444293

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.

• Synonym(s): MMP-9 Inhibitor II, MMP-9 PEX Inhibitor
• Empirical Formula (Hill Notation): C₁₆H₁₇F₂N₃O₃S
• CAS Number: 502887-71-0
• Molecular Weight: 369.39
• MDL number: MFCD32671875
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• 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

Description

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 K_d = 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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable