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Salinosporamide A (NPI-0052, Marizomib) (Synonyms: Marizomib, ML-858, NPI-0052)

Catalog No.GC10486

An orally bioactive proteasome inhibitor

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Salinosporamide A (NPI-0052, Marizomib) Chemical Structure

Cas No.: 437742-34-2

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100µg
$135.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Human MM-cell lines (MM.1S, INA-6, RPMI-8226, MM.1R,KMS12PE, and U266)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

24 h; 2nM

Applications

Human MM-cell lines were pretreated with lenalidomide for 24 hours; NPI-0052 was then added for an additional 24 hours, followed by assessment for cell viability using MTT assays. A significant decrease in viability of all cell lines was observed in response to treatment with combined low doses of NPI-0052 and lenalidomide compared with either agent alone(P<0.05; n=3). These data demonstrate synergistic anti-MM activity of NPI-0052 plus lenalidomide.

Animal experiment [2]:

Animal models

CB-17 SCID-male mice

Dosage form

0.15 mg/kg; i.v.

Applications

MM.1S-tumour bearing mice were injected with NPI-0052(0.15 mg/kg; i.v.) twice a week for 3 weeks, and tumour volume was measured. NPI-0052 treatment significantly decreased tumour growth relative to vehicle-treated control mice (P =0.005). NPI-0052 treatment was not associated with any toxicity, because no differences in body weight and overall appearance were noted. Importantly, the anti-MM activity of NPI-0052 was evident as early as day 5–7, when significant proteasome inhibition was observed in the tumours.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Chauhan D, Singh A V, Ciccarelli B, et al. Combination of novel proteasome inhibitor NPI-0052 and lenalidomide trigger in vitro and in vivo synergistic cytotoxicity in multiple myeloma[J]. Blood, 2010, 115(4): 834-845.

[2] Singh A V, Palladino M A, Lloyd G K, et al. Pharmacodynamic and efficacy studies of the novel proteasome inhibitor NPI‐0052 (marizomib) in a human plasmacytoma xenograft murine model[J]. British journal of haematology, 2010, 149(4): 550-559.

Background

Salinosporamide A is a potent inhibitor of 20S proteasome with IC50 value of 1.3 nM [1].

Salinosporamide A was isolated from the crude extract of a Salinospora strain CNB-392. It showed potent anti-tumor activity with an IC50 value of 11 ng/mL in HCT-116 cells. It also exerted a mean GI50 value of less than 10 nM in the NCI’s 60 cell line-panel. Among these cell lines, Salinosporamide A showed the greatest potent efficacies in NCI-H226, SF-539, SK-MEL-28 and MDA-MB-435 cells. Salinosporamide A inhibited the purified 20S proteasome with IC50 value of 1.3 nM. It was about 35-fold more potent than the first discovered specific proteasome inhibitor, omuralide [1].

References:
[1] Feling R H, Buchanan G O, Mincer T J, et al. Salinosporamide A: a highly cytotoxic proteasome inhibitor from a novel microbial source, a marine bacterium of the new genus Salinospora. Angewandte Chemie International Edition, 2003, 42(3): 355-357.

Chemical Properties

Cas No. 437742-34-2 SDF
Synonyms Marizomib, ML-858, NPI-0052
Chemical Name (1S,2R,5R)-2-(2-chloroethyl)-5-[(S)-[(1S)-cyclohex-2-en-1-yl]-hydroxymethyl]-1-methyl-7-oxa-4-azabicyclo[3.2.0]heptane-3,6-dione
Canonical SMILES CC12C(C(=O)NC1(C(=O)O2)C(C3CCCC=C3)O)CCCl
Formula C15H20ClNO4 M.Wt 313.78
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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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. )

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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