MNS (3,4-Methylenedioxy-Î²-nitrostyrene, MDBN)

貨號 Cat. No.: S4921
規格 Size: 25mg
品牌 Brand: Selleckchem

Description

MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)

Catalog No.S4921

MNS is a tyrosine kinases inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.

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25mg

USD 185

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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Biological Activity

Description	MNS is a tyrosine kinases inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.
Targets	Syk	Src	p97
IC50	2.5 μM	29.3 μM [1]	1.7 μM [2]
In vitro	MNS (3,4-methyl-enedioxy-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. MNS 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. MNS (20 μM) decreases dthrombin-induced P-selectin expression on platelets to levels comparable to those observed in PGE1-treated platelets. MNS (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] MNS stimulates UbG76V-GFP and ODD-Luc degradation with IC50 of 1.6 μM and 5.9 μM, respectively. MNS 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] MNS is much more potent than genistein in inhibiting platelet aggregation and protein tyrosine phosphorylation. MNS (3,4-Methylenedioxy-β-nitrostyrene) is equally potent as inhibitors of platelet aggregation as 3,4-dimethoxy-β-nitrostyrene. MNS (20 μM) concentration-dependently prevents ATP release from platelets stimulated by thrombin or collagen. MNS (20 μM) inhibits thrombin-induced PAC-1 binding to human platelets.[4]
In vivo
Features	The nitro group of MNS (3,4-Methylenedioxy-β-nitrostyrene) is essential for its antiplatelet effect.

Protocol(Only for Reference)

Kinase Assay: [1]

Tyrosine Kinase Assay

For immune complex kinase assay, platelets treated with MNS, PP1, or piceatannol are lysed and immunoprecipitated with either anti-Src or anti-Syk antibody. In some experiments, recombinant human Src, Syk, FAK, or JAK2 is used and treated with MNS or tyrosine kinase inhibitors for 5 min. The activity of the immunoprecipitated kinases or the recombinant enzymes is determined by using a tyrosine kinase assay kit. Samples are incubated with biotinylated poly[Glu:Tyr] (4:1), an exogenous substrate, in kinase assay buffer (20 mM HEPES, 5 mM MgCl2, 5 mM MnCl2, 0.1 mM sodium orthovanadate, and 1 mM dithiothreitol) for 37â„ƒ for 30 to 45 min. After stopping the enzyme reaction with EDTA (final concentration of 20 mM), both the phosphorylated and dephosphorylated substrates are immobilized by binding to the streptavidin-coated plate. The fraction of phosphorylated substrate is determined using a phosphotyrosine monoclonal antibody conjugated to HRP and an ensuing chromogenic substrate reaction.

References

Chemical Information

Download MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN) SDF

Molecular Weight (MW)	193.16
Formula	C9H7NO4
CAS No.	1485-00-3

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	39 mg/mL (201 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.