Description
NNGH is a cell-
permeable, broad-
spectrum inhibitor of matrix metalloproteinases (MMPs). It blocks the activity of MMP-8, -9, -12, -13, and -20 with K
i values of 9, 2.6, 4.3, 3.1, and 17 nM, respectively. It also inhibits MMP-1, -3, -7, and -10 with K
i values of 0.17, 0.13, 13, and 0.1 μM, respectively. It is commonly used to study the role of MMP-3 (stromelysin 1) in biological systems.
Uses
MMP-3 Inhibitor II is a cell-permeable, broad-spectrum inhibitor of matrix metalloproteinases (MMPs). It blocks the activity of MMP-8, -9, -12, -13, and -20 with Ki values of 9, 2.6, 4.3, 3.1, and 17 nM, respectively. It also inhibits MMP-1, -3, -7, and -10 with Ki values of 0.17, 0.13, 13, and 0.1 μM, respectively. It is commonly used to study the role of MMP-3 (stromelysin 1) in biological systems.[Cayman Chemical]
Uses
NNGH acts as a matrix metalloproteinase (MMP) inhibitor affecting the degredation of all the components of the extracellular matrix. Thought to be crucial for agressive processes tumor metastasis and angiogenesis.
General Description
Contains 5 mg each of MMP-2/MMP-9 Inhibitor I (Cat. No.
444241) and MMP-3 Inhibitor II (Cat. No.
444225), and 1 mg each of GM 6001 (Cat. No.
364205), GM 6001, Negative Control (Cat. No.
364210), and MMP-8 Inhibitor I (Cat. No.
444237).
Biochem/physiol Actions
Primary TargetMMP
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].
References
[1] LAWRENCE J. MACPHERSON. Discovery of CGS 27023A, a Non-Peptidic, Potent, and Orally Active Stromelysin Inhibitor That Blocks Cartilage Degradation in Rabbits[J]. Journal of Medicinal Chemistry, 1997, 40 16: 2525-2532. DOI:
10.1021/jm960871c[2] ARCO Y. JENG ∗ David T P Mary Chou. Sulfonamide-based hydroxamic acids as potent inhibitors of mouse macrophage metalloelastase[J]. Bioorganic & Medicinal Chemistry Letters, 1998, 8 8: Pages 897-902. DOI:
10.1016/s0960-894x(98)00142-5[3] C.A. CHRISTIANSON . Spinal matrix metalloproteinase 3 mediates inflammatory hyperalgesia via a tumor necrosis factor-dependent mechanism[J]. Neuroscience, 2012, 200: Pages 199-210. DOI:
10.1016/j.neuroscience.2011.10.019
aMino]- Structure](https://www.chemicalbook.com/CAS/GIF/161314-17-6.gif)
