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MedChemExpress LLC (MCE)
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MedChemExpress - Model MNS - 1485-00-3

MedChemExpress - Model MNS - 1485-00-3

MNS (NSC 170724), the beta-nitrostyrene derivative, is a potent tyrosine kinase inhibitor and a broad-spectrum antiplatelet agent. 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 inhibits Src, Syk, and FAK with IC50 of 27.3, 2.8, and 97.6 μM, respectively[1][2].

MNS

MCE China：MNS

Brand：MedChemExpress (MCE)

Cat. No.HY-78263

CAS：1485-00-3

Synonyms：NSC 170724; 5-(2-Nitrovinyl)benzodioxole

Purity：99.43%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：MNS (NSC 170724), the beta-nitrostyrene derivative, is an orally active tyrosine kinase inhibitor and a broad-spectrum antiplatelet agent. 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.

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].

In Vivo：MNS (20 mg/kg, i.p.) ameliorates experimental burn wound progression in Wistar rats by inhibiting the NLRP3 inflammasome activation[7]. 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].

IC50 & Target：NLRP3 inflammasome

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]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。