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

製品コードS4921 バッチS492101

印刷

化学情報

Chemical Structure Synonyms MDBN Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C9H7NO4
分子量 193.16 CAS No. 1485-00-3
Solubility (25°C)* 体外 DMSO 39 mg/mL (201.9 mM)
Water Insoluble
Ethanol Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MNS is a tyrosine kinase inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.
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]
特徴 The nitro group of MNS (3,4-Methylenedioxy-β-nitrostyrene) is essential for its antiplatelet effect.

プロトコル(参考用のみ)

キナーゼアッセイ 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 37℃ 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.

カスタマーフィードバック

Data from [Data independently produced by , , Toxicol Res (Camb), 2016, 5(1):188-196]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Curdione inhibits thrombin-induced platelet aggregation via regulating the AMP-activated protein kinase-vinculin/talin-integrin αIIbβ3 sign pathway [ Phytomedicine, 2019, 61:152859] PubMed: 31039534
Biomolecular interaction of a platelet aggregation inhibitor, 3,4-methylenedioxy-β-nitrostyrene with human serum albumin: Multi-spectral and computational characterization [ J Biomol Struct Dyn, 2019, 10.1080/07391102.2019.1640133] PubMed: 31271347
Kavain Inhibition of LPS-Induced TNF-α via ERK/LITAF. [Tang X, et al. Toxicol Res (Camb), 2016, 5(1):188-196] PubMed: 26918116

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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