2. Metabolic Enzyme/Protease
  3. Proteasome
  4. Marizomib

Marizomib  (Synonyms: Salinosporamide A; NPI-0052)

Cat. No.: HY-10985 Purity: 99.13%
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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).

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Marizomib Chemical Structure

Marizomib Chemical Structure

CAS No. : 437742-34-2

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100 μg USD 150 In-stock
500 μg USD 410 In-stock
1 mg USD 670 In-stock
5 mg USD 1450 In-stock
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Based on 10 publication(s) in Google Scholar

Marizomib Related Antibodies

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Description

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)[1][2][3].

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 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]
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]
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.

Marizomib Related Antibodies

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.
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
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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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)

g

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%

SDS (557 KB)

COA (256 KB) HNMR (277 KB) LCMS (100 KB)

Handling Instructions (2659 KB)
References

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.

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
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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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