NSC 405020
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NSC-405020是一种新型的膜型1基质金属蛋白酶(MT1-MMP)小分子抑制剂。相对于MT1-MMP的催化结构域,NSC-405020特异性地靶向血红素结合蛋白(PEX)结构域,其IC50值大于100 μmol/L,同时不影响MT1-MMP或MMP-2的催化活性。NSC-405020直接结合到PEX并与其相互作用(完整MT1-MMP结构成药口袋Met-328、Arg-330、Asp-376、Met-22和Ser-470位点附近),影响β-螺旋片I~ IV的构象和灵活性,从而降低细胞内PEX依赖性的MT1-MMP同源二聚化。NSC-405020不影响MT1-MMP对MMP-2的激活,但影响其降解COL-I的能力。
参考文献:
Remacle AG, Golubkov VS, Shiryaev SA, Dahl R, Stebbins JL, Chernov AV, Cheltsov AV, Pellecchia M, Strongin AY. Novel MT1-MMP small-molecule inhibitors based on insights into hemopexin domain function in tumor growth. Cancer Res. 2012 May 1;72(9):2339-49. doi: 10.1158/0008-5472.CAN-11-4149. Epub 2012 Mar 9.
- 1. Patricia Llorente, Víctor Mejías, et al. "Matrix metalloproteinase 14 regulates HSV-1 infection in neuroblastoma cells." Antiviral Res. 2021 Aug;192:105116. PMID: 34107282
- 2. Patricia Llorente, Soraia Martins, et al. "Matrix Metalloproteinase 14 Mediates APP Proteolysis and Lysosomal Alterations Induced by Oxidative Stress in Human Neuronal Cells." Oxid Med Cell Longev. 2020 Nov 16;2020:5917187. PMID: 33282112
- 3. El Azzouzi K, Wiesner C, Linder S. "Metalloproteinase MT1-MMP islets act as memory devices for podosome reemergence." J Cell Biol. 2016 Apr 11;213(1):109-25. PMID: 27069022
Physical Appearance | A solid |
Storage | Store at RT |
M.Wt | 260.16 |
Cas No. | 7497-07-6 |
Formula | C12H15Cl2NO |
Synonyms | NSC405020, NSC-405020 |
Solubility | insoluble in H2O; ≥11.4 mg/mL in DMSO; ≥96.4 mg/mL in EtOH |
Chemical Name | 3,4-dichloro-N-pentan-2-ylbenzamide |
SDF | Download SDF |
Canonical SMILES | CCCC(C)NC(=O)C1=CC(=C(C=C1)Cl)Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | NSC 405020是膜型I基质金属蛋白酶(MT1-MMP)的小分子抑制剂,其IC50值大于100 μM。 | |||||
靶点 | MT1-MMP | |||||
IC50 | > 100 μM |
质量控制和MSDS
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