MNS
Based on 3 publication(s) in Google Scholar
MNS (NSC 170724), the beta-nitrostyrene derivative, is an orally active tyrosine kinase inhibitor, a broad-spectrum antiplatelet agent, and a PANoptosis inhibitor. MNS inhibits Src, Syk, and FAK with IC50 of 27.3, 2.8, and 97.6 μM, respectively. MNS inhibits NLRP3 inflammasome and β1 integrin. MNS completely inhibits U46619, ADP-, arachidonic acid-, collagen-, and thrombin-induced platelet aggregation with IC50 values of 2.1, 4.1, 5.8, 7.0, and 12.7 μM, respectively. MNS is cytotoxic to a variety of cells.
For research use only. We do not sell to patients.
- CAS No.: 1485-00-3
- Formula: C9H7NO4
- Molecular Weight:193.16
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) MNS
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Biological Activity
Description
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NLRP3 inflammasome |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | GI50 |
1.7 μg/mL
Compound: 4m
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Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay
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[PMID: 19709889] |
| DU-145 | GI50 |
1.8 μg/mL
Compound: 4m
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Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay
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[PMID: 19709889] |
| HBL-100 | IC50 |
>20 μM
Compound: MNS
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Cytotoxicity against human HBL100 cells after 72 hrs by MTT assay
Cytotoxicity against human HBL100 cells after 72 hrs by MTT assay
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[PMID: 20850977] |
| HeLa | IC50 |
3.9 μM
Compound: 2
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Inhibition of proteasomal turnover of p97-independent ODD-luciferase reporter substrate in human HeLa cells incubated for 120 mins by luciferase reporter gene assay
Inhibition of proteasomal turnover of p97-independent ODD-luciferase reporter substrate in human HeLa cells incubated for 120 mins by luciferase reporter gene assay
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[PMID: 33476933] |
| KM-20L2 | GI50 |
1.8 μg/mL
Compound: 4m
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Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay
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[PMID: 19709889] |
| L02 | IC50 |
39.24 μM
Compound: MNS
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Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
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[PMID: 35428012] |
| L02 | IC50 |
41.1 μM
Compound: MNS
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Cytotoxicity against human L-02 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human L-02 cells incubated for 24 hrs by MTT assay
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[PMID: 34506712] |
| MCF7 | GI50 |
0.58 μg/mL
Compound: 4m
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Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay
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[PMID: 19709889] |
| MDA-MB-231 | IC50 |
14 μM
Compound: MNS
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Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
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[PMID: 20850977] |
| NCI-H460 | GI50 |
2 μg/mL
Compound: 4m
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Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay
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[PMID: 19709889] |
| P388 | ED50 |
2 μg/mL
Compound: 4m
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Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay
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[PMID: 19709889] |
| Platelet | IC50 |
14 μM
Compound: MNS
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Antiaggregatory activity in human platelets assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins before thrombin challenge by turbidimetry analysis
Antiaggregatory activity in human platelets assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins before thrombin challenge by turbidimetry analysis
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[PMID: 20850977] |
| Platelet | IC50 |
7.2 μM
Compound: MNS
|
Antiaggregatory activity in human platelets assessed as inhibition of collagen-induced platelet aggregation preincubated for 3 mins before collagen challenge by turbidimetry analysis
Antiaggregatory activity in human platelets assessed as inhibition of collagen-induced platelet aggregation preincubated for 3 mins before collagen challenge by turbidimetry analysis
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[PMID: 20850977] |
| SF-268 | GI50 |
1.9 μg/mL
Compound: 4m
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Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay
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[PMID: 19709889] |
In Vitro
MNS (48 h) shows cytotoxicity against human BxPC3, DU145, and KM20L2 cells, with GI50 of 1.7 μg/mL, 1.8 μg/mL, 1.8 μg/mL, respectively[3].
MNS (1-20 μM, 1-15 h) inhibits adhesion and migration of MDA-MB-231 cells by suppressing β1 integrin function and surface protein disulfide isomerase[4].
MNS (1-10 μM, 15 min) inhibits NLRP3 inflammasome activation in LPS-primed BMDMs by blocking assembly of the inflammasome[5].
MNS (2.5-10 μM, 4-24 h) decreases the motility and colony formation of osteosarcoma cells[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-231
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Concentration:1, 2, 5, 10, 20 μM
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Incubation Time:15 h
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Result:Concentration-dependently prevented MDA-MB-231 cells from migrating.
Failed to migrate into and close a wound at 10 and 20 μM.
Abolished the migration at 5 μM.
