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NNGH
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NNGH图片
CAS NO:161314-17-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
25mg电议

产品介绍
NNGH 是一种溶基质素-1 (MMP-3) 抑制剂。 MMP-3 既是直接转录靶标,也是 Wnt/β-catenin 信号通路的必要贡献者。基质金属蛋白酶 (MMP) 在肿瘤进展的后期发挥着明确的作用。
Cas No.161314-17-6
别名N-Isobutyl-N-(4-methoxyphenylsulfonyl)glycyl Hydroxamic Acid,Matrix Metalloproteinase-3 Inhibitor II,MMP-3 Inhibitor II
化学名N-hydroxy-2-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-acetamide
Canonical SMILESONC(CN(S(C1=CC=C(OC)C=C1)(=O)=O)CC(C)C)=O
分子式C13H20N2O5S
分子量316.4
溶解度≤25mg/ml in ethanol;100mg/ml in DMSO
储存条件Room temperature
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ki: 9, 2.6, 4.3, 3.1, and 17 nM for MMP-8, -9, -12, -13, and -20, respectively.

NNGH is an inhibitor of MMPs.

Matrix metalloproteinases (MMPs), a large class of strictly-related zincdependent enzymes, belong to the family of proteolytic enzymes. MMPs are involved in various aspects of physiological cellular processes and pathologies, such as pulmonary emphysema, reumathoid arthritis, tumor growth and metastasis.

In vitro: Previous study found that NNGH was one of the most prominent representatives of a family of nanomolar inhibitors for some MMPs. In addition, the X-Ray structure of the NNGH-MMP-12 complex showed that the interaction of NNGH with the active site of the enzyme involved the binding of the hydroxamic functional group to the catalytic Zn ion and the binding of the aromatic group to the S1 subsite [1].

In vivo: Previous animal study found that the repeated administration of NNGH to WT mice was able to block the MMP-3 levels, which could reduce the number of adherent retinal leukocytes by 60% as compared to vehicle-treated mice. In addition, the administration of NNGH could even lead to a more pronounced decrease in leukocyte adhesion and the treatment of MMP-3-/- mice with NNGH showed a reduced hypothermic response as compared to vehicle-injected MMP-3-/- mice [2].

Clinical trial: Up to now, NNGH is still in the preclinical development stage.

References:
[1] E.  Attolino, V. Calderone, E. Dragoni, et al. Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs). European Journal of Medicinal Chemistry (2010).
[2] Inge Van Hove et al.  MMP-3 Deficiency Alleviates Endotoxin-Induced Acute Inflammation in the Posterior Eye SegmentInt J Mol Sci. 2016 Nov; 17(11): 1825.