marizomib (Synonyms: Salinosporamide A; NPI-0052)

Name: Marizomib
Brand: MedChemExpress
SKU: HY-10985
Rating: 5.0 (17 reviews)

Cat. No.: HY-10985 Purity: 99.13%: Data Sheet
COA

SDS
Handling Instructions
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Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively).

For research use only. We do not sell to patients.

CAS No. : 437742-34-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 μg	In-stock	Estimated Time of Arrival: December 31
500 μg	In-stock	Estimated Time of Arrival: December 31
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	Get quote
50 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 17 publication(s) in Google Scholar

17 Publications Citing Use of MCE Marizomib

Cell Proliferation/Viability Assay

Flow Cytometry

RT-PCR

In Vivo Efficacy Study

: Marizomib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Oct 22;41(1):311. [Abstract]; Cell viability (top) and CI (bottom) of MB002 and D283 cells treated with Marizomib (2.5-4 nM for MB002; 12.5-100 nM for D283; 72 h).

: Marizomib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Oct 22;41(1):311. [Abstract]; FACS analyses of cell proliferation (top) and apoptosis (bottom) of MB002 cells treated with Marizomib (2.5 nM).

: Marizomib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Oct 22;41(1):311. [Abstract]; Marizomib (4 nM for MB002; 50 nM for D283; 8 h) induced expression of seven representative UPR genes (BiP, CHOP, IRE1α, ATF3, ATF4, GADD34, HERPUD1) in MB002 and D283 cells.

: Marizomib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Oct 22;41(1):311. [Abstract]; Kaplan-Meier survival curve of nude mice carrying orthotopic xenografts of MB002-GFP-luc cells treated with Marizomib (150 μg/kg; i.v.; once a week).

: Marizomib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Oct 22;41(1):311. [Abstract]; Cell viability of MB002 and D425 cells treated with Marizomib (3.25 nM for MB002; 125 nM for D425) was measured at Day 0/2/4 post treatment and normalized to Day 0-value.

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Biological Activity
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References
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Description

IC₅₀ & Target

IC50: 3.5 nM (CT-L), 28 nM (CT-T-laspase-like), 430 nM (trypsin-like)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	GI₅₀	35 nM Compound: 66	Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition	[PMID: 35063731]
HCT-116	IC₅₀	16 nM Compound: 1	Cytotoxicity against human HCT116 cells after 72 hrs by MTS/PMS assay Cytotoxicity against human HCT116 cells after 72 hrs by MTS/PMS assay	[PMID: 19746976]
HCT-116	IC₅₀	35 nM Compound: marizomib, NPI-0052	Cytotoxicity against human HCT116 cells Cytotoxicity against human HCT116 cells	[PMID: 21835627]
HCT-116	IC₅₀	<= 2 ng/mL Compound: 1, NPI-0052	Cytotoxicity against human HCT116 cells Cytotoxicity against human HCT116 cells	[PMID: 19022674]
HEK293	IC₅₀	11 nM Compound: 1	Inhibition of NF-kB activation in HEK293 cells Inhibition of NF-kB activation in HEK293 cells	[PMID: 15916417]
HOP-92	GI₅₀	< 11 nM Compound: 66	Cytotoxicity against human HOP-92 cells assessed as cell growth inhibition Cytotoxicity against human HOP-92 cells assessed as cell growth inhibition	[PMID: 35063731]
LOX IMVI	GI₅₀	< 11 nM Compound: 66	Cytotoxicity against human LOX IMVI cells assessed as cell growth inhibition Cytotoxicity against human LOX IMVI cells assessed as cell growth inhibition	[PMID: 35063731]
OVCAR-3	GI₅₀	< 11 nM Compound: 66	Cytotoxicity against human OVCAR-3 cells assessed as cell growth inhibition Cytotoxicity against human OVCAR-3 cells assessed as cell growth inhibition	[PMID: 35063731]
PC-3	GI₅₀	< 11 nM Compound: 66	Cytotoxicity against human PC-3 cells assessed as cell growth inhibition Cytotoxicity against human PC-3 cells assessed as cell growth inhibition	[PMID: 35063731]
RPMI-8226	IC₅₀	11 nM Compound: 1, NPI-0052	Cytotoxicity against human RPMI8226 cells after 48 hrs by resazurin assay Cytotoxicity against human RPMI8226 cells after 48 hrs by resazurin assay	[PMID: 19133779]
RPMI-8226	IC₅₀	8.2 nM Compound: 1	Cytotoxic activity against RPMI 8226 cells Cytotoxic activity against RPMI 8226 cells	[PMID: 15916417]

In Vitro

Marizomib (Salinosporamide A) (0.1-10000 nM; 72 hours) effectively reduces survival of D-54 and U-251 cells in a dose-dependent manner. The IC₅₀s are ～52 nM for U-251 and ～20 nM for D-54^[1].
Marizomib (24 hours; 60 nM) induces apoptosis and caspase-3 activation in glioma cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	U-251 and D-54 cells
Concentration:	0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time:	72 hours
Result:	Effectively reduced survival of D-54 and U-251 cells in a dose-dependent manner.