In Vivo
MNS (30 mg/kg, p.o., 5 days) alleviates DSS-induced mouse colitis by inhibiting the NLRP3 inflammasome[8].
MNS (20 mg/kg, i.p., 30 min before reperfusion) significantly protects the kidneys from RIR injury in rats by reducing PANoptosis through specific inhibition of NLRP3[9].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1485-00-3
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Appearance Solid
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Molecular Weight 193.16
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Formula C9H7NO4
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Color Light yellow to green yellow
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SMILES
O=[N+]([O-])/C=C/C1=CC(OCO2)=C2C=C1
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Synonyms
NSC 170724; 5-(2-Nitrovinyl)benzodioxole
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (258.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (12.94 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang WY, et al. Synthesis and pharmacological evaluation of novel beta-nitrostyrene derivatives as tyrosine kinase inhibitors with potent antiplatelet activity. Biochem Pharmacol. 2007;74(4):601-611. [Content Brief]
[2]. Wang WY, et al. Prevention of platelet glycoprotein IIb/IIIa activation by 3,4-methylenedioxy-beta-nitrostyrene, a novel tyrosine kinase inhibitor. Mol Pharmacol. 2006;70(4):1380-1389. [Content Brief]
[3]. Pettit RK, et al. E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes. Bioorg Med Chem. 2009 Sep 15;17(18):6606-12. [Content Brief]
[4]. Chen IH, et al. 3,4-Methylenedioxy-β-nitrostyrene inhibits adhesion and migration of human triple-negative breast cancer cells by suppressing β1 integrin function and surface protein disulfide isomerase. Biochimie. 2015 Mar;110:81-92. [Content Brief]
[5]. He Y, et al. 3,4-methylenedioxy-β-nitrostyrene inhibits NLRP3 inflammasome activation by blocking assembly of the inflammasome. J Biol Chem. 2014 Jan 10;289(2):1142-50. [Content Brief]
[6]. Messerschmitt PJ, et al. Osteosarcoma Phenotype Is Inhibited by 3,4-Methylenedioxy-β-nitrostyrene. Sarcoma. 2012;2012:479712. [Content Brief]
[7]. Xiao M, et al. 3,4-Methylenedioxy-β-Nitrostyrene Ameliorates Experimental Burn Wound Progression by Inhibiting the NLRP3 Inflammasome Activation. Plast Reconstr Surg. 2016 Mar;137(3):566e-575e. [Content Brief]
[8]. Zheng J, et al. 3,4-Methylenedioxy-β-Nitrostyrene Alleviates Dextran Sulfate Sodium-Induced Mouse Colitis by Inhibiting the NLRP3 Inflammasome. Front Pharmacol. 2022 Jun 15;13:866228. [Content Brief]
[9]. Uysal E, et al. Targeting the PANoptosome with 3,4-Methylenedioxy-β-Nitrostyrene, Reduces PANoptosis and Protects the Kidney against Renal İschemia-Reperfusion Injury. J Invest Surg. 2022 Nov-Dec;35(11-12):1824-1835. [Content Brief]
[10]. Wang L, et al. Mechanisms of PANoptosis and relevant small-molecule compounds for fighting diseases. Cell Death Dis. 2023 Dec 21;14(12):851. [Content Brief]
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 | 5.1771 mL | 25.8853 mL | 51.7706 mL | 129.4264 mL |
| 5 mM | 1.0354 mL | 5.1771 mL | 10.3541 mL | 25.8853 mL | |
| 10 mM | 0.5177 mL | 2.5885 mL | 5.1771 mL | 12.9426 mL | |
| 15 mM | 0.3451 mL | 1.7257 mL | 3.4514 mL | 8.6284 mL | |
| 20 mM | 0.2589 mL | 1.2943 mL | 2.5885 mL | 6.4713 mL | |
| 25 mM | 0.2071 mL | 1.0354 mL | 2.0708 mL | 5.1771 mL | |
| 30 mM | 0.1726 mL | 0.8628 mL | 1.7257 mL | 4.3142 mL | |
| 40 mM | 0.1294 mL | 0.6471 mL | 1.2943 mL | 3.2357 mL | |
| 50 mM | 0.1035 mL | 0.5177 mL | 1.0354 mL | 2.5885 mL | |
| 60 mM | 0.0863 mL | 0.4314 mL | 0.8628 mL | 2.1571 mL | |
| 80 mM | 0.0647 mL | 0.3236 mL | 0.6471 mL | 1.6178 mL | |
| 100 mM | 0.0518 mL | 0.2589 mL | 0.5177 mL | 1.2943 mL |