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444293
Sigma-AldrichMMP-9 Inhibitor II - CAS 502887-71-0 - Calbiochem
The MMP-9 Inhibitor II controls the biological activity of MMP-9. This small molecule/inhibitor is primarily used for Biochemicals applications.
More>>The MMP-9 Inhibitor II controls the biological activity of MMP-9. This small molecule/inhibitor is primarily used for Biochemicals applications. Less<<
MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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.).
MMP-9 Inhibitor II - CAS 502887-71-0 - Calbiochem 分析证书
标题
批号
444293
参考
参考信息概述
Dufour, A., et al. 2011. Cancer Res.71, 4977.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
26-April-2012 JSW
Synonyms
MMP-9 PEX Inhibitor
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.).
Form
Yellow-white solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
502887-71-0
Chemical formula
C₁₆H₁₇F₂N₃O₃S
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (50 mg/ml; light yellow solution)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.