Apoptosis Analysis^[1]

Cell Line:	D-54 cells
Concentration:	60 nM
Incubation Time:	24 hours
Result:	Induces D-54 cells apoptosis.

Western Blot Analysis^[1]

Cell Line:	D-54 cells
Concentration:	60 nM
Incubation Time:	24 hours
Result:	Led to increased activity of caspase-3 in a dose-dependent manner.

In Vivo

Marizomib (Salinosporamide A) (0.15 mg/kg; i.v; twice a week for three weeks) significantly decreases tumor growth, and is not associated with any toxicity^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CB-17 SCID-male mice (4-6 weeks old)^[3]
Dosage:	0.15 mg/kg
Administration:	i.v; twice a week for three weeks
Result:	Significantly decreased tumor growth, and was not associated with any toxicity.

Clinical Trial

Molecular Weight

313.78

Formula

C₁₅H₂₀ClNO₄

CAS No.

437742-34-2

Appearance

Solid

Color

Off-white to pink

SMILES

O=C([C@H](CCCl)[C@]1(C)O2)N[C@@]1([C@H]([C@@H]3C=CCCC3)O)C2=O

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (318.69 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1869 mL	15.9347 mL	31.8695 mL
5 mM	0.6374 mL	3.1869 mL	6.3739 mL
10 mM	0.3187 mL	1.5935 mL	3.1869 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.13%

Select Batch:

Data Sheet (283 KB) SDS (557 KB)

COA (256 KB) HNMR (277 KB) LCMS (104 KB)

Handling Instructions (2659 KB)

References

[1]. Di K, et al. Marizomib activity as a single agent in malignant gliomas: ability to cross the blood-brainbarrier. Neuro Oncol. 2016 Jun;18(6):840-8. [Content Brief]

[2]. Kale AJ, et al. Molecular mechanisms of acquired proteasome inhibitor resistance. J Med Chem. 2012 Dec 13;55(23):10317-27. [Content Brief]

[3]. Singh AV, et al. Pharmacodynamic and efficacy studies of the novel proteasome inhibitor NPI-0052 (marizomib) in a human plasmacytoma xenograft murine model. Br J Haematol. 2010 May;149(4):550-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1869 mL	15.9347 mL	31.8695 mL	79.6737 mL
	5 mM	0.6374 mL	3.1869 mL	6.3739 mL	15.9347 mL
	10 mM	0.3187 mL	1.5935 mL	3.1869 mL	7.9674 mL
	15 mM	0.2125 mL	1.0623 mL	2.1246 mL	5.3116 mL
	20 mM	0.1593 mL	0.7967 mL	1.5935 mL	3.9837 mL
	25 mM	0.1275 mL	0.6374 mL	1.2748 mL	3.1869 mL
	30 mM	0.1062 mL	0.5312 mL	1.0623 mL	2.6558 mL
	40 mM	0.0797 mL	0.3984 mL	0.7967 mL	1.9918 mL
	50 mM	0.0637 mL	0.3187 mL	0.6374 mL	1.5935 mL
	60 mM	0.0531 mL	0.2656 mL	0.5312 mL	1.3279 mL
	80 mM	0.0398 mL	0.1992 mL	0.3984 mL	0.9959 mL
	100 mM	0.0319 mL	0.1593 mL	0.3187 mL	0.7967 mL

Marizomib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Marizomib437742-34-2Salinosporamide A NPI-0052NPI0052NPI 0052NPI-0052Proteasomeirreversiblebrain-penetrantpanglioblastomablood-brainbarriercaspasesantitumorInhibitorinhibitorinhibit

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Marizomib (Synonyms: Salinosporamide A; NPI-0052)

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Marizomib Related Antibodies

17 Publications Citing Use of MCE Marizomib

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Biological Activity

Purity & Documentation

References

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Complete Stock Solution Preparation Table

Marizomib Related Classifications

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