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Key Documents

444293

Sigma-Aldrich

MMP-9 Inhibitor II

The MMP-9 Inhibitor II controls the biological activity of MMP-9. This small molecule/inhibitor is primarily used for Biochemicals applications.

Sinónimos:

MMP-9 Inhibitor II, MMP-9 PEX Inhibitor

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About This Item

Fórmula empírica (notación de Hill):
C16H17F2N3O3S
Número de CAS:
Peso molecular:
369.39
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow-white

solubility

DMSO: 50 mg/mL, light yellow

shipped in

ambient

storage temp.

2-8°C

SMILES string

O=C(CSC(NC(CCC)=C1)=NC1=O)NC2=CC=C(OC(F)F)C=C2

General description

This compound is a cell-permeable, selective, and reversible thiopyrimidone MMP-9 allosteric inhibitor that binds specifically to the non-catalytic site of MMP-9 at the PEX domain with a Kd = 2.1 µM and thereby disrupts MMP-9 homodimerization and its cross-talk with CD44 and the EGFR-MAPK signaling pathway. It does not bind to the PEX domain of MMP-2 or MT1-MMP and it is shown to decrease MMP-9 mediated cell migration in COS-1 cells at 100 µM. Also, it inhibits cell migration and invasion of HT-1080 and MDA-MB-435 human cancer cells in a dose-dependent manner from 0.1 to 100 µM, without altering MMP-9 expression or proteolytic activity in HT-1080 cells. In addition, it attenuates both primary tumor growth and metastasis in vivo in a mouse model without obvious toxicity (20 mg/kg, 6 days/week, i.v. and i.t.).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Dufour, A., et al. 2011. Cancer Res.71, 4977.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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Jun-Chao Xue et al.
Translational cancer research, 11(7), 2050-2060 (2022-10-18)
Interleukin-8 (IL-8) and matrix metallopeptidase 9 (MMP9) are overexpressed in hepatocellular carcinoma (HCC), and both are related to tumor metastasis, but whether they regulate HCC metastasis is still unclear. HCC orthotopic implantation and colonization mice models were established in vivo.

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