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MNS (3,4-Methylenedioxy-β-nitrostyrene) p97 inhibitor

Cat.No.S4921

MNS (3,4-Methylenedioxy-β-nitrostyrene) is a tyrosine kinase inhibitor that inhibits Syk, Src, and p97 with IC50 values of 2.5 μM, 29.3 μM, and 1.7 μM, respectively.
MNS (3,4-Methylenedioxy-β-nitrostyrene) p97 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 193.16

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 193.16 Formula

C9H7NO4

Storage (From the date of receipt)
CAS No. 1485-00-3 Download SDF Storage of Stock Solutions

Synonyms MDBN Smiles C1OC2=C(O1)C=C(C=C2)C=C[N+](=O)[O-]

Solubility

In vitro
Batch:

DMSO : 39 mg/mL (201.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Features
The nitro group of MNS (3,4-Methylenedioxy-β-nitrostyrene) is essential for its antiplatelet effect.
Targets/IC50/Ki
p97 [2]
1.7 μM
Syk [1]
2.5 μM
Src [1]
29.3 μM
In vitro
MNS (3,4-methylenedioxy-β-nitrostyrene) completely inhibits 2 μM U46619-(a thromboxane A2 mimic), 5 μM ADP-, 100 μM arachidonic acid-(AA), 10 μg/ml collagen-, and 0.1 U/ml thrombin-induced platelet aggregation in a concentration-dependent manner with IC50 of 2.1 μM, 4.1 μM, 5.8 μM, 7.0 μM, and 12.7 μM, respectively. It inhibits platelet aggregation caused by either the calcium ionophore A23187 (1 μM) or the protein kinase C (PKC) activator PDBu (200 nM) with IC50 of 25.9 μM and 4.8 μM, respectively. This compound (20 μM) decreases thrombin-induced P-selectin expression on platelets to levels comparable to those observed in PGE1-treated platelets. It (20 μM) markedly inhibits thrombin-but not PDBu-induced MARCKS phosphorylation in platelets. MNS (20 μM) markedly inhibits protein tyrosine phosphorylation at either 0.5 min or 3 min after thrombin or collagen stimulation in platelets. [1] It stimulates UbG76V-GFP and ODD-Luc degradation with IC50 of 1.6 μM and 5.9 μM, respectively, and inhibits MG132-induced accumulation of the reporter with IC50 of 2.1 μM. [2] MNS inhibits Gram-positive (Staphylococcus aureus and Enterococcus faecalis) and Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacteria with minimum inhibitory concentrations (MICs) of 128 mg/L. [3] It is much more potent than genistein in inhibiting platelet aggregation and protein tyrosine phosphorylation, and is equally potent as inhibitors of platelet aggregation as 3,4-dimethoxy-β-nitrostyrene. This compound (20 μM) concentration-dependently prevents ATP release from platelets stimulated by thrombin or collagen, and inhibits thrombin-induced PAC-1 binding to human platelets. [4]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04473027 Terminated
Melanoma|Cancer
University Hospital Ghent|Jessa Hospital|University Hospital Antwerp|Algemeen Ziekenhuis Maria Middelares|GZA Ziekenhuizen Campus Sint-Augustinus|AZ Sint-Jan AV|AZ Nikolaas|AZ Sint-Lucas Gent|AZ Sint-Lucas Brugge|General Hospital Groeninge|OLV van Lourdes Hospital Waregem|AZ Damiaan|AZ Delta|ASZ Aalst|Belgian Red Cross
September 1 2020 --
NCT01362244 Completed
Nasal Polyps
GlaxoSmithKline
May 12 2009 Phase 2
NCT00474799 Completed
Healthy
Javelin Pharmaceuticals
January 2007 Phase 1

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